Binding molecules for bcma and cd3.
Abstract
The present invention relates to a binding molecule that is at least bispecific, comprising a first and a second binding domain, wherein (a) the first binding domain is capable of binding to the epitope cluster 3 of BCMA, ( CQLRCSSNTPPLTCQRYC); and the second binding domain is capable of binding to the CD3 cell receptor complex; and wherein the cluster of BCMA epitopes 3 corresponds to amino acid residues 24 to 41 of the sequence as shown in SEQ ID NO: 1002.

Term
6.1 yearsleft in the term
Expires 15 November 2032.
- Priority
- Filed
- Granted
- Today
- Expires
52 claims: 50 independent, 2 dependent
- 1REIVINDICACIONES 1. Una molécula de unión la cual es al menos biespecífica que comprende un primer y un segundo dominio de unión, en donde 5 (a) el primer dominio de unión es capaz de unirse al clúster de epítopes 3 de BCMA (CQLRCSSNTPPLTCQRYC); y (b) el segundo dominio de unión es capaz de unirse al complejo CD3 receptor de células T; y en donde el clúster de epítopes 3 de BCMA corresponde a los residuos 10 aminoácidos 24 a 41 de la secuencia tal como se muestra en la SEQ ID NO:1002. 2. La molécula de unión de acuerdo con la reivindicación 1, en donde el primer dominio de unión es capaz de unirse al clúster de epítopes 3 de BCMA de macaco (CQLRCSSTPPLTCQRYC). 3. La molécula de unión de acuerdo con la reivindicación 1 o 2, en donde el segundo dominio de unión es capaz de unirse a CD3 épsilon. 4. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones 20 precedentes, en donde el segundo dominio de unión es capaz de unirse a CD3 humano y a CD3 de macaco. 5. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, en donde el primer y/o el segundo dominio de unión son derivados 25 de un anticuerpo. 240 IMPI INSTITUTO MEXICANO DE LA PROPIEDAD INDUSTRIAL 6. La molécula de unión de acuerdo con la reivindicación 5,13 ¿Uál esta seleccionada a partir del grupo que consiste de (scFv) 2 , (mAb de dominio único) 2 , scFv-mAb de dominio único, diacuerpos y oligómeros de los mismos. 7. Una molécula de unión la cual es al menos biespecífica que comprende un primer y un segundo dominio de unión, en donde (a) el primer dominio de unión es capaz de unirse a BCMA;y (b) el segundo dominio de unión es capaz de unirse al complejo CD3 receptor de células T;y en donde el primer dominio de unión comprende una región VH que comprende CDR-H1, CDR-H2 y CDR-H3 y una región VL que comprende CDR-L1, CDR-L2 y CDR-L3, seleccionados a partir del grupo que consiste en: (1) CDR-H1 tal como se describe en la SEQ ID NO: 1, CDR-H2 tal como se describe en la SEQ ID NO: 2, CDR-H3 tal como se describe en la SEQ ID NO: 3, CDR-L1 tal como se describe en la SEQ ID NO: 4, CDR-L2 tal como se describe en la SEQ ID NO: 5 y CDR-L3 tal como se describe en la SEQ ID NO: 6;
- 2(2) CDR-H1 tal como se describe en la SEQ ID NO:11, CDR-H2 tal como se describe en la SEQ ID NO: 12, CDR-H3 tal como se describe en la SEQ ID NO: 13, CDR-L1 tal como se describe en la SEQ ID NO: 14, CDR-L2 tal como se describe en la SEQ ID NO: 15 y CDR-L3 tal como se describe en la SEQ ID NO: 16;
- 3(3) CDR-H1 tal como se describe en la SEQ ID NO:21, CDR-H2 tal como se describe en la SEQ ID NO: 22, CDR-H3 tal como se describe en la SEQ ID NO: 23, CDR-L1 tal como se describe en la SEQ ID NO: 24, CDR-L2 tal 241 IMPI iNSTnynj muucanu oturaomDAL· industrial como se describe en la SEQ ID NO: 25 y CDR-L3 tal como se describe en la SEQ ID NO: 26;
- 4(4) CDR-H1 tal como se describe en la SEQ ID NO:31, CDR-H2 tal como se describe en la SEQ ID NO: 32, CDR-H3 tal como se describe en la SEQ ID NO: 33, CDR-L1 tal como se describe en la SEQ ID NO: 34, CDR-L2 tal como se describe en la SEQ ID NO: 35 y CDR-L3 tal como se describe en la SEQ ID NO: 36;
- 5(5) CDR-H1 tal como se describe en la SEQ ID NO:41, CDR-H2 tal como se describe en la SEQ ID NO: 42, CDR-H3 tal como se describe en la SEQ ID NO: 43, CDR-L1 tal como se describe en la SEQ ID NO: 44, CDR-L2 tal como se describe en la SEQ ID NO: 45 y CDR-L3 tal como se describe en la SEQ ID NO: 46;
- 6(6) CDR-H1 tal como se describe en la SEQ ID NO:51, CDR-H2 tal como se describe en la SEQ ID NO: 52, CDR-H3 tal como se describe en la SEQ ID NO: 53, CDR-L1 tal como se describe en la SEQ ID NO: 54, CDR-L2 tal como se describe en la SEQ ID NO: 55 y CDR-L3 tal como se describe en la SEQ ID NO: 56;
- 7(7) CDR-H1 tal como se describe en la SEQ ID NO:61, CDR-H2 tal como se describe en la SEQ ID NO: 62, CDR-H3 tal como se describe en la SEQ ID NO: 63, CDR-L1 tal como se describe en la SEQ ID NO: 64, CDR-L2 tal como se describe en la SEQ ID NO: 65 y CDR-L3 tal como se describe en la SEQ ID NO: 66;
- 8(8) CDR-H1 tal como se describe en la SEQ ID NO:71, CDR-H2 tal como se describe en la SEQ ID NO: 72, CDR-H3 tal como se describe en la SEQ ID NO: 73, CDR-L1 tal como se describe en la SEQ ID NO: 74, CDR-L2 tal 242 como se describe en la SEQ ID NO: 75 y ODR-I 3 tal como se describe en la SEQ ID NO: 76;
- 9(9) CDR-H1 tal como se describe en la SEQ ID NO:161, CDR-H2 tal como se describe en la SEQ ID NO: 162, CDR-H3 tal como se describe en la SEQ ID NO: 163, CDR-L1 tal como se describe en la SEQ ID NO: 164, CDR-L2 tal como se describe en la SEQ ID NO: 165 y CDR-L3 tal como se describe en la SEQ ID NO: 166;
- 10(10) CDR-H1 tal como se describe en la SEQ ID NO:171, CDR-H2 tal como se describe en la SEQ ID NO: 172, CDR-H3 tal como se describe en la SEQ ID NO: 173, CDR-L1 tal como se describe en la SEQ ID NO: 174, CDR-L2 tal como se describe en la SEQ ID NO: 175 y CDR-L3 tal como se describe en la SEQ ID NO: 176;
- 11(11) CDR-H1 tal como se describe en la SEQ ID NO:181, CDR-H2 tal como se describe en la SEQ ID NO: 182, CDR-H3 tal como se describe en la SEQ ID NO: 183, CDR-L1 tal como se describe en la SEQ ID NO: 184, CDR-L2 tal como se describe en la SEQ ID NO: 185 y CDR-L3 tal como se describe en la SEQ ID NO: 186;
- 12(12) CDR-H1 tal como se describe en la SEQ ID NO:191, CDR-H2 tal como se describe en la SEQ ID NO: 192, CDR-H3 tal como se describe en la SEQ ID NO: 193, CDR-L1 tal como se describe en la SEQ ID NO: 194, CDR-L2 tal como se describe en la SEQ ID NO: 195 y CDR-L3 tal como se describe en la SEQ ID NO: 196;
- 13(13) CDR-H1 tal como se describe en la SEQ ID NO:201, CDR-H2 tal como se describe en la SEQ ID NO: 202, CDR-H3 tal como se describe en la SEQ ID NO: 203, CDR-L1 tal como se describe en la SEQ ID NO: 204, CDR-L2 tal 243 IMPI INSTITUTO ΜtXICANl. DE LA FBOPIEDAL INDUSTRIA! como se describe en la SEQ ID NO: 205 y CDR4r3-4af-eeme^&e-^®*a4be.^u^ la SEQ ID NO: 206;
- 14(14) CDR-H1 tal como se describe en la SEQ ID NO:211, CDR-H2 tal como se describe en la SEQ ID NO: 212, CDR-H3 tal como se describe en la SEQ ID NO: 213, CDR-L1 tal como se describe en la SEQ ID NO:214 , CDR-L2 tal como se describe en la SEQ ID NO: 215 y CDR-L3 tal como se describe en la SEQ ID NO: 216;
- 15(15) CDR-H1 tal como se describe en la SEQ ID NO:221, CDR-H2 tal como se describe en la SEQ ID NO: 222, CDR-H3 tal como se describe en la SEQ ID NO: 223, CDR-L1 tal como se describe en la SEQ ID NO: 224, CDR-L2 tal como se describe en la SEQ ID NO: 225 y CDR-L3 tal como se describe en la SEQ ID NO: 226;
- 16(16) CDR-H1 tal como se describe en la SEQ ID NO:311, CDR-H2 tal como se describe en la SEQ ID NO: 312, CDR-H3 tal como se describe en la SEQ ID NO: 313, CDR-L1 tal como se describe en la SEQ ID NO: 314, CDR-L2 tal como se describe en la SEQ ID NO: 315 y CDR-L3 tal como se describe en la SEQ ID NO: 316;
- 17(17) CDR-H1 tal como se describe en la SEQ ID NO:321, CDR-H2 tal como se describe en la SEQ ID NO: 322, CDR-H3 tal como se describe en la SEQ ID NO: 323, CDR-L1 tal como se describe en la SEQ ID NO: 324, CDR-L2 tal como se describe en la SEQ ID NO: 325 y CDR-L3 tal como se describe en la SEQ ID NO: 326;
- 18(18) CDR-H1 tal como se describe en la SEQ ID NO:331, CDR-H2 tal como se describe en la SEQ ID NO: 332, CDR-H3 tal como se describe en la SEQ ID NO: 333, CDR-L1 tal como se describe en la SEQ ID NO: 334, CDR-L2 tal 244 IMPI INSTITUTO MIXICAM DF LA FMOHIDAl INDUSTRIA! como se describe en la SEQ ID NO: 335 y nng-i A tai mmn go Pn la SEQ ID NO: 336;
- 19(19) CDR-H1 tal como se describe en la SEQ ID NO:341, CDR-H2 tal como se describe en la SEQ ID NO: 342, CDR-H3 tal como se describe en la SEQ ID NO: 343, CDR-L1 tal como se describe en la SEQ ID NO: 344, CDR-L2 tal como se describe en la SEQ ID NO: 345 y CDR-L3 tal como se describe en la SEQ ID NO: 346;
- 20(20) CDR-H1 tal como se describe en la SEQ ID NO:351, CDR-H2 tal como se describe en la SEQ ID NO: 352, CDR-H3 tal como se describe en la SEQ ID NO: 353, CDR-L1 tal como se describe en la SEQ ID NO: 354, CDR-L2 tal como se describe en la SEQ ID NO: 355 y CDR-L3 tal como se describe en la SEQ ID NO: 356;
- 21(21) CDR-H1 tal como se describe en la SEQ ID NO:361, CDR-H2 tal como se describe en la SEQ ID NO: 362, CDR-H3 tal como se describe en la SEQ ID NO: 363, CDR-L1 tal como se describe en la SEQ ID NO: 364, CDR-L2 tal como se describe en la SEQ ID NO: 365 y CDR-L3 tal como se describe en la SEQ ID NO: 366;
- 22(22) CDR-H1 tal como se describe en la SEQ ID NO:371, CDR-H2 tal como se describe en la SEQ ID NO: 372, CDR-H3 tal como se describe en la SEQ ID NO: 373, CDR-L1 tal como se describe en la SEQ ID NO: 374, CDR-L2 tal como se describe en la SEQ ID NO: 375 y CDR-L3 tal como se describe en la SEQ ID NO: 376;
- 23(23) CDR-H1 tal como se describe en la SEQ ID NO:381, CDR-H2 tal como se describe en la SEQ ID NO: 382, CDR-H3 tal como se describe en la SEQ ID NO: 383, CDR-L1 tal como se describe en la SEQ ID NO: 384, CDR-L2 tal 245 IMPI iRSTmiTO MtXlCANí DF LA PIOPIBUAL INDUSTRIAL como se describe en la SEQ ID NO: 385 y CDR-L3 lál como i>é déscribé en la SEQ ID NO: 386;
- 24(24) CDR-H1 tal como se describe en la SEQ ID NO:581, CDR-H2 tal como se describe en la SEQ ID NO: 582, CDR-H3 tal como se describe en la SEQ ID 5 NO: 583, CDR-L1 tal como se describe en la SEQ ID NO: 584, CDR-L2 tal como se describe en la SEQ ID NO: 585 y CDR-L3 tal como se describe en la SEQ ID NO: 586;
- 25(25) CDR-H1 tal como se describe en la SEQ ID NO:591, CDR-H2 tal como se describe en la SEQ ID NO: 592, CDR-H3 tal como se describe en la SEQ ID 10 NO: 593, CDR-L1 tal como se describe en la SEQ ID NO: 594, CDR-L2 tal como se describe en la SEQ ID NO: 595 y CDR-L3 tal como se describe en la SEQ ID NO: 596;
- 26(26) CDR-H1 tal como se describe en la SEQ ID NO:601, CDR-H2 tal como se describe en la SEQ ID NO: 602, CDR-H3 tal como se describe en la SEQ ID 15 NO: 603, CDR-L1 tal como se describe en la SEQ ID NO: 604, CDR-L2 tal como se describe en la SEQ ID NO: 605 y CDR-L3 tal como se describe en la SEQ ID NO: 606;
- 27(27) CDR-H1 tal como se describe en la SEQ ID NO:611, CDR-H2 tal como se describe en la SEQ ID NO: 612, CDR-H3 tal como se describe en la SEQ ID 20 NO: 613, CDR-L1 tal como se describe en la SEQ ID NO: 614, CDR-L2 tal como se describe en la SEQ ID NO: 615 y CDR-L3 tal como se describe en la SEQ ID NO: 616;
- 28(28) CDR-H1 tal como se describe en la SEQ ID NO:621, CDR-H2 tal como se describe en la SEQ ID NO: 622, CDR-H3 tal como se describe en la SEQ ID 25 NO: 623, CDR-L1 tal como se describe en la SEQ ID NO: 624, CDR-L2 tal 246 IMPI INSTITUTO MtXlCANt DE LA MOHEDA! INDUSTRIA! como se describe en la SEQ ID NO: 625 y CDR-LS talTU!110 se duscribe en la SEQ ID NO: 626;
- 29(29) CDR-H1 tal como se describe en la SEQ ID NO:631, CDR-H2 tal como se describe en la SEQ ID NO: 632, CDR-H3 tal como se describe en la SEQ ID NO: 633, CDR-L1 tal como se describe en la SEQ ID NO: 634, CDR-L2 tal como se describe en la SEQ ID NO: 635 y CDR-L3 tal como se describe en la SEQ ID NO: 636;
- 30(30) CDR-H1 tal como se describe en la SEQ ID NO:641, CDR-H2 tal como se describe en la SEQ ID NO: 642, CDR-H3 tal como se describe en la SEQ ID NO: 643, CDR-L1 tal como se describe en la SEQ ID NO: 644, CDR-L2 tal como se describe en la SEQ ID NO: 645 y CDR-L3 tal como se describe en la SEQ ID NO: 646;
- 31(31) CDR-H1 tal como se describe en la SEQ ID NO:651, CDR-H2 tal como se describe en la SEQ ID NO: 652, CDR-H3 tal como se describe en la SEQ ID NO: 653, CDR-L1 tal como se describe en la SEQ ID NO: 654, CDR-L2 tal como se describe en la SEQ ID NO: 655 y CDR-L3 tal como se describe en la SEQ ID NO: 656;
- 32(32) CDR-H1 tal como se describe en la SEQ ID NO:661, CDR-H2 tal como se describe en la SEQ ID NO: 662, CDR-H3 tal como se describe en la SEQ ID NO: 663, CDR-L1 tal como se describe en la SEQ ID NO: 664, CDR-L2 tal como se describe en la SEQ ID NO: 665 y CDR-L3 tal como se describe en la SEQ ID NO: 666;
- 33(33) CDR-H1 tal como se describe en la SEQ ID NO:671, CDR-H2 tal como se describe en la SEQ ID NO: 672, CDR-H3 tal como se describe en la SEQ ID NO: 673, CDR-L1 tal como se describe en la SEQ ID NO: 674, CDR-L2 tal 247 IMPI tNSTHVTOMEJtlCANt nt u noMtüAi CVfc.XSLJF WITTSIAI como se describe en la SEQ ID NO: 675 y CDR4^4eFeoFfta-&e-d©eGrib®^a la SEQ ID NO: 676;
- 34(34) CDR-H1 tal como se describe en la SEQ ID NO:681, CDR-H2 tal como se describe en la SEQ ID NO: 682, CDR-H3 tal como se describe en la SEQ ID NO: 683, CDR-L1 tal como se describe en la SEQ ID NO: 684, CDR-L2 tal como se describe en la SEQ ID NO: 685 y CDR-L3 tal como se describe en la SEQ ID NO: 686;
- 35(35) CDR-H1 tal como se describe en la SEQ ID NO:691, CDR-H2 tal como se describe en la SEQ ID NO: 692, CDR-H3 tal como se describe en la SEQ ID NO: 693, CDR-L1 tal como se describe en la SEQ ID NO: 694, CDR-L2 tal como se describe en la SEQ ID NO: 695 y CDR-L3 tal como se describe en la SEQ ID NO: 696;
- 36(36) CDR-H1 tal como se describe en la SEQ ID NO:701, CDR-H2 tal como se describe en la SEQ ID NO: 702, CDR-H3 tal como se describe en la SEQ ID NO: 703, CDR-L1 tal como se describe en la SEQ ID NO: 704, CDR-L2 tal como se describe en la SEQ ID NO: 705 y CDR-L3 tal como se describe en la SEQ ID NO: 706;
- 37(37) CDR-H1 tal como se describe en la SEQ ID NO:711, CDR-H2 tal como se describe en la SEQ ID NO: 712, CDR-H3 tal como se describe en la SEQ ID NO: 713, CDR-L1 tal como se describe en la SEQ ID NO: 714, CDR-L2 tal como se describe en la SEQ ID NO: 715 y CDR-L3 tal como se describe en la SEQ ID NO: 716;
- 38(38) CDR-H1 tal como se describe en la SEQ ID NO:721, CDR-H2 tal como se describe en la SEQ ID NO: 722, CDR-H3 tal como se describe en la SEQ ID NO: 723, CDR-L1 tal como se describe en la SEQ ID NO: 724, CDR-L2 tal 248 iNnumiAL como se describe en la SEQ ID NO: 725 y -r-nn L? t? 1 co Racrriho on la SEQ ID NO: 726;
- 39(39) CDR-H1 tal como se describe en la SEQ ID NO:731, CDR-H2 tal como se describe en la SEQ ID NO: 732, CDR-H3 tal como se describe en la SEQ ID NO: 733, CDR-L1 tal como se describe en la SEQ ID NO: 734, CDR-L2 tal como se describe en la SEQ ID NO: 735 y CDR-L3 tal como se describe en la SEQ ID NO: 736;
- 40(40) CDR-H1 tal como se describe en la SEQ ID NO:741, CDR-H2 tal como se describe en la SEQ ID NO: 742, CDR-H3 tal como se describe en la SEQ ID NO: 743, CDR-L1 tal como se describe en la SEQ ID NO: 744, CDR-L2 tal como se describe en la SEQ ID NO: 745 y CDR-L3 tal como se describe en la SEQ ID NO: 746;
- 41(41) CDR-H1 tal como se describe en la SEQ ID NO:751, CDR-H2 tal como se describe en la SEQ ID NO: 752, CDR-H3 tal como se describe en la SEQ ID NO: 753, CDR-L1 tal como se describe en la SEQ ID NO: 754, CDR-L2 tal como se describe en la SEQ ID NO: 755 y CDR-L3 tal como se describe en la SEQ ID NO: 756;
- 42(42) CDR-H1 tal como se describe en la SEQ ID NO:761, CDR-H2 tal como se describe en la SEQ ID NO: 762, CDR-H3 tal como se describe en la SEQ ID NO: 763, CDR-L1 tal como se describe en la SEQ ID NO: 764, CDR-L2 tal como se describe en la SEQ ID NO: 765 y CDR-L3 tal como se describe en la SEQ ID NO: 766;
- 43(43) CDR-H1 tal como se describe en la SEQ ID NO:771, CDR-H2 tal como se describe en la SEQ ID NO: 772, CDR-H3 tal como se describe en la SEQ ID NO: 773, CDR-L1 tal como se describe en la SEQ ID NO: 774, CDR-L2 tal 249 IMPI INSTITUTO MUlCANi OF LA PROPIKDAI iN»urrwiA« como se describe en la SEQ ID NO: 775 y CDR-L3 tal como se describe en la SEQ ID NO: 776;
- 44(44) CDR-H1 tal como se describe en la SEQ ID NO:781, CDR-H2 tal como se describe en la SEQ ID NO: 782, CDR-H3 tal como se describe en la SEQ ID NO: 783, CDR-L1 tal como se describe en la SEQ ID NO: 784, CDR-L2 tal como se describe en la SEQ ID NO: 785 y CDR-L3 tal como se describe en la SEQ ID NO: 786;
- 45(45) CDR-H1 tal como se describe en la SEQ ID NO:791, CDR-H2 tal como se describe en la SEQ ID NO: 792, CDR-H3 tal como se describe en la SEQ ID NO: 793, CDR-L1 tal como se describe en la SEQ ID NO: 794, CDR-L2 tal como se describe en la SEQ ID NO: 795 y CDR-L3 tal como se describe en la SEQ ID NO: 796;
- 46(46) CDR-H1 tal como se describe en la SEQ ID NO:801, CDR-H2 tal como se describe en la SEQ ID NO: 802, CDR-H3 tal como se describe en la SEQ ID NO: 803, CDR-L1 tal como se describe en la SEQ ID NO: 804, CDR-L2 tal como se describe en la SEQ ID NO: 805 y GDR-L3 tal como se describe en la SEQ ID NO: 806;
- 47(47) CDR-H1 tal como se describe en la SEQ ID NO:811, CDR-H2 tal como se describe en la SEQ ID NO: 812, CDR-H3 tal como se describe en la SEQ ID NO: 813, CDR-L1 tal como se describe en la SEQ ID NO: 814, CDR-L2 tal como se describe en la SEQ ID NO: 815 y CDR-L3 tal como se describe en la SEQ ID NO: 816;
- 48(48) CDR-H1 tal como se describe en la SEQ ID NO:821, CDR-H2 tal como se describe en la SEQ ID NO: 822, CDR-H3 tal como se describe en la SEQ ID NO: 823, CDR-L1 tal como se describe en la SEQ ID NO: 824, CDR-L2 tal 250 como se describe en la SEQ ID NO: 825 y nDR-i 3 tal nomo se describe en la SEQ ID NO: 826;
- 49(49) CDR-H1 tal como se describe en la SEQ ID NO:831, CDR-H2 tal como se describe en la SEQ ID NO: 832, CDR-H3 tal como se describe en la SEQ ID NO: 833, CDR-L1 tal como se describe en la SEQ ID NO: 834, CDR-L2 tal como se describe en la SEQ ID NO: 835 y CDR-L3 tal como se describe en la SEQ ID NO: 836, (50) CDR-H1 tal como se describe en la SEQ ID NO: 961, CDR-H2 tal como se describe en la SEQ ID NO: 962, CDR-H3 tal como se describe en la SEQ ID NO: 963, CDR-L1 tal como se describe en la SEQ ID NO: 964, CDR-L2 tal como se describe en la SEQ ID NO: 965 y CDR-L3 tal como se describe en la SEQ ID NO: 966;(51) CDR-H1 tal como se describe en la SEQ ID NO: 971, CDR-H2 tal como se describe en la SEQ ID NO: 972, CDR-H3 tal como se describe en la SEQ ID NO: 973, CDR-L1 tal como se describe en la SEQ ID NO: 974, CDR-L2 tal como se describe en la SEQ ID NO: 975 y CDR-L3 tal como se describe en la SEQ ID NO: 976;(52) CDR-H1 tal como se describe en la SEQ ID NO: 981, CDR-H2 tal como se describe en la SEQ ID NO: 982, CDR-H3 tal como se describe en la SEQ ID NO: 983, CDR-L1 tal como se describe en la SEQ ID NO: 984, CDR-L2 tal como se describe en la SEQ ID NO: 985 y CDR-L3 tal como se describe en la SEQ ID NO: 986;y (53) CDR-H1 tal como se describe en la SEQ ID NO: 991, CDR-H2 tal como se describe en la SEQ ID NO: 992, CDR-H3 tal como se describe en la SEQ ID NO: 993, CDR-L1 tal como se describe en la SEQ ID NO: 994, CDR-L2 tal 251 IMPI ΙΝΠΙΐυΐυ MttlCANl DF LA riOPIFDZO INDUSTRIAL como se describe en la SEQ ID NO: 995 y CDRTJ Tal CUinu se ifesci ¡be onla SEQ ID NO: 996. 8. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, en donde el primer dominio de unión comprende una región VH seleccionada a partir del grupo que consiste de regiones VH tal como se describen en SEQ ID NO: 7, SEQ ID NO: 17, SEQ ID NO: 27, SEQ ID NO: 37, SEQ ID NO: 47, SEQ ID NO: 57, SEQ ID NO: 67, SEQ ID NO: 77, SEQ ID NO: 167, SEQ ID NO: 177, SEQ ID NO: 187, SEQ ID NO: 197, SEQ ID NO: 207, SEQ ID NO: 217, SEQ ID NO: 227, SEQ ID NO: 317, SEQ ID NO: 327, SEQ ID NO: 337, SEQ ID NO: 347, SEQ ID NO: 357, SEQ ID NO: 367, SEQ ID NO: 377, SEQ ID NO: 387, SEQ ID NO: 587, SEQ ID NO: 597, SEQ ID NO: 607, SEQ ID NO: 617, SEQ ID NO: 627, SEQ ID NO: 637, SEQ ID NO: 647, SEQ ID NO: 657, SEQ ID NO: 667, SEQ ID NO: 677, SEQ ID NO: 687, SEQ ID NO: 697, SEQ ID NO: 707, SEQ ID NO: 717, SEQ ID NO: 727, SEQ ID NO: 737, SEQ ID NO: 747, SEQ ID NO: 757, SEQ ID NO: 767, SEQ ID NO: 777, SEQ ID NO: 787, SEQ ID NO: 797, SEQ ID NO: 807, SEQ ID NO: 817, SEQ ID NO: 827, SEQ ID NO: 837, SEQ ID NO: 967, SEQ ID NO: 977, SEQ ID NO: 987, y SEQ ID NO: 997. 9. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, en donde el primer dominio de unión comprende una región VL seleccionada a partir del grupo que consiste de regiones VL tal como se describen en SEQ ID NO: 8, SEQ ID NO: 18, SEQ ID NO: 28, SEQ ID NO: 38, SEQ ID NO: 48, SEQ ID NO: 58, SEQ ID NO: 68, SEQ ID NO: 78, SEQ ID NO: 168, SEQ ID NO: 178, SEQ ID NO: 188, SEQ ID NO: 198, SEQ ID NO: 208, SEQ ID 252 IMPIg instituto muium , nr la nortEDAi INDUSTRIAL NO: 218, SEQ ID NO: 228, SEQ ID NO: 318, SEQfO’NO. 920, GEQ-ID NO: 330, SEQ ID NO: 348, SEQ ID NO: 358, SEQ ID NO: 368, SEQ ID NO: 378, SEQ ID NO: 388, SEQ ID NO: 588, SEQ ID NO: 598, SEQ ID NO: 608, SEQ ID NO: 618, SEQ ID NO: 628, SEQ ID NO: 638, SEQ ID NO: 648, SEQ ID NO: 658, SEQ ID NO: 668, SEQ ID NO: 678, SEQ ID NO: 688, SEQ ID NO: 698, SEQ ID NO: 708, SEQ ID NO: 718, SEQ ID NO: 728, SEQ ID NO: 738, SEQ ID NO: 748, SEQ ID NO: 758, SEQ ID NO: 768, SEQ ID NO: 778, SEQ ID NO: 788, SEQ ID NO: 798, SEQ ID NO: 808, SEQ ID NO: 818, SEQ ID NO: 828, SEQ ID NO: 838, SEQ ID NO: 968, SEQ ID NO: 978, SEQ ID NO: 988, y SEQ ID NO: 998. 10. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, en donde el primer dominio de unión comprende una región VH y una región VL seleccionada a partir del grupo que consiste en: (1) una región VH tal como se describe en la SEQ ID NO: 7, y una región VL tal como se describe en la SEQ ID NO: 8;(2) una región VH tal como se describe en la SEQ ID NO: 17, y una región VL tal como se describe en la SEQ ID NO: 18;(3) una región VH tal como se describe en la SEQ ID NO: 27, y una región VL tal como se describe en la SEQ ID NO: 28;(4) una región VH tal como se describe en la SEQ ID NO: 37, y una región VL tal como se describe en la SEQ ID NO: 38;(5) una región VH tal como se describe en la SEQ ID NO: 47, y una región VL tal como se describe en la SEQ ID NO: 48;(6) una región VH tal como se describe en la SEQ ID NO: 57, y una región VL tal como se describe en la SEQ ID NO: 58;IMPI IMSTTTUtC MUiCanl mí la promedai iNpumiAi (7) una región VH tal como se describe en la SFQJD NO: 67, y una región VL tal como se describe en la SEQ ID NO: 68;(8) una región VH tal como se describe en la SEQ ID NO: 77, y una región VL tal como se describe en la SEQ ID NO: 78;(9) una región VH tal como se describe en la SEQ ID NO: 167, y una región VL tal como se describe en la SEQ ID NO: 168;(10) una región VH tal como se describe en la SEQ ID NO: 177, y una región VL tal como se describe en la SEQ ID NO: 178;(11) una región VH tal como se describe en la SEQ ID NO: 187, y una región VL tal como se describe en la SEQ ID NO: 188;(12) una región VH tal como se describe en la SEQ ID NO: 197, y una región VL tal como se describe en la SEQ ID NO: 198;(13) una región VH tal como se describe en la SEQ ID NO: 207, y una región VL tal como se describe en la SEQ ID NO: 208;(14) una región VH tal como se describe en la SEQ ID NO: 217, y una región VL tal como se describe en la SEQ ID NO: 218;(15) una región VH tal como se describe en la SEQ ID NO: 227, y una región VL tal como se describe en la SEQ ID NO: 228;(16) una región VH tal como se describe en la SEQ ID NO: 317, y una región VL tal como se describe en la SEQ ID NO: 318;(17) una región VH tal como se describe en la SEQ ID NO: 327, y una región VL tal como se describe en la SEQ ID NO: 328;(18) una región VH tal como se describe en la SEQ ID NO: 337, y una región VL tal como se describe en la SEQ ID NO: 338;254 institutomexicano DE LA MO P1 EDA I industrial (19) una región VH tal como se describe en la SEQ ID NO: 347, y una región VL tal como se describe en la SEQ ID NO: 348;(20) una región VH tal como se describe en la SEQ ID NO: 357, y una región VL tal como se describe en la SEQ ID NO: 358;(21) una región VH tal como se describe en la SEQ ID NO: 367, y una región VL tal como se describe en la SEQ ID NO: 368;(22) una región VH tal como se describe en la SEQ ID NO: 377, y una región VL tal como se describe en la SEQ ID NO: 378;(23) una región VH tal como se describe en la SEQ ID NO: 387, y una región VL tal como se describe en la SEQ ID NO: 388;(24) una región VH tal como se describe en la SEQ ID NO: 587, y una región VL tal como se describe en la SEQ ID NO: 588;(25) una región VH tal como se describe en la SEQ ID NO: 597, y una región VL tal como se describe en la SEQ ID NO: 598;(26) una región VH tal como se describe en la SEQ ID NO: 607, y una región VL tal como se describe en la SEQ ID NO: 608;(27) una región VH tal como se describe en la SEQ ID NO: 617, y una región VL tal como se describe en la SEQ ID NO: 618;(28) una región VH tal como se describe en la SEQ ID NO: 627, y una región VL tal como se describe en la SEQ ID NO: 628;(29) una región VH tal como se describe en la SEQ ID NO: 637, y una región VL tal como se describe en la SEQ ID NO: 638;(30) una región VH tal como se describe en la SEQ ID NO: 647, y una región VL tal como se describe en la SEQ ID NO: 648;255 ÍMPI INSTITUTO MEJUCANc PELA «OPIEDAI (31) una región VH tal como se describe en la SEQ ID NO: 657, y una región VL tal como se describe en la SEQ ID NO: 658;(32) una región VH tal como se describe en la SEQ ID NO: 667, y una región VL tal como se describe en la SEQ ID NO: 668;(33) una región VH tal como se describe en la SEQ ID NO: 677, y una región VL tal como se describe en la SEQ ID NO: 678;(34) una región VH tal como se describe en la SEQ ID NO: 687, y una región VL tal como se describe en la SEQ ID NO: 688;(35) una región VH tal como se describe en la SEQ ID NO: 697, y una región VL tal como se describe en la SEQ ID NO: 698;(36) una región VH tal como se describe en la SEQ ID NO: 707, y una región VL tal como se describe en la SEQ ID NO: 708;(37) una región VH tal como se describe en la SEQ ID NO: 717, y una región VL tal como se describe en la SEQ ID NO: 718;(38) una región VH tal como se describe en la SEQ ID NO: 727, y una región VL tal como se describe en la SEQ ID NO: 728;(39) una región VH tal como se describe en la SEQ ID NO: 737, y una región VL tal como se describe en la SEQ ID NO: 738;(40) una región VH tal como se describe en la SEQ ID NO: 747, y una región VL tal como se describe en la SEQ ID NO: 748;(41) una región VH tal como se describe en la SEQ ID NO: 757, y una región VL tal como se describe en la SEQ ID NO: 758;(42) una región VH tal como se describe en la SEQ ID NO: 767, y una región VL tal como se describe en la SEQ ID NO: 768;256 INSTITUTO MIXICANC DE LA EROPIIDAT INDUSTRIA I (43) una región VH tal como se describe en la SECTIL· NU. / / /, y una'ieyiún Vfe· tal como se describe en la SEQ ID NO: 778;(44) una región VH tal como se describe en la SEQ ID NO: 787, y una región VL tal como se describe en la SEQ ID NO: 788;(45) una región VH tal como se describe en la SEQ ID NO: 797, y una región VL tal como se describe en la SEQ ID NO: 798;(46) una región VH tal como se describe en la SEQ ID NO: 807, y una región VL tal como se describe en la SEQ ID NO: 808;(47) una región VH tal como se describe en la SEQ ID NO: 817, y una región VL tal como se describe en la SEQ ID NO: 818;(48) una región VH tal como se describe en la SEQ ID NO: 827, y una región VL tal como se describe en la SEQ ID NO: 828;(49) una región VH tal como se describe en la SEQ ID NO: 837, y una región VL tal como se describe en la SEQ ID NO: 838;
- 50(50) una región VH tal como se describe en la SEQ ID NO:967, y una región VL tal como se describe en la SEQ ID NO: 968;
- 51(51) una región VH tal como se describe en la SEQ ID NO:977, y una región VL tal como se describe en la SEQ ID NO: 978;
- 52(52) una región VH tal como se describe en la SEQ ID NO:987, y una región VL tal como se describe en la SEQ ID NO: 988;y (53) una región VH tal como se describe en la SEQ ID NO: 997, y una región VL tal como se describe en la SEQ ID NO: 998. 11. La molécula de unión de acuerdo con la reivindicación 10, en donde el primer dominio de unión comprende una secuencia de aminoácidos seleccionada a partir 257 IMPI fNSTnvrOMEXICAN· ne la pkopiedai· INriVSTRlAl del grupo que consiste en SEQ ID NO: 9, SEQ ID N(J? 19, ótQ IU NU! 29, SEQ I& NO: 39, SEQ ID NO: 49, SEQ ID NO: 59, SEQ ID NO: 69, SEQ ID NO: 79, SEQ ID NO: 169, SEQ ID NO: 179, SEQ ID NO: 189, SEQ ID NO: 199, SEQ ID NO: 209, SEQ ID NO: 219, SEQ ID NO;229, SEQ ID NO: 319, SEQ ID NO: 329, SEQ ID NO: 339, SEQ ID NO: 349, SEQ ID NO: 359, SEQ ID NO: 369, SEQ ID NO: 379, SEQ ID NO: 389, SEQ ID NO: 589, SEQ ID NO: 599, SEQ ID NO: 609, SEQ ID NO: 619, SEQ ID NO: 629, SEQ ID NO: 639, SEQ ID NO: 649, SEQ ID NO: 659, SEQ ID NO: 669, SEQ ID NO: 679, SEQ ID NO: 689, SEQ ID NO: 699, SEQ ID NO: 709, SEQ ID NO: 719, SEQ ID NO: 729, SEQ ID NO: 739, SEQ ID NO: 749, SEQ ID NO: 759, SEQ ID NO: 769, SEQ ID NO: 779, SEQ ID NO: 789, SEQ ID NO: 799, SEQ ID NO: 809, SEQ ID NO: 819, SEQ ID NO: 829, SEQ ID NO: 839, SEQ ID NO: 969, SEQ ID NO: 979, SEQ ID NO: 989, y SEQ ID NO: 999. 12. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones 1-6 que tiene la secuencia de aminoácidos que se describe en la SEQ ID NO: 340 o la SEQ ID NO: 980. 13. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, caracterizada por un EC 50 (pg/ml) de 350 o menor, preferiblemente 320 o menor. 14. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones precedentes, caracterizada por un EC 50 (pg/ml) el cual ¡guala el EC 50 (pg/ml) de uno cualquiera de BC E5 33-B11-B8, BC 5G9 92-E10, BC 5G9 91-D2-B10, BC 258 INSTTTVfO MU¡CAN< / M LA PROPIEDAD fMDI JST»IAL B12 33-A4-B2, BC 3A4 37-A11-G1, BC A7-27 C4-G7·, DO 00 034)7431,00 03 33·F8-E6B1. 15. Una secuencia de ácido nucleico que codifica una molécula de unión tal como se 5 define en una cualquiera de las reivindicaciones 1 a 14 16. Un vector que comprende una secuencia de ácido nucleico tal como se define en la reivindicación 15. 10 17. Una célula hospedadora transformada o transfectada con la secuencia de ácido nucleico tal como se define en la reivindicación 15 o con el vector tal como se define en la reivindicación 16. 18. Un procedimiento para la producción de una molécula de unión de acuerdo con 15 una cualquiera de las reivindicaciones 1 a 14, comprendiendo dicho proceso cultivar una célula hospedadora tal como se define en la reivindicación 17 bajo condiciones que permitan la expresión de la molécula de unión tal como se define en una cualquiera de las reivindicaciones 1 a 14 y recuperar la molécula de unión producida a partir del cultivo. 19. Una composición farmacéutica que comprende una molécula de unión de acuerdo con una cualquiera de las reivindicaciones 1 a 14, o producida de acuerdo con el procedimiento de la reivindicación 18. 1 I 259 IMPI PF la wdustriaT 20. La molécula de unión de acuerdo con una cualq ivindicaciones 1 a 14, o producida de acuerdo con el procedimiento de la reivindicación 18 para su uso en la prevención, tratamiento o mejora de una enfermedad seleccionada a partir del grupo que consiste en trastornos de células plasmáticas, otros trastornos 5 de células B que se correlacionan con la expresión de BCMA y enfermedades autoinmunes. 21. La molécula de unión de acuerdo con una cualquiera de las reivindicaciones 1 a 14 para usarse en el tratamiento de trastornos de células plasmáticas, otros 10 trastornos de células B que se correlacionan con la expresión de BCMA y enfermedades autoinmunes en un sujeto en necesidad del mismo. 22. La molécula de unión para usarse de acuerdo con la reivindicación 21, en donde el trastorno de células plasmáticas está seleccionado a partir del grupo que consiste 15 en mieloma múltiple, plasmocitoma, leucemia de células plasmáticas, macroglobulinemia, amiloidosis, macroglobulinemia de Waldenstrom, plasmocitoma óseo solitario, plasmocitoma extramedular, mieloma osteosclerótico, las enfermedades de la cadena pesada, la gamopatía monoclonal de significado incierto y mieloma múltiple latente. 23. La molécula de unión para usarse de acuerdo con la reivindicación 21, en donde la enfermedad autoinmune es lupus eritematoso sistémico. 24. Un kit que comprende una molécula de unión tal como se define en una cualquiera 25 de las reivindicaciones 1 a 14, una molécula de ácido nucleico tal como se define 260 IMPI IM«TTmW MÍXICAN<' ΓΕ LA PltOmOAD INDUmiAL en la reivindicación 15, un vector tal como se define en-la Ιΰίνΐιιόίϋ3~ϋ1όη 16, y/o una célula hospedadora tal como se define en la reivindicación 17. 25. Uso de la molécula de unión de acuerdo con una cualquiera de las reivindicaciones 1 a 14, para la preparación de un medicamento para el tratamiento de trastornos de células plasmáticas, otros trastornos de células B que se correlacionan con la expresión de BCMA y enfermedades autoinmunes en un sujeto en necesidad del mismo. 26. El uso de acuerdo con la reivindicación 25, en donde el trastorno de células plasmáticas está seleccionado a partir del grupo que consiste en mieloma múltiple, plasmocitoma, leucemia de células plasmáticas, macroglobulinemia, amiloidosis, macroglobulinemia de Waldenstrom, plasmocitoma óseo solitario, plasmocitoma extramedular, mieloma osteosclerótico, las enfermedades de la cadena pesada, la gamopatía monoclonal de significado incierto y mieloma múltiple latente. 27. El uso de acuerdo con la reivindicación 25, en donde la enfermedad autoinmune es lupus eritematoso sistémico. 261 IMPI INSTITUTO MBUCANC DF LA PÍ0P1EDAÍ ινγμ»<γπ»ιαι
Independent claims52
2,428 paragraphs in 217 sections, as filed
(54) Title: UNION MOLECULES FOR PUMP AND CD3.
(54) Title: BINDING MOLECULES FOR BCMA AND CD3.
(57) Summary
The present invention relates to a binding molecule that is at least bispecific, comprising a first and a second binding domain, wherein (a) the first binding domain is capable of binding to the BCMA 3 epitope cluster, ( CQLRCSSNTPPLTCQRYC); and the second binding domain is capable of binding to the CD3 T cell receptor complex; and where BCMA epitope cluster 3 corresponds to amino acid residues 24 to 41 of the sequence as shown in SEQ ID NO: 1002.
(57) Abstract
The present invention relates to a binding molecule which is at least bispecific comprising a first and a second binding domain, wherein the first binding domain is capable of binding to epitope cluster3 of BCMA, and the second binding domain is capable of binding to the Tcell CD3 receptor complex. Moreover, the invention provides a nucleic acid sequence encoding the binding molecule, a vector comprising said nucleic acid sequence and a host cell transformed or transfected with said vector. Furthermore, the invention provides a process for the production of the binding molecule of the invention, a medical use of said binding molecule and a kit comprising said binding molecule.
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PATENT TITLE No. 349396
AMGEN RESEARCH (MUNICH) GMBH; BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Address: Staffelseestrasse 2, 81477, Munich, GERMANY
Name: BINDING MOLECULES FOR BCMA AND CD3.
<td>Classification: CIP:</td><td>C07K16 / 28; A61K39 / 395, C07K14 / 575; C07K14 / 705; C07K16 / 46</td>
<td>CPC:</td><td>C07K16 / 2875; C07K14 / 70578; C07K16 / 468; C07K16 / 2809; C07K16 / 2878</td>
Inventor (s): PETER KUFER; TOBIAS RAUM; PATRICK HOFFMANN; ROMAN KISCHEL; RALF
LUTTERBUESE; DORIS RAU; PAUL ADAM; ERIC BORGES; * *
<td>Number: MX / a / 2014/005852</td><td>REQUEST International Presentation Date: November 15, 2012</td>
PRIORITY*
<td>Country:</td><td>Date:</td><td>Number:</td>
<td>US</td><td>November 15, 2011</td><td> 61/560,144</td>
<td>US</td><td>November 15, 2011</td><td> 61/560,149</td>
Validity: Twenty years
Expiration Date: November 15, 2032
Issue Date: July 26, 2017
The reference patent is granted based on articles 1, 2, section V, 6<sup>or</sup> fraction OI, and 89 of the Industrial Property Law.
In accordance with article 23 of the Industrial Property Law, this patent is valid for twenty years, non-extendable, counted from the filing date of the international application and will be subject to the payment of the fee to keep the rights in force. .
Whoever signs this title does so based on the provisions of articles 6<sup>or</sup> Sections III and 7 bis 2 of the Industrial Property Law (Official Gazette of the Federation (DOF) 06/27/1991, amended on 08/02/1994, 10/25/1996, 12/26/1997, 17 / 05/1999, 01/26/2004, 06/16/2005, 01/25/2006, 05/06/2009, 06/01/2010, 06/06/2010, 06/28/2010, 01/27 / 2012 and 04/09/2012); Articles 1, 3 “fraction V subsection a), 4<sup>or</sup> and 12th sections I and III of the Regulations of the Mexican Institute of Industrial Property (DOF 12/14/1999, amended on 07/01/2002, 07/15/2004, 07/28/2004 and 09/07/2007) ; items 1<sup>or</sup>, 3“, 4”, 5<sup>or</sup> fraction V subsection a), 16 sections l and III and 30 of the Organic Statute of the Mexican Institute of Industrial Property (DOF 12/27/1999, amended on 10/10/2002, 07/29/2004, 04818/2004 and 09/13/2007); 1 ', 3 · and 5 * subsection a) of the Agreement that delegates powers to the Deputy General Directors, Coordinator, Divisional Directors, Heads of Regional Offices ....., Divisional Deputy Directors, Departmental Coordinators and other subordinates of the Mexican Institute of Industrial Property. -fDrO.F. 12/15/1999, amended on 02/04/2000, 07/29/2004, 08/04/2004 and 09/13/2007).
This document is signed with an advanced electronic signature (FIEL), based on articles 7 BIS 2 of the Industrial Property Law; 3 of its Regulations, and 1 section III, 2 section V, 26 BIS and 26 TER of the Agreement establishing the guidelines for the use of the Payment and Electronic Services Portal (PASE) of the Mexican Institute of Industrial Property, in the procedures indicated.
THE DIVISIONAL DIRECTOR OF PATENTS
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(55) 53340700 www.gob.mx/¡nipi
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MEXICAN INSTITUTE
PE LA PROP1EDA d INDUSTRIAL
BINDING MOLECULES FOR BCMA AND CD3
The present invention relates to a binding molecule that is at least bispecific comprising a first and a second binding domain, wherein the first binding domain is capable of binding to the BCMA epitope 3 cluster, and the second domain of binding is capable of binding to the CD3 receptor complex of T cells. Furthermore, the invention provides a nucleic acid sequence encoding the binding molecule, a vector comprising said nucleic acid sequence and a host cell transformed or transfected with said vector. Furthermore, the invention provides a process for the production of the binding molecule of the invention, a medical use of said binding molecule and a kit comprising said binding molecule.
BCMA (B cell maturation antigen, TNFRSF17, CD269) is a transmembrane protein that belongs to the super family of TNF receptors. BCMA is originally reported as an integral membrane protein in the Golgi apparatus of mature human B lymphocytes, that is, as an intracellular protein (Gras et al., (1995) International Immunol 7 (7): 1093-1105) showing that BCMA appears to play an important role during B cell development and homeostasis. The finding of Gras et al. could be associated with the fact that the BCMA protein that was described in Gras et al. it is, due to a chromosomal translocation, a fusion protein between BCMA and IL2. In the meantime, however, it has been established that BCMA is, a B cell marker that is essential for B cell development and homeostasis (Schliemann et al., (2001) Science 293 (5537): 2111-2114) due to its interaction presumably essential with its ligand BAFF (B cell activating factor), also designated as TALL-1 or TNFSF13B, and APRIL (proliferation inducing ligand A).
IMPI
MEXICAN INSTITUTE
OF INDUSTRIAL PROPERTY
<img file="MX349396B_D0004.tif" />
BCMA expression is restricted to the B cell lineage and is present mainly in plasma cells and plasmoblasts and to some extent in B cells of<sup>-</sup> memory, but is virtually absent in naive and peripheral B cells. BCMA is also expressed in multiple myeloma (MM) cells. Together with members of its membrane activator and ligand cyclophilin interactor (TACI) family and the B-cell activating factor of the TNF receptor family (BAFF-R), BCMA regulates different aspects of humoral, developmental, and immunity. cell homeostasis. BCMA expression appears rather late in B-cell differentiation and contributes to the long-term survival of plasmoblasts and plasma cells in the bone marrow. The targeted deletion of the BCMA gene in mice does not affect the generation of mature B cells, the quality and magnitude of humoral immune responses, the formation of germinal centers, or the generation of short-lived plasma cells. However, such mice have significantly reduced numbers of long-lived plasma cells in the bone marrow, indicating the importance of BCMA for their survival (O'Connor et al., 2004).
In line with these findings, BCMA also supports the growth and survival of multiple myeloma (MM) cells. Novak et al. found that MM cell lines and newly isolated MM cells express BCMA and TACI protein on their cell surfaces and have variable expression of BAFF-R protein on their cell surface (Novak et al., (2004) Blood 103 (2): 689-694 ).
Multiple myeloma (MM) is the second most common hematologic malignancy, accounting for 2% of all cancer deaths. MM is a heterogeneous disease and caused mostly by chromosomal translocations among others t (11; 14), t (4; 14), t (8; 14), del (13), del (17) (Drach et al. , (1998) Blood 92 (3): 802-809; Gertz et al., (2005) Blood 106 (8): 2837-2840; Facón et al., (2001) Blood 97 (6): 1566-1571) . The
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INSTrn / To MOJCANI OE LA EBOHEDAL industrial MM patients may experience a variety of symptoms related to the disease, due to bone marrow infiltration, bone destruction, kidney failure, immunodeficiency, and the psychosocial burden of a cancer diagnosis. As of 2006, the 5-year relative survival rate for MM was approximately 34% highlighting that MM is a difficult disease to treat where there are currently no curative options.
Promising new treatments such as chemotherapy and stem cell transplantation are becoming available and survival rates have improved, but often bring unwanted side effects and therefore MM is still incurable (Lee et al., (2004) J Nati Compr Cañe Netw 8 (4): 379-383). To date, the two most frequently used treatment options for patients with multiple myeloma are combinations of spheroids, thalidomide, lenalidomide, bortezomib, or various cytotoxic agents, and for younger patients, high-dose chemotherapy concepts with autologous cell transplantation mother.
Most transplants are of the autologous type, that is, using the patient's own cells. Transplants of this type, although not curative, have been shown to prolong life in some patients. They can be carried out as initial therapy in newly diagnosed patients or at the time of relapse. Sometimes, in certain patients, more than one transplant may be recommended to adequately control the disease.
The chemotherapeutic agents used to treat the disease are cyclophosphamide, doxorubicin, vincristine, and melphalan; Combination therapies with immunomodulatory agents such as thalidomide (Thalomid ®), lenalidomide (Revlimid ®), bortezomib (Velcade ®), and corticosteroids (eg, dexamethasone) have become important options for the treatment of myeloma, both in patients
INSTITUTO MBUCaNC DE LA moHÍDAt recently diagnosed as in patients with advanced disease who have failed chemotherapy or transplantation. * '—The therapies currently used are generally non-curative. Stem cell transplantation may not be an option for many patients due to advanced age, the presence of another serious illness, or other physical limitations. Chemotherapy only partially controls multiple myeloma, rarely leading to complete remission. Therefore, there is an urgent need for new innovative treatments.
Bellucci et al. (Blood, 2005; 105 (10) identified BCMA-specific antibodies in multiple myeloma patients after they had received donor lymphocyte infusions (DLI). Serum from these patients was able to mediate BCMA-specific cell lysis by ADCC and CDC and it was detected only in patients with antitumor responses (4/9), but not in non-responders (0/6). The authors speculate that induction of BCMA-specific antibodies contributes to the clearance of myeloma cells and long-term remission in patients.
Ryan et al. (Mol. Cancer Ther 2007; 6 (11)) reported the generation of a BCMA-specific antagonist antibody that prevents the activation of NF-κΒ that is associated with a potent pro-survival signaling pathway in normal and malignant B cells. Furthermore, the antibody conferred potent antibody-mediated cell-dependent cytotoxicity (ADCC) to multiple myeloma cell lines, in vitro, which was significantly enhanced by Fe engineering.
Other approaches in the fight against tumors present in the blood or autoimmune disorders focus on the interaction between BAFF and APRIL, that is, ligands of the super family of ligands TNF, and their receptors TACI, BAFF-R and BCMA, which are activated by BAFF and / or APRIL. For example, by fusing the Fe domain of human immunoglobulin to TACI, Zymogenetics, Inc. has generated Atacicept (TACI-lg)
<img file="MX349396B_D0005.tif" />
INÍTTTUTO MBtICANQ jk to neutralize these two ligands and prevent the activation of O ^ gJft ^^ táq ^ e ^ currently in clinical trials for the treatment of systemic lupus erythematosus (SLE, phase III), multiple sclerosis (MS, phase II) and rheumatoid arthritis (RA, phase II), as well as in phase I clinical trials for the treatment of B-cell neoplasia, chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL) and MM. In preclinical studies, atacicept reduces the growth and survival of primary MM cells and MM cell lines in vitro (Moreaux et al, Blood, 2004, 103) and in vivo (Yaccoby et al., Leukemía, 2008, 22, 406 -13), demonstrating the relevance of TACI ligands for MM cells. Since most MM cells and derived cell lines express BCMA and TACI, both receptors could contribute to ligand-mediated growth and survival. These data suggest that antagonizing both BCMA and TACI could be beneficial in the treatment of plasma cell disorders. Furthermore, BCMA-specific antibodies that cross-react with TACI have been described (WO 02/066516).
Human Genome Sciences and GlaxoSmithKIine have developed an antibody directed at BAFF called Belimumab. Belimumab blocks the binding of soluble BAFF to its BAFF-R, BCMA and TACI receptors in B cells. Belimumab does not bind directly to B cells, but by binding to BAFF, belimumab inhibits the survival of B cells, including cells. B autoreactive, and reduces the differentiation of B cells into immunoglobulin-producing plasma cells.
However, despite the fact that BCMA; BAFF-R and TACI, that is, B cell receptors belonging to the TNF receptor super family, and their ligands BAFF and
APRIL are used in therapies in the fight against cancer and / or autoimmune disorders, there is still a need to have other options available for the treatment of such medical conditions.
<sup>6</sup>
MBlCANQ INSTITUTE
Í'E INDUSTRIAL PROPERTY
Accordingly, means and methods for solving this problem are provided herein in the form of an at least bispecific binding molecule with a cytotoxic cell binding domain, i.e. cytotoxic T cells, and with a second domain of binding to BCMA.
Thus, in a first aspect the present invention provides a binding molecule that is at least bispecific comprising a first and a second binding domain, wherein (a) the first binding domain is capable of binding to the epitope 3 cluster of BCMA (CQLRCSSNTPPLTCQRYC) (SEQ ID NO: 1016); and (b) the second binding domain is capable of binding to the CD3 T cell receptor complex; and wherein the BCMA epitope cluster 3 corresponds to amino acid residues 24 to 41 of the sequence represented in SEQ ID NO: 1002.
***
It should be noted that, as used herein, the singular forms a, an, and the, include plural references unless the context clearly indicates otherwise. Thus, for example, reference to a reagent includes one or more of these different reagents and reference to method includes reference to equivalent steps and methods known to those of ordinary skill in the art that could be modified or substituted by the methods described. at the moment.
Unless stated otherwise, the term at least preceding a series of elements is to be understood as referring to all elements of the series. Those skilled in the art will recognize, or be able to determine using no more than routine experimentation, many equivalents to specific embodiments of the
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INSTITUTE MaOCANC DE LA PROPERTY inoustuial invention described herein. Such equivalents are intended to be encompassed by the present invention.
The term and / or where used herein includes the meaning of and, or and all or any other combination of the elements connected by such term.
The term "about or about as used herein means within ± 20%, preferably within ± 15%, more preferably within ± 10%, and even more preferably within ± 5% of a given value or range.
Throughout this description and the claims that follow, unless the context requires otherwise, the word comprise, and variations such as comprises and comprising, will be understood to imply the inclusion of an integer or step stated or group of whole numbers or stages but not the exclusion of any other whole number or stage or group of whole numbers or stages. When used herein the term comprising may be substituted with the term containing or including or, sometimes when used herein, with the term having.
When used herein that consists of excludes any unspecified element, step, or ingredient in the claimed element. When used herein, it essentially consists of not excluding materials or steps that do not materially affect the basic and novel features of the claim.
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In each instance in the present description, any of the terms comprising, consisting essentially of, and consisting of may be substituted with udlÍ | UIUI U I3é the other two terms.
Epitope cluster 3 is comprised in the extracellular domain of BCMA. The extracellular domain of BCMA or ECD of BCMA refers to a form of BCMA that is essentially free of the transmembrane and cytoplasmic domains of BCMA. It will be understood by those skilled in the art that the transmembrane domain identified for the BCMA polypeptide of the present invention is identified in accordance with the criteria routinely used in the art to identify that type of hydrophobic domain. The exact boundaries of a transmembrane domain can vary, but more likely by no more than about 5 amino acids at either end of the domain specifically mentioned in the present disclosure. A preferred BCMA ECD is shown in SEQ ID NO: 1007.
The CD3 T cell receptor complex is a protein complex and is made up of four distinct chains. In mammals, the complex contains one CD3y chain, one CD3o chain, and two CD3e (epsilon) chains. These chains associate with a molecule known as a T cell receptor (TCR) and with the ζ chain to generate an activation signal in T lymphocytes.
The redirected lysis of target cells through T cell recruitment by bispecific molecules involves the formation of cytolytic synapses and the release of perforin and granzymes. Involved T cells are capable of serial lysis
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IIWTITI rro MtxiCAN »Oí INDUSTRIAL PROPERTY of target cells, and are not affected by immune escape mechanisms that interfere with the processing and presentation of peptide antigens, or clonal differentiation of T cells, see, for example, WO 2007/042261 .
The term "binding molecule" in the sense of the present description indicates any molecule capable of (specifically) binding to, or interacting with or recognizing the target molecules BCMA and CD3. In accordance with the present invention, the binding molecules are preferably polypeptides. Such polypeptides can include protein and non-protein moieties (eg, chemical ligands or chemical crosslinking agents such as glutaraldehyde).
A binding molecule can be said to provide the scaffold for said one or more binding domains so that said binding domains can bind / interact with the target molecules BCMA and CD3. For example, such a scaffold could be provided by protein A, and in particular, its Z domain (affibodies), lmmE7 (immunity proteins), BPTI / APPI (Kunitz domains), AF-6 protein that binds a Ras (PDZ domains), charibdotoxin (scorpion toxin), CTLA-4, Min-23 (knottins), lipocalins (anticalins), neocarcinostatin, a fibronectin domain, an ankyrin or thioredoxin consensus repeat domain (Skerra, Curr. Opin. BiotechnoL 18, 295-304 (2005); Hosse et 20 al., Protein Sci. 15, 14-27 (2006); Nícaise et al., Protein Scí. 13, 1882-1891 (2004);
Nygren and Uhlen, Curr. Opin. Struc. Biol. 7, 463-469 (1997)). A preferred binding molecule is an antibody.
It is contemplated that the binding molecule is produced by (or can be obtained by) phage display or library screening methods rather than
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by grafting CDR sequences from a pre-existing (monoclonal) antibody into a scaffold, eg, a scaffold as described herein.
The term "bispecific" as used herein refers to a binding molecule comprising at least a first and a second binding domain, wherein the first domain is capable of binding to an antigen or target, and the second binding domain it is capable of binding to another antigen or target. The binding molecule of the invention also comprises multispecific binding molecules, such as, for example, trispecific binding molecules, the latter including three binding domains.
It is also contemplated that the binding molecule of the invention has, in addition to its function of binding to target molecules BCMA and CD3, an additional function. In this format, the binding molecule is a tri-or multifunctional binding molecule by targeting plasma cells through binding to BCMA, mediating cytotoxic activity of T cells through binding to CD3, and providing a functional function. additional, such as a fully functional Fe constant domain that mediates antibody-dependent cellular cytotoxicity through recruitment of effector cells such as NK cells, a tag (fluorescent, etc), a therapeutic agent, such as, for example, a toxin or radionuclide, and / or means to increase the serum half-life, etc.
The term "domain or binding" characterizes in relation to the present invention a domain that is capable of specifically binding to / interacting with a given target epitope or a given target site on the BCMA and CD3 target molecules.
ΙΜΚΤΤηπν MEXICAN. . ... .. ... ... pE u «OPIEDAR O» <«3lJU
The binding domains can be derived from a binding domain? Ftsmrrte tarcomE? R for example an antibody, protein A, lmmE7 (
Kunitz), Ras-binding protein AF-6 (PDZ domains), charybdotoxin (scorpion toxin), CTLA-4, Min-23 (knottins), lipocalins (anticalins), neocarcinostatin, a fibronectin domain, a repeat domain consensus of ankyrin or thioredoxin (Skerra, Curr. Opin. Biotechnol. 18, 295-304 (2005); Hosse et al., Protein Sci. 15, 14-27 (2006); Nicaise et al., Protein Sci. 13, 1882-1891 (2004); Nygren and Uhlen, Curr. Opin. Struc. BioL 7, 463-469 (1997)). A preferred binding domain is derived from an antibody. It is contemplated that a binding domain of the present invention comprises at least such part of any of the aforementioned binding domains that is required to bind / interact with a given target epitope or a given target site of the BCMA and CD3 target molecules. .
It is contemplated that the binding domain of the aforementioned binding domain donors is characterized by that part of these donors that is responsible for binding to the respective target, that is, when that part is removed from the binding domain donor, said donor loses its ability to bond. Lose means a reduction of at least 50% in binding capacity compared to donor binding. Methods for mapping these binding sites are well known in the art - therefore it is within the standard knowledge of the skilled person to locate / map the binding site of a binding domain donor and therefore derive said domain. binding from the respective binding domain donors.
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INSTITUTE MRXICANi. J>)
OF Ά PROPERTY
INDUSTRY! ** W -
The term "epitope" refers to a site on the antigen to which a binding domain, such as an antibody or immunoglobulin or derivative or fragment of an antibody or immunoglobulin, specifically binds. An "epitope is antigenic and thus the term epitope is sometimes also referred to herein as" antigenic structure or "antigenic determinant". Thus, the binding domain is an "antigen interaction site." Said binding / interaction is also understood to define a "specific recognition". In one example, said binding domain that binds to / interacts with (specifically) a given target epitope or a given target site on target molecules BCMA and CD3 is an antibody or immunoglobulin, and said binding domain is a VH region and / or VL of an antibody or immunoglobulin.
The "epitopes" can be made up of either contiguous or non-contiguous amino acids juxtaposed by tertiary folding of a protein. A "linear epitope" is an epitope where a primary amino acid sequence comprises the recognized epitope. A linear epitope typically includes at least 3 or at least 4, and more usually, at least 5 or at least 6 or at least 7, for example about 8 to about 10 amino acids in a single sequence. A "conformational epitope", in contrast to a linear epitope, is an epitope where the primary sequence of amino acids that comprise the epitope is not the only component that defines the recognized epitope (eg, an epitope where the primary amino acid sequence is not is necessarily recognized by the binding domain). Typically, a conformational epitope comprises an increased number of amino acids relative to a linear epitope. With respect to the recognition of conformational epitopes, the binding domain recognizes a three-dimensional structure of the antigen, preferably a peptide or a protein or fragment thereof (in the context of the present invention, the antigen for one of
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INDUSTRY! ** ».,. * _“ The binding domains is comprised within the BOMA protein). For example, when a protein molecule is folded into a three-dimensional structure, certain amino acids and / or the polypeptide backbone that make up the conformational epitope are juxtaposed allowing the antibody to recognize the epitope. Methods for determining the conformation of epitopes include, but are not limited to, X-ray crystallography, two-dimensional nuclear magnetic resonance spectroscopy (2D-NMR) and marking with spin probes and electron paramagnetic resonance spectroscopy (EPR). ). Furthermore, the provided examples describe an additional method to check whether a certain binding domain binds to one or more epitope cluster (s) of a given protein, in particular BCMA.
In one aspect, the first binding domain of the present invention is capable of binding to human BCMA epitope cluster 3, preferably human BCMA ECD. Consequently, when the respective epitope cluster on the human BCMA protein is exchanged with the respective epitope cluster on a murine BCMA antigen (resulting in a construct comprising human BCMA, in which the epitope cluster 3 is replaced with cluster of murine epitopes 3 (see SEQ ID NO: 1011), there will be a decrease in binding of the binding domain. Said decrease is preferably at least 10%, 20%, 30%, 40%, 50%, more preferably at least 60%, 70%, 80%, 90%, 95% or even 100% compared to the epitope cluster respective epitope cluster in human BCMA protein, wherein binding to the respective epitope cluster in human BCMA protein is set to 100%. It is contemplated that said human BCMA / murine BCMA chimeras are expressed in CHO cells. Human BCMA / murine BCMA chimeras are also contemplated to fuse
INSTITUTE M EMC A Ν 'DE LA FROP1EDAL · i,, · · _ i _ —J _, _ _ ·. i. . ·। INDUSTVI AL with a transmembrane domain and / or a cytoplasmic domain from a different membrane-bound protein such as EpCAM; see Figure 2a.
A method for testing this loss of binding due to exchange with the respective epitope cluster of a non-human (eg murine) BCMA antigen is described in the accompanying Examples, in particular in Examples 1-3. An additional method of determining the contribution of a specific residue of a target antigen to recognition by a given binding molecule or binding domain is alanine scanning (see for example Morrison KL & Weiss GA. Cur Opin Chem Biol. 2001 Jun; 5 (3): 302-7), where each residue to be analyzed is replaced by alanine, for example by site-directed mutagenesis. Alanine is used because it is non-bulky, chemically inert, with a methyl functional group that nonetheless limits the secondary structure references that many of the other amino acids possess. Bulky amino acids such as valine or leucine can sometimes be used, in cases where conservation of the size of the mutated residues is desired. Alanine tracing is a mature technology that has been in use for an extended period of time.
As used herein, the term "epitope cluster" indicates the totality of epitopes that lie on a defined contiguous stretch of an antigen. An epitope cluster can comprise one, two, or more epitopes. The epitope clusters that were defined -in the context of the present invention- in the extracellular domain of BCMA are described above and are represented in Figure 1.
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The terms "(capable) of binding to", "specifically recognizing", "targeting" and "reacting with" mean according to this invention that a binding domain is capable of specifically interacting with one or more, preferably at least two , more preferably at least three and more preferably at least four amino acids of an epitope.
As used herein, the terms "specifically interact," "specifically bind," or "specifically binds" mean that a binding domain exhibits appreciable affinity for a particular protein or antigen and generally exhibits no reactivity. significant with proteins or antigens other than BCMA or CD3. "Appreciable affinity" includes binding with an affinity of about 10<sup>6</sup>M (KD) or stronger. Preferably, binding is considered specific when the binding affinity is approximately 10 '<sup>12</sup> at 10 '<sup>8</sup>M, 10 '<sup>12</sup> at 10 '<sup>9</sup>M, 10 '<sup>12</sup> at 10 '<sup>10</sup>M, 10 '<sup>11</sup> at 10 '<sup>8</sup>M, preferably about 10 '<sup>11</sup> at 10 '<sup>9</sup>M. Whether a binding domain specifically reacts with, or binds to, a target can be easily assessed by, inter alia, comparing the reaction of said binding domain with a target protein or antigen to the reaction of that domain of binding with proteins or antigens other than BCMA or CD3. Preferably, a binding domain of the invention does not bind essentially or is not capable of binding to proteins or antigens other than BCMA or CD3 (i.e., the first binding domain is not capable of binding to proteins other than BCMA and the second binding domain is not capable of binding to proteins other than CD3).
The expression "does not bind essentially", or "is not capable of binding" means that a binding domain of the present invention does not bind to another protein or antigen other than BCMA or CD3, that is, it does not show reactivity of more than 30%, preferably no more
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Dt LA fROWEDAL 20%, more preferably not more than 10%, particularly preferably notes of 9%, 8%, 7%, 6% or 5% with proteins or antigens other than BCMA or CÚ3, where binding to BCMA or CD3, respectively, is set to be 100%.
Specific binding is believed to be effected by specific motifs in the amino acid sequence of the binding domain and of the antigen. Therefore, the union is achieved as a result of its primary, secondary and / or tertiary structure as well as the result of secondary modifications of said structures. The specific interaction of the antigen interaction site with its specific antigen can result in a simple binding of that site to the antigen. Furthermore, the specific interaction of the antigen interaction site with its specific antigen may alternatively or additionally result in the initiation of a signal, for example, due to the induction of a conformational change of the antigen, an oligomerization of the antigen, etc.
In one aspect, the first binding domain of the present invention binds to human BCMA epitope 3 cluster and is further capable of binding to macaque BCMA epitope 3 cluster such as Macaca mulatta BCMA (SEQ ID NO: 1017 ) or Macaca fascicularis (SEQ ID NO: 1017). The first binding domain is contemplated to bind or not bind to murine BCMA.
Accordingly, in one embodiment, a binding domain that binds to human BCMA, in particular to the epitope cluster 3 of the extracellular protein domain of BCMA formed by amino acid residues 24 to 41 of the human sequence as represented in SEQ ID NO: 1002, also binds to macaque BCMA, in particular to the epitope cluster 3 of the extracellular protein domain of BCMA formed by the
<img file="MX349396B_D0007.tif" />
amino acid residues 24 to 41 of the macaque BCMA sequence as depicted in SEQ ID NO: 1006.
In one embodiment, a first binding domain of a binding molecule is capable of binding to BCMA epitope 3 cluster, wherein BCMA epitope 3 cluster corresponds to amino acid residues 24 to 41 of the sequence depicted in SEQ ID NO: 1002 (full-length polypeptide of human BCMA) or SEQ ID NO: 1007 (extracellular domain of human BCMA: amino acids 1-54 of SEQ ID NO: 1002).
In one aspect of the present invention, the first binding domain of the binding molecule is additionally or alternatively capable of binding to the BCMA epitope 3 cluster of Callithrix jacchus, Saguinus oedipus and / or Saimirí sciureus.
Proteins (including fragments thereof, preferably biologically active fragments, and peptides, usually having less than 30 amino acids) comprise one or more amino acids coupled to each other by a covalent peptide bond (resulting in a chain of amino acids). The term "polypeptide" as used herein describes a group of molecules, consisting of more than 30 amino acids. Polypeptides can further form multimers such as dimers, trimers and higher oligomers, that is, they consist of one or more than one polypeptide molecule. The polypeptide molecules that form such dimers, trimers, etc. they can be identical or non-identical. Corresponding higher-order structures of multimers of this type are therefore called homo- or heterodimers, homo- or heterotrimers, etc. An example for a hereteromultimer is an antibody molecule, which, in its natural form, is made up of two polypeptide chains
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identical light chains and two identical heavy polypeptide chains. The terms polypeptide and protein also refer to naturally modified polypeptides / proteins where the modification is effected for example by post-translational modifications such as glycosylation, acetylation, phosphorylation and the like. When a polypeptide is referred to herein, they can also be chemically modified, such as pegylated. Such modifications are well known in the art.
In another aspect of the invention, the second binding domain is capable of binding CD3 epsilon. In yet another aspect of the invention, the second binding domain is capable of binding to human CD3 and macaque CD3, preferably human epsilon CD3 and macaque CD3 epsilon. Additionally or alternatively, the second binding domain is capable of binding CD3 epsilon from Callithrix jacchus, Saguinus oedipus and / or Saimirí sciureus. According to these embodiments, one or both of the binding domains of the binding molecule of the invention are preferably cross-species specific for members of the mammalian order of primates. Cross species specific CD3 binding domains are described in WO 2008/119567.
It is particularly preferred for the binding molecule of the present invention that the second binding domain capable of binding to the CD3 receptor T cell complex comprises a VL region comprising CDR-L1, CDR-L2 and CDR-L3 selected from:
(a) CDR-L1 as depicted in SEQ ID NO: 27 of WO 2008/119567, CDR-L2 as depicted in SEQ ID NO: 28 of WO 2008/119567 and CDR-L3 as depicted in SEQ ID NO: 29 of WO 2008/119567;
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INDUSTRIAL (b) CDR-L1 as represented in SEQ ID NO: 117 of WO 2008/119567, CDRT2 as represented in SEQ ID NO: 118 of WO 2008/119567 and CÜR-L3 as represented in SEQ ID NO: 119 of WO 2008 / 119567; and (c) CDR-L1 as represented in SEQ ID NO: 153 of WO 2008/119567, CDR-L2 as represented in SEQ ID NO: 154 of WO 2008/119567 and CDR-L3 as represented in SEQ ID NO: 155 of WO 2008/119567.
In an alternatively preferred embodiment of the binding molecule of the present invention, the second binding domain capable of binding to the CD3 T cell receptor complex comprises a VH region comprising CDR-H 1, CDR-H2 and CDR-H3 selected from :
(a) CDR-H1 as represented in SEQ ID NO: 12 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 13 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 14 of WO 2008/119567;
(b) CDR-H1 as represented in SEQ ID NO: 30 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 31 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 32 of WO 2008/119567;
(c) CDR-H1 as represented in SEQ ID NO: 48 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 49 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 50 of WO 2008/119567;
(d) CDR-H1 as represented in SEQ ID NO: 66 and WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 67 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 68 of WO 2008/119567;
<img file="MX349396B_D0009.tif" />
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INSTmiTOMaiCAW I HEARD THE PkOWEDAI 'NWSTRIAI (e) CDR-H1 as depicted in SEQ ID NO: 84 de. WO 2008/119567, CDR-H2 as depicted in SEQ ID NO: 85 of WO 2008/119567 and CDR-H3 as depicted in SEQ ID NO: 86 of WO 2008/119567;
(f) CDR-H1 as represented in SEQ ID NO: 102 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 103 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 104 of WO 2008/119567;
(g) CDR-H1 as represented in SEQ ID NO: 120 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 121 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 122 of WO 2008/119567;
(h) CDR-H1 as represented in SEQ ID NO: 138 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 139 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 140 of WO 2008/119567;
(i) CDR-H1 as represented in SEQ ID NO: 156 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 157 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 158 of WO 2008/119567; and (j) CDR-H1 as represented in SEQ ID NO: 174 of WO 2008/119567, CDR-H2 as represented in SEQ ID NO: 175 of WO 2008/119567 and CDR-H3 as represented in SEQ ID NO: 176 of WO 2008/119567.
It is further preferred for the binding molecule of the present invention that the second binding domain capable of binding to the CD3 receptor T cell complex comprises a VL region selected from the group consisting of a VL region as represented in SEQ ID NO: 35, 39, 125, 129, 161 or 165 of WO 2008/119567.
It is alternatively preferred that the second binding domain capable of binding to the CD3 T cell receptor complex comprises a VH region selected from the group consisting of a VH region as represented in SEQ ID NO: 15,19, 33, 37, 51, 55 , 69, 73, 87, 91, 105, 109, 123, 127, 141, 145, 159, 163, 177 or 181 of WO 2008/119567.
More preferably, the binding molecule of the present invention is characterized by the second binding domain capable of binding to the CD3 receptor T cell complex comprising a VL region and a VH region selected from the group consisting of:
(a) a VL region as represented in SEQ ID NO: 17 or 21 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 15 or 19 of WO 2008/119567;
(b) a VL region as represented in SEQ ID NO: 35 or 39 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 33 or 37 of WO 2008/119567;
(c) a VL region as represented in SEQ ID NO: 53 or 57 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 51 or 55 of WO 2008/119567;
(d) a VL region as represented in SEQ ID NO: 71 or 75 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 69 or 73 of WO 2008/119567;
(e) a VL region as represented in SEQ ID NO: 89 or 93 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 87 or 91 of WO 2008/119567;
(f) a VL region as represented in SEQ ID NO: 107 or 111 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 105 or 109 of WO 2008/119567;
(g) a VL region as represented in SEQ ID NO: 125 or 129 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 123 or 127 of WO 2008/119567;
(h) a VL region as represented in SEQ ID NO: 143 or 147 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 141 or 145 of WO 2008/119567;
<img file="MX349396B_D0010.tif" />
and a VH region as depicted in SEQ ID NO: 159 ivinn d * -W £ L9nnR / i 19567;
and (j) a VL region as represented in SEQ ID NO: 179 or 183 of WO 2008/119567 and a VH region as represented in SEQ ID NO: 177 or 181 of WO 2008/119567.
According to a preferred embodiment of the binding molecule of the present invention, in particular the second binding domain capable of binding to the CD3 receptor complex of T cells, the pairs of VH regions and VL regions are in the format of an antibody of simple string (scFv). The VH and VL regions are arranged in the order VH-VL or VL-VH. It is preferred that the VH region is positioned N-terminal to a linker sequence. The VL region is positioned C-terminus of the linker sequence.
A preferred embodiment of the above-described binding molecule of the present invention is characterized by the second binding domain capable of binding to the CD3 receptor T-cell complex comprising an amino acid sequence selected from the group consisting of SEQ ID NOs: 23, 25, 41, 43, 59, 61, 77, 79, 95, 97, 113, 115, 131, 133, 149, 151, 167, 169, 185 or 187 of WO2008 / 119567.
The affinity of the first binding domain for human BCMA is preferably - 15 nM, more preferably <10 nM, even more preferably <5 nM, still more preferably - 1 nM, still more preferably <0.5 nM, even more preferably <0 , 1 nM, and still preferably - 0.05 nM. The affinity of the first binding domain for macaque BCMA is preferably - 15 nM, more preferably - 10 nM, even more preferably - 5 nM,
IMPI ^ • msxicano NSTITUTC / 5
OF THE INDUSTRIAL EBOPIETY W> still more preferably <1 nM, still more preferably <0.5 nM, still more preferably <0.1 nM, and still more preferably <0.05 nM or even <0.01 nM. Affinity can be measured for example in a Biacore assay or in a Scatchard assay, eg as described in the Examples. The affinity difference for binding to macaque BCMA versus human BCMA is preferably [1: 10-1: 5] or [5: 1-10: 1], more preferably [1: 5-5: 1], and still more preferably [1: 2-3: 1] or even [1: 1-3: 1]. Other methods of determining affinity are well known to the person skilled in the art.
Cytotoxicity mediated by bispecific binding molecules for BCMA / CD3 can be measured in a number of ways. The effector cells can be, for example, enriched stimulated CD8 positive (human) T cells or unstimulated (human) peripheral blood mononuclear cells (PBMC). If the target cells are of macaque origin or express or are transfected with macaque BCMA, the effector cells must also be of macaque origin such as a macaque T cell line, eg, 4119LnPx. The target cells must express (at least the extracellular domain of) BCMA, eg, human or macaque BCMA. The target cells can be a cell line (such as CHO), which is stably or transiently transfected with BCMA, eg, human or macaque BCMA.
Alternatively, the target cells can be a natural expressing cell line.
BCMA positive, such as human multiple myeloma cell line L363 or NCI H929.
In general, EC values are expected to<sub>50</sub> are lower with target cell lines expressing higher levels of BCMA on the cell surface. The relationship of
<img file="MX349396B_D0011.tif" />
IMPI effector to target cell (E: T) is usually around 10: 1, but can as well. The cytotoxic activity of UCM / VbEW bispecific binding molecules can be measured in a chromium 51 release assay (incubation time of about 18 hours) or in a FACS-based cytotoxicity assay (incubation time of about 48 hours. ). Modifications of the incubation time of the assay (cytotoxic reaction) are also possible. Other methods of measuring cytotoxicity are well known to the skilled person and include MTT or MTS assays, ATP-based assays including bioluminescence assays, the sulforhodamine B (SRB) assay, WST assay, clonogenic assay and ECIS technology.
The cytotoxic activity mediated by bispecific binding molecules for BCMA / CD3 of the present invention is preferably measured in a cell-based cytotoxicity assay. This is represented by an EC value<sub>50</sub>, which corresponds to the maximum effective mean concentration (concentration of the binding molecule that induces a cytotoxic response halfway between the baseline and the maximum). Preferably, the EC value<sub>50</sub> of the bispecific binding molecules for BCMA / CD3 is - 20,000 pg / ml, more preferably - 5000 pg / ml, even more preferably - 1000 pg / ml, even more preferably - 500 pg / ml, even more preferably - 350 pg / ml. ml, even more preferably 320 pg / ml, even more preferably 250 pg / ml, even more preferably 100 pg / ml, even more preferably 50 pg / ml, even more preferably 10 pg / ml, and most preferred 5 pg / ml.
Any of the EC values<sub>50</sub> given above can be combined with any one of the indicated scenarios of a cell-based cytotoxicity assay. For example, when CD8 positive (human) T cells or a macaque T cell line
<img file="MX349396B_D0012.tif" />
IMPI ΙΜΠΤΗΤΤΟ MBXICANO DS THE INDUSTRIAL PROPERTY are used as effector cells, the EC value<sub>50</sub> of the bispecific binding molecule for BCMA / CD3 is preferably £ 1000 pg / ml, more preferably <500 pg / ml, even more preferably <250 pg / ml, even more preferably £ 100 pg / ml, even more preferably - 50 pg / ml, even more preferably £ 10 pg / ml, and most preferably £ 5 pg / ml. If the target cells in this assay are BCMA-transfected cells (human or macaque) such as CHO cells, the EC value<sub>50</sub> of the bispecific binding molecule for BCMA / CD3 is preferably £ 150 pg / ml, more preferably £ 100 pg / ml, even more preferably £ 50 pg / ml, even more preferably £ 30 pg / ml, even more preferably £ 10 pg / ml, and most preferred £ 5 pg / ml.
If the target cells are a natural BCMA positive expressing cell line, then the EC value<sub>50</sub> is preferably £ 350 pg / ml, more preferably £ 320 pg / ml, even more preferably £ 250 pg / ml, even more preferably £ 200 pg / ml, even more preferably £ 100 pg / ml, still more preferably £ 150 pg / ml, even more preferably £ 100 pg / ml, and most preferred £ 50 pg / ml, or less.
When PBMCs (human) are used as effector cells, the EC50 value of the bispecific binding molecule for BCMA / CD3 is preferably £ 1000 pg / ml, more preferably £ 750 pg / ml, more preferably <500 pg / ml, even more preferably £ 350 pg / ml, even more preferably £ 320 pg / ml, even more preferably £ 250 pg / ml, still more preferably £ 100 pg / ml, and most preferably £ 50 pg / ml, or less.
In a particularly preferred embodiment, the bispecific binding molecules for BCMA / CD3 of the present invention are characterized by an EC<sub>5</sub>or <350 pg / ml or less, more preferably £ 320 pg / ml or less. In such an embodiment the target cells are L363 cells and the effector cells are human unstimulated PBMCs. Person
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MEXICAN INSTITUTE
OF. UA FROTUDAb expert knows how to measure EC value<sub>50</sub> without further effort. Furthermore, the ^ esTri ^ tionSmoa a specific instruction on how to measure the EC value<sub>50</sub>; see for example he Exernplu 0.3, - later. A suitable protocol is as follows:
a) Prepare peripheral human blood mononuclear cells (PBMC) by Ficoll density gradient centrifugation from lymphocyte-enriched preparations (buffy coat)
b) Optionally wash with Dulbecco's PBS (Gibco)
c) Remove remaining erythrocytes from PBMC by incubation with erythrocyte lysis buffer (155 mM NH<sub>4</sub>IC, 10 mM KHCO<sub>3</sub>, 100 μΜ EDTA)
c) Remove platelets using the supernatant from the PBMC centrifugation at 100 xg
d) Remove (deplete) CD14 cells<sup>+</sup> and NK cells
e) Isolate CD14 / CD56 negative cells using, for example, LS Columns (Miltenyi Biotec, # 130-042-401)
f) Cultivate PBMC without CD14 + / CD56 + cells, for example in complete RPMI medium that is RPMI1640 (Biochrom AG, # FG1215) supplemented with 10% FBS (Biochrom AG, # S0115), 1x non-essential amino acids (Biochrom AG, # K0293) , 10 mM Hepes buffer (Biochrom AG, # L1613), 1 mM sodium pyruvate (Biochrom AG, # L0473) and 100 U / ml penicillin / streptomycin (Biochrom AG, # A2213) at 37 ° C in an incubator until it is necessary.
g) Label target cells
h) Mix effector cells (E) and target cells (target: T), preferably at equal volumes, so as to have an E: T ratio of 10: 1
i) Add the binding molecule, preferably in a serial dilution
j) Proceed for 48 hours in a humidified incubator with 7% CO<sub>2</sub>.
<img file="MX349396B_D0013.tif" />
IMPI
INfTTTVTO MtXíCAN (
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Monitor the integrity of the cell membrane, for example by adding propidium (Pl) iodide to a final concentration of 1 pg / ml, for example by flow cytometry
I) Calculate the EC<sub>50</sub>, for example according to the following formula:
Cytotoxicilad [%] = ”« lulasdiandead <sub>χ</sub> j θθ ^ target cells n = number of events
Using the GraphPad Prism 5 program (Graph Pad Software, San Diego), the percent cytotoxicity was plotted against the corresponding bispecific antibody concentrations. The dose response curves can be analyzed with the four parametric logistic regression models for the evaluation of the sigmoid dose response curves with fixed Hill slope and the EC values were calculated.<sub>S0</sub>.
In view of the above, it is preferred that the binding molecule of the present invention is characterized by an EC<sub>50</sub> (pg / ml) of 350 or less, preferably 320 or less.
The present invention also relates to binding molecules described herein that are characterized by an EC<sub>50</sub> (pg / ml) which is equivalent to EC<sub>50</sub> (pg / ml) of any one of the bispecific binding molecules for BCMA / CD3: BCMA-83 x CD3, BCMA-62 x CD3, BCMA-5 x CD3, BCMA-98 x CD3, BCMA-71 x CD3, BCMA -34 x CD3, BCMA-74 x CD3, BCMA-20 x CD3. In order to determine whether the EC<sub>50</sub> of a binding molecule as described herein is equivalent to the EC<sub>50</sub> of any one of BCMA-83 x CD3, BCMA-62 x CD3, BCMA-5 x CD3, BCMA-98 x CD3, BCMA-71 x CD3, BCMA-34 x CD3, BCMA-74 x CD3, BCMA-20 x CD3, it is contemplated that for the determination of the value
IMPI
INSTmnrO MCUCANC
FROM THE MONSIMD INtM * STiiAL of EC<sub>50</sub>, the same test is applied. The term equates to therefore includes a deviation of +/- 10%, preferably +/- 7.5%, more preferably +/- 5%, more preferably still +/- 2.5% from the respective EC value<sub>50</sub>. Bispecific binding molecules for BCMA / CD3: BCMA-83 x CD3, BCMA-62 x CD3, BCMA-5 x CD3, BCMA-98 x CD3, BCMA-71 x CD3, BCMA-34 x CD3, BCMA-74 x CD3, BCMA-20 x CD3 that serve as reference binding molecules in the assay described above are preferably produced in CHO cells.
The difference in cytotoxic activity between the monomeric and dimeric isoform of individual bispecific binding molecules for BCMA / CD3 (such as antibodies) is referred to as the potency difference. This power difference can, for example, be calculated as the ratio between the EC values<sub>50</sub> of the monomeric and dimeric forms of the molecules. The potency differences of the bispecific binding molecules for BCMA / CD3 of the present invention are preferably - 5, more preferably - 4, even more preferably - 3, even more preferably <2, and most preferably <1.
Preferably, the bispecific BCMA / CD3 binding molecules of the present invention do not bind to, interact with, recognize, or cross-react with human BAFF-R and / or human TACI. Methods for detecting cross-reactivity with human BAFF-R and / or human TACI are described in Example 9.
It is also preferred that the BCMA / CD3 bispecific binding molecules of the present invention exhibit very low dimer conversion after a number of freeze / thaw cycles. Preferably the percentages of dimers are <5%, more preferably <4%, even more preferably 3%, still more preferably <2.5%, still more preferably £ 2%, even more preferably <3%! , 5%, and more<sup>1 </sup>preferably £ 1%, for example after three thaw / freeze cycles. A freeze-thaw cycle and the determination of the percentage of dimer can be carried out according to Example 16.
The bispecific binding molecules for BCMA / CD3 (such as antibodies) of the present invention preferably show favorable thermostability with melting temperatures above 60 ° C.
To determine the potential interaction of bispecific binding molecules for BCMA / CD3 (such as antibodies) with human plasma proteins, a plasma interference assay can be performed (see for example Example 18). In a preferred embodiment, there is no significant reduction in target binding of bispecific binding molecules for BCMA / CD3 mediated by plasma proteins. The relative plasma interference value is preferably s 2.
It is also contemplated that the BCMA / CD3 bispecific binding molecules of the present invention are capable of exhibiting therapeutic efficacy or anti-tumor activity.
This can be evaluated, for example, in a study as described in Example 19 (advanced stage human tumor xenograft model). The skilled person knows how to modify or adapt certain parameters of this study, such as the number of tumor cells injected, the injection site, the number of transplanted human T cells, the amount of bispecific binding molecules for BCMA / CD3 to be administered. , and the timelines, while still reaching a meaningful result and
<img file="MX349396B_D0014.tif" />
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reproducible. Preferably, tumor growth inhibition T / C [%] is lower, more preferably 50 or 40 or lower, even more preferably 20 or lower, and more preferably 10 or lower, 5 or lower, or even 2.5 or lower .
Preferably, the bispecific BCMA / CD3 binding molecules of the present invention do not induce / mediate lysis or essentially do not induce / mediate BCMA negative cells such as HL60, MES-SA, and SNU-16. The terms "does not induce lysis," "essentially does not induce lysis", "does not mediate lysis" or "essentially does not mediate lysis" mean that a binding molecule of the present invention does not induce or mediate lysis of more than 30%, preferably not more than 20%, more preferably not more than 10%, particularly preferably not more than 9%, 8%, 7%, 6% or 5% of BCMA negative cells, wherein the lysis of a BCMA positive cell line such such as NCIH929, L-363 or OPM-2 it is set to 100%. This applies for binding molecule concentrations of at least up to 500 nM. The skilled person knows how to measure cell lysis without requiring additional explanations. Furthermore, this description provides specific instruction on how to measure cell lysis; see Example 20 below.
In one embodiment, the first or second binding domain is or is derived from an antibody. In another embodiment, the two binding domains are or are derived from an antibody.
The definition of the term antibody includes such embodiments as monoclonal, chimeric, single chain, humanized and human antibodies. In addition to full-length antibodies, the definition also includes derivatives of antibodies and antibody fragments, such as, among others, Fab fragments. Antibody fragments or derivatives further comprise F (ab ') fragments<sub>2</sub>, Fv,
INSTITUTO MEXICani.
O »LA ΡΧΟΠΕΡΛΓ OsseXaJS / industrial scFv or single domain antibodies, such as domain antibodies or nanobodies, single variable domain antibodies or single variable domain immunoglobulin antibodies comprising only one variable domain, which can be VHH, VH or VL, that specifically bind to an antigen or epitope independently of other V regions or domains; see, for example, Harlow and Lañe (1988) and (1999), loe. cit .; Kontermann and Dübel, Antibody Engineering, Springer, 2nd ed. 2010 and Little, Recombinant Antibodies for Immunotherapy, Cambridge University Press 2009. This term also includes Dual-Affinity Re-Targeting (DART) diabodies or antibodies. Additionally contemplated are single chain diabodies (bispecific), tandem diabodies (Tandab's), "minibodies" exemplified by a structure that is as follows: antibodies (VH-VL-CH3)<sub>2</sub>, (scFv-CH3)<sub>2</sub> or (scFv-CH3-scFv)<sub>2</sub>, "Fe DART" and IgG DART antibodies, and multibodies such as tribodies. Variable single domain immunoglobulin comprises not only an isolated single variable domain antibody polypeptide, but also larger polypeptides comprising one or more monomers of a variable single domain antibody polypeptide sequence.
Various procedures are known in the art and can be used for the production of such antibodies and / or fragments. Thus, derivatives (of antibodies) can be prepared by peptidoimimetics. Furthermore, the techniques described for the production of single chain antibodies (see, among others, US Patent 4,946,778, Kontermann and Dübel (2010), loe. Cit. And Little (2009), loe. cit.) can be adapted to produce specific single chain antibodies for polypeptide (s) of choice. Transgenic animals can also be used to express humanized antibodies specific for fusion polypeptides and proteins of this invention. For the preparation of monoclonal antibodies, any technique can be used, which
<img file="MX349396B_D0015.tif" />
IMPI Mexican institute
OF INDUSTRY PROPERTY!
provide antibodies produced by culture rnntinnrtirw iíhuj ». »» Ininrnr Fjamping for such techniques include the hybridoma technique (Kohler and Milstein Nature 256 (1975), 495-497), the trioma technique, the B-cell hybridoma technique (Kozbor, Immunology Today 4 (1983), 72 ) and the EBV hybridoma technique to produce human monoclonal antibodies (Cole et al., Monoclonal Antibodies and Cancer Therapy, Alan R. Liss, Inc. (1985), 77-96). Surface plasmon resonance as employed in the BIAcore system can be used to increase the efficiency of antibodies on phage that bind to an epitope of a target polypeptide, such as CD3 epsilon (Schier, Human Antibodies Hybridomas 7 (1996), 97 -105; Malmborg, J. Immunol. Methods 183 (1995), 713). It is also contemplated in the context of this invention that the term "antibody" encompasses constructs, which can be expressed in a host as described herein below, for example, antibody constructs that can be transfected and / or transduced by , among others, viruses, or plasmid vectors.
Furthermore, the term "antibody" as used herein also refers to derivatives or variants of the antibodies described herein that show the same specificity as the described antibodies. Examples of antibody variants include humanized non-human antibody variants, affinity matured antibodies (see, eg. Hawkins et al. J. Mol. Biol. 254, 889-896 (1992) and Lowman et al., Biochemistry 30, 10832-10837 (1991)) and mutant antibodies with altered effector function (s) (see for example, US Pat. No. 5,648,260 , Kontermann and Dübel (2010), loe. Cit. And Little (2009), loe. Cit.).
<img file="MX349396B_D0016.tif" />
<sup>33</sup> IMPI
INSTITTO MÍXICano DE LA ROPIBDAD INNOUTTWIAL
The terms antigen-binding domain, antigen-binding fragment, and antibody-binding region when used herein refer to a part of an antibody molecule that comprises amino acids responsible for the specific binding between the antibody and the antigen. . The part of the antigen that is specifically recognized and bound by the antibody is referred to as the epitope, as described hereinbefore. As mentioned above, an antigen-binding domain can typically comprise an antibody light chain (VL) variable region and an antibody heavy chain (VH) variable region, however, it need not comprise both. Fd fragments, for example, have two VH regions and often retain some antigen-binding function of intact antigen-binding domain. Examples of antigen-binding fragments include (1) a Fab fragment, a monovalent fragment having the VL, VH, CL, and CH1 domains; (2) an F (ab ') 2 fragment, a bivalent fragment having two Fab fragments linked by a bisulfide bridge in the hinge region; (3) an Fd fragment having two domains VH and CH1; (4) an Fv fragment having the VL and VH domains of a single arm of an antibody, (5) a dAb fragment (Ward et al., (1989) Nature 341: 544-546), which has a VH domain ; (6) an isolated complementarity determining region (CDR), and (7) a single Fv chain (scFv), the latter being preferred (eg, derived from a scFV library). Although the two domains of the Fv fragment, VL and VH are encoded by two separate genes, they can be joined, using recombinant methods, by a synthetic coupler that allows them to be in a single protein chain in which the VL and VH regions are linked. put together to form monovalent molecules (known as single chain Fv (scFv); see for example, Huston et al.
(1988) Proc. Nati. Acad. Sci USA 85: 5879-5883). These antibody fragments are obtained using standard techniques known to those of skill in the art, and the performance of the fragments is evaluated in the same way as for intact antibodies.
The term "monoclonal antibody" as used herein refers to an antibody obtained from a population of substantially homogeneous antibodies, that is, the individual antibodies that comprise the population are identical except for possible naturally occurring mutations and / or modifications subsequent to translation (eg isomerizations, amidations) which may be present in minor amounts. Monoclonal antibodies are highly specific, being directed against a single antigenic site. Furthermore, in contrast to conventional (polyclonal) antibody preparations that typically include different antibodies directed against different determinants (epitopes), each monoclonal antibody is directed against a single determinant on the antigen. In addition to their specificity, monoclonal antibodies are advantageous since they are synthesized by hybridoma culture, not contaminated by other immunoglobulins. The modifier "monoclonal" indicates the character of the antibody as derived from a substantially homogeneous population of antibodies, and should not be construed as requiring the production of the antibody by any particular method. For example, monoclonal antibodies to be used in accordance with the present invention can be prepared by the hybridoma procedure first described by Kohler et al, Nature, 256 :. 495 (1975), or they can be prepared by recombinant DNA methods (see, for example, US Patent No. 4,816,567). Monoclonal antibodies can also be isolated from phage antibody libraries using the techniques described in Clackson et al, Nature, 352 :. 624-628 (1991) and Marks et al, J. Mol .. BioL, 222 :. 581-597 (1991), for example.
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The monoclonal antibodies of the present invention specifically include chimeric antibodies (immunoglobulins) in which a heavy and / or light portion of the chain is identical or homologous to the corresponding sequences in antibodies derived from a particular species or belonging to a particular class or subclass. of antibody, while the rest of the chain (s) is (are) identical (s) or homologous (s) to the corresponding sequences in antibodies derived from other species or belonging to another class or subclass of antibodies, as well as fragments of said antibodies, as long as they show the desired biological activity (US Patent No. <sup>0 </sup>4,816, 567; Morrison et al, Proc Nati Acad Sci USA, 81: 6851-6855 (1984)). Chimeric antibodies of interest herein include primatized antibodies comprising variable domain antigen-binding sequences derived from a non-human primate (eg, Old World Monkey, Ape, etc.) and human constant region sequences.
Humanized forms of non-human (e.g., murine) antibodies are chimeric immunoglobulins, immunoglobulin chains, or fragments thereof (such as Fv, Fab, Fab ', F (ab') 2 or other antibody subsequences that bind to antigens) of the mostly human sequences, which contain a minimal portion of sequence derived from non-human immunoglobulin. For the most part, humanized antibodies are human immunoglobulins (recipient antibody) in which residues from a hypervariable region (also called CDR) from the receptor are replaced by residues from a hypervariable region from a non-human species (donor antibody) such as mouse, rat, or rabbit having the desired specificity, affinity, and capacity. In some cases, residues in the human immunoglobulin Fv framework region (FR) are replaced by corresponding non-human residues. Furthermore, humanized antibodies as used herein can also comprise residues that are found neither in the recipient antibody nor in the donor antibody. These modifications are made to refine and optimize the performance of the antibody. The optimally humanized antibody will also comprise at least a portion of an immunoglobulin (Fe) constant region, typically that of a human immunoglobulin. For more details see Jones et al., Nature, 321: 522-525 (1986); Reichmann et al., Nature, 332: 323-329 (1988); and Presta, Curr. Op. Struct. BioL, 2: 593-596 (1992).
The term "human antibody" includes antibodies that have variable and constant regions corresponding substantially to human germline immunoglobulin sequences known in the art, including, for example, those described by Kabat et al. (See Kabat et al. (1991) loe. Cit.). The human antibodies of the invention may include amino acid residues not encoded by human germline immunoglobulin sequences (for example, mutations introduced by random or site-specific mutagenesis in vitro or by somatic mutation in vivo), for example in CDRs, and in particular, CDR3. The human antibody can have at least one, two, three, four, five, or more positions replaced with an amino acid residue that is not encoded by the human germline immunoglobulin sequence.
As used herein, "in vitro generated antibody" refers to an antibody where all or part of the variable region (eg, at least one CDR) is generated in a selection of non-immune cells (eg, a phage display in vitro, a protein chip or any other method in which candidate sequences can be tested for their ability to bind to an antigen). This expression therefore
<img file="MX349396B_D0017.tif" />
IMPJ
MEXICAN INSTITUTE
Industrial L> E rA PROFreDAp preferably excludes sequences generated by genomic rearrangement in an immune cell.
A "bisepecific or bifunctional antibody or immunoglobulin" is a hybrid artificial antibody or immunoglobulin that has two different heavy / light chain pairs and two different binding sites. Bispecific antibodies can be produced by a variety of methods including hybridoma fusion or ligation of Fab 'fragments. See, for example, Songsivilai & Lachmann, Clin. Exp. Immunol. 79: 315321 (1990). Numerous methods known to those skilled in the art are available to obtain antigen-binding antibodies or fragments thereof. For example, antibodies can be produced using recombinant DNA methods (US Patent 4,816,567). Monoclonal antibodies can also be produced by generation of hybridomas (see for example Kohlery Milstein (1975) Nature, 256: 495-499) according to known methods. Hybridomas formed in this way are then screened using standard methods, such as enzyme-linked immunosorbent assay (ELISA) and surface plasmon resonance assay (BIACORE ™), to identify one or more hybridomas that produce an antibody that binds. specifically with a specified antigen. Any form of the specified antigen can be used as the immunogen, for example, recombinant antigen, natural forms and any variants or fragments thereof as well as antigenic peptides thereof.
An exemplary method of preparing antibodies includes screening protein expression libraries, eg phage or ribosome display libraries. Phage display is described, for example, in Ladner et al., US Pat.
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Di LA PROPERTY V ^ - ™ INDUSTRIAL FIO V * * 9 ^
No. 5,223,409; Smith (1985) Science 228: 1315-1317; Claeteewxrf-aMJSaiXWaMe ^^ 624-628.
In addition to the use of display libraries, the specified antigen can be used to immunize a non-human animal, eg, a rodent, eg, a mouse, hamster, or rat. In one embodiment, the non-human animal includes at least part of a human immunoglobulin gene. For example, mouse lines deficient in mouse antibody production can be engineered with large fragments of human Ig loci. Using hybridoma technology, antigen-specific monoclonal antibodies derived from genes with the desired specificity can be produced and selected. See for example, XENOMOUSE ™, Green et al. (1994) Nature Genetics 7: 13-21, US 2003-0070185, WO 96/34096, and WO96 / 33735.
A monoclonal antibody can be obtained from a non-human animal, and then modified, for example humanized, deimmunized, chimeric, or it can be produced using recombinant DNA techniques known in the art. A variety of approaches to making chimeric antibodies have been described. See, for example, Morrison et al., Proc. Nati. Acad. ScL USA 81: 6851, 1985; Takeda et al., Nature 314: 452, 1985, Cabilly et al., US Patent No. 4,816,567; Boss et al., US Patent No. 4,816,397; Tanaguchi et al., EP 0171496; EP 0173494, GB 2177096. Humanized antibodies can also be produced, for example, using transgenic mice that express the human heavy and light chain genes, but are unable to express the endogenous mouse immunoglobulin heavy and light chain genes. Winter describes an example of a CDR grafting method that can be used to prepare the
USTITUTOMEXlCAN ·: PE THE INDUSTRIAL AVERAGE humanized antibodies described herein (US Patent No. 5,225,539). ~ All CDRs of a particular human antibody can be substituted with at least a portion of a non-human CDR or only some of the CDRs they can be substituted with non-human CDRs. It is only necessary to replace the number of CDRs required for the binding of the humanized antibody to a predetermined antigen.
Humanized antibodies or fragments thereof can be generated by replacing variable Fv domain sequences that are not directly involved in antigen binding with equivalent sequences from human Fv variable domains. Exemplary methods for the generation of humanized antibodies or fragments thereof are provided by Morrison (1985) Science 229: 12021207; by Oí et al. (1986) BioTechniques 4: 214; and by US No. 5,585,089; US No. 5,693,761; US No. 5,693,762; US No. 5,859,205; and US No. 6,407,213. These methods include the isolation, manipulation, and expression of the nucleic acid sequences that encode all or part of the immunoglobulin Fv variable domains of at least one of a heavy or light chain. Such nucleic acids can be obtained from a hybridome that produces an antibody against a predetermined target, as described above, as well as from other sources. The recombinant DNA encoding the humanized antibody molecule can then be cloned into an appropriate expression vector.
A humanized antibody can be optimized by introducing conservative substitutions, consensus sequence substitutions, germline substitutions, and / or retro mutations. Such altered immunoglobulin molecules can be prepared by any of a number of techniques known in the art, (eg, Teng et al, 'Ν ^ ΤΙ / ΤΟΜΕΧΚλν, ·
OR<sub>L</sub> M PRCJMDAI ^ «« 3
Proc Nati Acad Sci USA, 80: 7308-7312, 1983; Kozbor et al, lrfWídTfü1üg9 ^ 3EMr4: 7279, 1983; Olsson et al, Meth Enzymol, 92: 3-16, ios?) And "........"! <- ar.iArdn with the teachings of EP 239 400.
An antibody or fragment thereof can also be modified by specific deletion of human T cell epitopes or deimmunization by the methods described in WO 98/52976 and WO 00/34317. Briefly, the heavy and light chain variable domains of an antibody can be analyzed for peptides that bind to MHC class II; these peptides represent potential T cell epitopes (as defined in WO 98/52976 and WO 00/34317). For the detection of potential T-cell epitopes, a computer modeling approach called peptide threading can be applied, and a database of human MHC class II-binding peptides can be searched for motifs present in the VH sequences. and VL, as described in WO 98/52976 and WO 00/34317. These motifs bind to any of the 18 major MHC class II DR allotypes, and thus constitute potential T-cell epitopes. The potential detected T cell epitopes can be eliminated by substituting a small number of amino acid residues in the variable domains, or preferably, by substituting a single amino acid. Typically, conservative substitutions are made. Often, but not exclusively, an amino acid common to a position in human germline antibody sequences can be used. Human germline sequences are described, for example, Tomlinson, et al. (1992) J. Mol. BioL. 227: 776-798; Cook, GP et al. (1995) Immunol. Today vol. 16 (5): 237-242, and Tomlinson et al. (1995) EMBO J. 14: 14: 4628-4638. Catalog V BASE offers a complete directory of human immunoglobulin variable region sequences (compiled by Tomlinson, LA. Et al. MRC Center for Protein Engineering, Cambridge, UK). These sequences are
<img file="MX349396B_D0018.tif" />
IMPI
MEXICAN INSTITUTE
OF THE INDUSTRIAL NOTICE can be used as a source of human sequence, for example, for framework regions and CDRs. Consensus human framework regions can also be used, for example, as described in US Patent No. 6,300,064.
The pairing of VH and VL together forms a single antigen-binding site. The CH domain most proximal to VH is designated CH1. Each L chain is linked to an H chain by a covalent disulfide bond, while the two H chains are linked by one or more disulfide bonds depending on the isotype of the H chain. The VH and VL domains consist of four relatively conserved sequence regions called framework regions (FR1, FR2, FR3, and FR4), which form a framework for three hypervariable sequence regions (complementarity determining regions, CDRs). CDRs contain most of the residues responsible for the specific interactions of the antibody with the antigen. The sor CDRs referenced as CDR1, CDR2, and CDR3. Consequently, the constituent CDRs of the heavy chain are known as H1, H2, and H3, while the constituent CDRs of the light chain are known as L1, L2, and L3.
The term variable refers to the portions of the immunoglobulin domains that exhibit variability in their sequence and that are involved in determining the specificity and binding affinity of a particular antibody (i.e., the variable domain (s) ( s)). The variability is not uniformly distributed throughout the antibody variable domains, but is concentrated in subdomains of each of the heavy and light chain variable regions. These subdomains are called "hypervariable regions or complementarity determining regions (CDRs)." The most conserved (that is, non-hypervariable) portions of the variable domains are called
<img file="MX349396B_D0019.tif" />
framework regions (FRM). The naturally occurring heavy and light chain variable domains each comprise four FRM regions, largely adopting a β-sheet configuration, connected by three hypervariable regions, which form loops that connect, and in some cases are part of, the structure of sheet β. The hypervariable regions in each chain are held together in close proximity by the FRM and, with the hypervariable regions on the other chain, contribute to the formation of the antigen-binding site (see Kabat et al., Loe. Cit.). Constant domains are not directly involved in antigen binding, but exhibit various effector functions, such as, for example, cell-mediated cytotoxicity and antibody-dependent complement activation.
It is also preferred for the binding molecule of the invention that the first and second binding domains form a molecule that is selected from the group of (scFv)<sub>2</sub>, (single domain monoclonal antibody)<sub>2</sub>, scFv-single domain monoclonal antibody, diabody, or oligomers thereof.
The terms CDRs and their plural CDRs refer to a complementarity determining region (CDR) of which three constitute the binding character of a light chain variable region (CDRL1, CDRL2 and CDRL3) and three constitute the binding character of a heavy chain variable region (CDRH1, CDRH2 and CDRH3). CDRs contribute to the functional activity of an antibody molecule and are separated by amino acid sequences that comprise framework or structure regions. The exact CDR definition limits and lengths are subject to different classification and numbering systems. Therefore the CDRs can be referenced by Kabat, Chothia, contact or any other defiiífEI6ft<sup>,TO</sup>tle Tfrnrfes, including the numbering system described herein. - '......
Despite differing in boundaries, each of these systems has a certain degree of overlap in what constitutes the so-called hypervariable regions within the variable sequences. The CDR definitions according to these systems may therefore differ in length and boundary areas with respect to the adjacent framework region. See, for example, Kabat, Chothia, and / or MacCallum (Kabat et al, loe cit; Chothia et al, J. Mol Biol., 1987, 196: 901, and MacCallum et al, J. Mol BioL, 1996, 262: 732). However, numbering according to the so-called Kabat system is preferred.
The term "amino acid" or "amino acid residue" typically refers to an amino acid having its definition recognized in the art, such as an amino acid selected from the group consisting of: alanine (Ala or A); arginine (Arg or R); asparagine (Asn or N), aspartic acid (Asp or D); cysteine (Cys or C); glutamine (Gln or Q), glutamic acid (Glu or E), glycine (Gly or G); histidine (His or H); isoleucine (He or I): leucine (Leu or L); lysine (Lys or K); methionine (Met or M); phenylalanine (Phe or F); proline (Pro or P), serine (Ser or S); threonine (Thr or T); tryptophan (Trp or W); tyrosine (Tyr or Y) and valine (Val or V), although modified, synthetic, or rare amino acids can be used as desired. Generally, amino acids can be grouped according to having a non-polar side chain (eg Ala, Cys, He, Leu, Met, Phe, Pro, Val); a negatively charged side chain (eg, Asp, Glu); a positively charged side chain (eg, Arg, His, Lys) or an uncharged polar side chain (eg, Asn, Gln Cys, Gly, His, Met, Phe, Ser, Thr, Trp, and Tyr).
IMPI
The term hypervariable region (also known as complementarity determining regions or CDRs) when used herein, refers to the amino acid residues of an antibody (usually three or four short regions of extreme sequence variability) that are within the domain of the V region of an immunoglobulin which forms the antigen-binding site and is the main determinant of antigen specificity. There are at least two methods for the 'identification of CDR residues: (1) An approach based on cross-species sequence variability (i.e. Kabat et al, loe cit.), And (2) An approach based on studies crystallography of antigen-antibody complexes (Chothia, C. et al, J. Mol BioL 196 901917 (1987)). However, to the extent that two residue identification techniques define regions of overlap, though not identical regions, they can be combined to define a hybrid CDR. However, in general, CDR residues are preferably identified according to the so-called Kabat (numbering) system.
The term "framework region" refers to the art-recognized portions of an antibody variable region that exist among the most divergent CDRs (ie, hypervariables). Such framework regions are typically referred to as framework region 1 to 4 (FR1, FR2, FR3, and FR4) and provide a scaffold for the presentation of the six CDRs (three heavy chain and three light chain) in a three-dimensional space, to form an antigen-binding surface.
Typically, CDRs form a loop structure that can be classified as a canonical structure. The term canonical structure refers to the conformation adopted by the main chain of antigen-binding loops (CDR). From comparative structural studies, it has been found that five of the six
INSTTH rro MUlCANí ω * la ηορίίΟΑΓ '. . rW<sup>r</sup>> HSTRIAt antigen only have a limited repertoire of conformations available. Each canonical structure can be characterized by the torsion angles of the polypeptide backbone. Corresponding bonds between antibodies can therefore have very similar three-dimensional structures, despite a high amino acid sequence variability in most of the bonds (Chothia and Lesk, J. Mol. Biol., 1987, 196: 901; Chothia eí al . Nature, 1989, 342: 877; Martin and Thornton, J. Mol. Biol., 1996, 263: 800, each of which is incorporated by reference in its entirety). Furthermore, there is a relationship between the structure adopted by the loop and the amino acid sequences that surround it. The conformation of a particular canonical class is determined by the length of the loop and the amino acid residues that reside at key positions within the loop, as well as within the region of conserved structure (ie outside the loop). Assignment to a particular canonical class, therefore, can be done on the basis of the presence of these key amino acid residues. The term "canonical structure" may also include considerations as to the linear sequence of the antibody, for example, as cataloged by Kabat (Kabat et al., Loe. Cit.). The Kabat numbering scheme (system) is a widely adopted standard for numbering the amino acid residues of an antibody variable domain in a consistent manner and is the preferred scheme applied in the present invention as also mentioned elsewhere in the document. Present. Additional structural considerations can also be used to determine the canonical structure of an antibody. For example, such differences not fully reflected by the Kabat numbering can be described by the numbering system of Chothia et al. and / or revealed by other techniques, eg, crystallography, and two- or three-dimensional computational modeling. Accordingly, a given antibody sequence can be placed in a canonical class that allows, among other things, proper identification
IMPI rNSTWUTO MhlICANf m the INDUSTRIAL rtopBDAt of chassis sequences (eg, based on the desire to include a variety of canonical structures in a library). Kabat numbering of antibody amino acid sequences and structural considerations described by Chothia et al., Loe. cit. and its implications for interpreting canonical aspects of antibody structure are described in the literature.
CDR3 is typically the largest source of molecular diversity within the antibody binding site. H3, for example, can be as short as two amino acid residues or longer than 26 amino acids. The subunit structures and three-dimensional configurations of different classes of immunoglobulins are well known in the art. For a review of the structure of antibodies, see Antibodies: A Laboratory Manual, Coid Spring Harbor Laboratory, eds. Harlow et al., 1988. One skilled in the art will recognize that each subunit structure, eg, a CH, VH, CL, VL, CDR, FR structure, comprises active fragments, eg, the portion of the VH, VL, or CDR subunit that binds to the antigen, ie, the antigen-binding fragment, or, for example, the portion of the CH subunit that binds and / or activates, for example, an Fe and / or complement receptor. CDRs are commonly referred to as Kabat CDRs, as described in "Sequences of Proteins of Immunological Interest, US Department of Health and Human Services" (1991), eds. Kabat et al. Another standard for characterizing the antigen-binding site is to refer to hypervariable loops as described by Chothia. See, for example, Chothia, et al. (1987, J. Mol. Biol. 227: 799817), and Tomlinson et al. (1995) EMBO J. 14: 4628-4638. Still another standard is the definition of AbM used by Oxford Molecular's AbM antibody modeling software. See generally, for example, "Protein Sequence and Structure Analysis of Antibody Variable Domains", in: Antibody Engineering Lab Manual (Ed .: Duebel, S. and Kontermann,
IMPI rwrmrroMUjcANc ·
OF THE INDUSTKIAL MYRITY
<img file="MX349396B_D0020.tif" />
R., Springer-Verlag, Heidelberg). The embodiments described with respect to the CDRs of
Kabat can alternatively be implemented using similar relationships described with respect to Chothia hypervariable loops or AbM-defined loops.
The sequence of antibody genes after assembly and somatic mutation is highly varied, and these varied genes are estimated to encode 10<sup>10</sup> different antibody molecules (Immunoglobulin Genes, 2<sup>to</sup> ed., Eds. Jomo et al., Academic Press, San Diego, CA, 1995). Consequently, the immune system provides a repertoire of immunoglobulins. The term "repertoire" refers to at least one nucleotide sequence wholly or partially derived from at least one sequence encoding at least one immunoglobulin. The sequence (s) can be generated by in vivo rearrangement of the V, D and J segments of the heavy chains, and the V and J segments of the light chains. Alternatively, the sequence (s) can be generated from a cell in response to what rearrangement occurs, eg, in vitro stimulation. Alternatively, part or all of the sequence (s) can be obtained by DNA splicing, nucleotide synthesis, mutagenesis, and other methods, see, for example, US Patent 5,565,332. A repertoire can include a single sequence or it can include a plurality of sequences, including those from a genetically varied collection.
In one embodiment, the first binding domain of the binding molecule of the invention comprises a VH region comprising CDR-H1, CDR-H2 and CDR-H3 and a VL region comprising CDR-L1, CDR-L2 and CDR- L3 selected from the group consisting of:
(1) CDR-H1 as described in SEQ ID NO: 1, CDR-H2 as described in
SEQ ID NO: 2, CDR-H3 as described in SEQ ID NO: 3, CDR-L1 as described
<img file="MX349396B_D0021.tif" />
ΓΈΙΛΛΟΡ1 £ Ο<sub>ΑΙ;</sub> , described in SEQ ID NO: 4, CDR-L2 as described in SEq'TidW or 'and as described in SEQ ID NO: 6;
<img file="MX349396B_D0022.tif" />
(2) CDR-H1 as described in SEQ ID NO: 11, CDR-H2 as described in SEQ ID NO: 12, CDR-H3 as described in SEQ ID NO: 13, CDR-L1 as described in SEQ ID NO: 14, CDR-L2 as described in SEQ ID NO: 15 and ODRES as described in SEQ ID NO: 16;
(3) CDR-H1 as described in SEQ ID NO: 21, CDR-H2 as described in SEQ ID NO: 22, CDR-H3 as described in SEQ ID NO: 23, CDR-L1 as described in SEQ ID NO: 24, CDR-L2 as described in SEQ ID NO: 25 and CDRL3 as described in SEQ ID NO: 26;
(4) CDR-H1 as described in SEQ ID NO: 31, CDR-H2 as described in SEQ ID NO: 32, CDR-H3 as described in SEQ ID NO: 33, CDR-L1 as described in SEQ ID NO: 34, CDR-L2 as described in SEQ ID NO: 35 and CDRL3 as described in SEQ ID NO: 36;
(5) CDR-H1 as described in SEQ ID NO: 41, CDR-H2 as described in SEQ ID NO: 42, CDR-H3 as described in SEQ ID NO: 43, CDR-L1 as described in SEQ ID NO: 44, CDR-L2 as described in SEQ ID NO: 45 and CDRL3 as described in SEQ ID NO: 46;
(6) CDR-H1 as described in SEQ ID NO: 51, CDR-H2 as described in SEQ ID NO: 52, CDR-H3 as described in SEQ ID NO: 53, CDR-L1 as described in SEQ ID NO: 54, CDR-L2 as described in SEQ ID NO: 55 and CDRL3 as described in SEQ ID NO: 56;
(7) CDR-H1 as described in SEQ ID NO: 61, CDR-H2 as described in SEQ ID NO: 62, CDR-H3 as described in SEQ ID NO: 63, CDR-L1 as described
ΙΜΡί @ ^ ίΝτπτυτο mexican <Ji
DE LA nOHEDAD described in SEQ ID NO: 64, CDR-L2 as described θη'βϊΦ + Ε) NrekaS-poDRL3 as described in SEQ ID NO: 66; -.
(8) CDR-H1 as described in SEQ ID NO: 71, CDR-H2 as described in SEQ ID NO: 72, CDR-H3 as described in SEQ ID NO: 73, CDR-L1 as described in SEQ ID NO: 74, CDR-L2 as described in SEQ ID NO: 75 and CDRL3 as described in SEQ ID NO: 76;
(9) CDR-H1 as described in SEQ ID NO: 161, CDR-H2 as described in SEQ ID NO: 162, CDR-H3 as described in SEQ ID NO: 163, CDR-L1 as described in SEQ ID NO: 164, CDR-L2 as described in SEQ ID NO: 165 and CDR-L3 as described in SEQ ID NO: 166;
(10) CDR-H1 as described in SEQ ID NO: 171, CDR-H2 as described in SEQ ID NO: 172, CDR-H3 as described in SEQ ID NO: 173, CDR-L1 as described in SEQ ID NO: 174, CDR-L2 as described in SEQ ID NO: 175 and CDR-L3 as described in SEQ ID NO: 176;
(11) CDR-H1 as described in SEQ ID NO: 181, CDR-H2 as described in SEQ ID NO: 182, CDR-H3 as described in SEQ ID NO: 183, CDR-L1 as described in SEQ ID NO: 184, CDR-L2 as described in SEQ ID NO: 185 and CDR-L3 as described in SEQ ID NO: 186;
(12) CDR-H1 as described in SEQ ID NO: 191, CDR-H2 as described in SEQ ID NO: 192, CDR-H3 as described in SEQ ID NO: 193, CDR-L1 as described in SEQ ID NO: 194, CDR-L2 as described in SEQ ID NO: 195 and CDR-L3 as described in SEQ ID NO: 196;
(13) CDR-H1 as described in SEQ ID NO: 201, CDR-H2 as described in
SEQ ID NO: 202, CDR-H3 as described in SEQ ID NO: 203, CDR-L1 as Mexican ΐΝϊττηπυ ** OWBDA O is described in SEQ ID NO: 204, CDR-L2 as described in ^ P ©<sup>1</sup>1D TwüW ^ and CDR-L3 as described in SEQ ID NO: 206; ** · * ..
(14) CDR-H1 as described in SEQ ID NO: 211, CDR-H2 as described in SEQ ID NO: 212, CDR-H3 as described in SEQ ID NO: 213, CDR-L1 as described in SEQ ID NO: 214, CDR-L2 as described in SEQ ID NO: 215 and CDR-L3 as described in SEQ ID NO: 216;
(15) CDR-H1 as described in SEQ ID NO: 221, CDR-H2 as described in SEQ ID NO: 222, CDR-H3 as described in SEQ ID NO: 223, CDR-L1 as described in SEQ ID NO: 224, CDR-L2 as described in SEQ ID NO: 225 and CDR-L3 as described in SEQ ID NO: 226;
(16) CDR-H1 as described in SEQ ID NO: 311, CDR-H2 as described in SEQ ID NO: 312, CDR-H3 as described in SEQ ID NO: 313, CDR-L1 as described in SEQ ID NO: 314, CDR-L2 as described in SEQ ID NO: 315 and CDR-L3 as described in SEQ ID NO: 316;
(17) CDR-H1 as described in SEQ ID NO: 321, CDR-H2 as described in SEQ ID NO: 322, CDR-H3 as described in SEQ ID NO: 323, CDR-L1 as described in SEQ ID NO: 324, CDR-L2 as described in SEQ ID NO: 325 and CDR-L3 as described in SEQ ID NO: 326;
(18) CDR-H1 as described in SEQ ID NO: 331, CDR-H2 as described in SEQ ID NO: 332, CDR-H3 as described in SEQ ID NO: 333, CDR-L1 as described in SEQ ID NO: 334, CDR-L2 as described in SEQ ID NO: 335 and CDR-L3 as described in SEQ ID NO: 336;
(19) CDR-H1 as described in SEQ ID NO: 341, CDR-H2 as described in
SEQ ID NO: 342, CDR-H3 as described in SEQ ID NO: 343, CDR-L1 as described in SEQ ID NO: 344, CDR-L2 as described in SEQ ID ΝΟΓ345 and CDR-L3 as described in SEQ ID NO: 346; —————— (20) CDR-H1 as described in SEQ ID NO: 351, CDR-H2 as described in SEQ ID NO: 352, CDR-H3 as described in SEQ ID NO: 353, CDR- L1 as described in SEQ ID NO: 354, CDR-L2 as described in SEQ ID NO: 355 and CDR-L3 as described in SEQ ID NO: 356;
(21) CDR-H1 as described in SEQ ID NO: 361, CDR-H2 as described in SEQ ID NO: 362, CDR-H3 as described in SEQ ID NO: 363, CDR-L1 as described in SEQ ID NO: 364, CDR-L2 as described in SEQ ID NO: 365 and CDR-L3 as described in SEQ ID NO: 366;
(22) CDR-H1 as described in SEQ ID NO: 371, CDR-H2 as described in SEQ ID NO: 372, CDR-H3 as described in SEQ ID NO: 373, CDR-L1 as described in SEQ ID NO: 374, CDR-L2 as described in SEQ ID NO: 375 and CDR-L3 as described in SEQ ID NO: 376;
(23) CDR-H1 as described in SEQ ID NO: 381, CDR-H2 as described in SEQ ID NO: 382, CDR-H3 as described in SEQ ID NO: 383, CDR-L1 as described in SEQ ID NO: 384, CDR-L2 as described in SEQ ID NO: 385 and CDR-L3 as described in SEQ ID NO: 386;
(24) CDR-H1 as described in SEQ ID NO: 581, CDR-H2 as described in SEQ ID NO: 582, CDR-H3 as described in SEQ ID NO: 583, CDR-L1 as described in SEQ ID NO: 584, CDR-L2 as described in SEQ ID NO: 585 and CDR-L3 as described in SEQ ID NO: 586;
(25) CDR-H1 as described in SEQ ID NO: 591, CDR-H2 as described in SEQ ID NO: 592, CDR-H3 as described in SEQ ID NO: 593, CDR-L1 as
IMPI INSTITUTO MBUCANC »» LA ΚΟΡΙίΠΑΌ INDUSTRIAL is described in SEQ ID NO: 594, CDR-L2 as described in SEQ ID NO: 595 and
CDR-L3 as described in SEQ ID NO: 596; '(26) CDR-H1 as described in SEQ ID NO: 601, CDR-H2 as described in
SEQ ID NO: 602, CDR-H3 as described in SEQ ID NO: 603, CDR-L1 as described in SEQ ID NO: 604, CDR-L2 as described in SEQ ID NO: 605 and
CDR-L3 as described in SEQ ID NO: 606;
(27) CDR-H1 as described in SEQ ID NO: 611, CDR-H2 as described in
SEQ ID NO: 612, CDR-H3 as described in SEQ ID NO: 613, CDR-L1 as described in SEQ ID NO: 614, CDR-L2 as described in SEQ ID NO: 615 and
CDR-L3 as described in SEQ ID NO: 616;
(28) CDR-H1 as described in SEQ ID NO: 621, CDR-H2 as described in
SEQ ID NO: 622, CDR-H3 as described in SEQ ID NO: 623, CDR-L1 as described in SEQ ID NO: 624, CDR-L2 as described in SEQ ID NO: 625 and
CDR-L3 as described in SEQ ID NO: 626;
(29) CDR-H1 as described in SEQ ID NO: 631, CDR-H2 as described in
SEQ ID NO: 632, CDR-H3 as described in SEQ ID NO: 633, CDR-L1 as described in SEQ ID NO: 634, CDR-L2 as described in SEQ ID NO: 635 and
CDR-L3 as described in SEQ ID NO: 636;
(30) CDR-H1 as described in SEQ ID NO: 641, CDR-H2 as described in
SEQ ID NO: 642, CDR-H3 as described in SEQ ID NO: 643, CDR-L1 as described in SEQ ID NO: 644, CDR-L2 as described in SEQ ID NO: 645 and
CDR-L3 as described in SEQ ID NO: 646;
(31) CDR-H1 as described in SEQ ID NO: 651, CDR-H2 as described in
SEQ ID NO: 652, CDR-H3 as described in SEQ ID NO: 653, CDR-L1 as
<img file="MX349396B_D0023.tif" />
described in SEQ ID NO: 654, CDR-L2 as described in SEQ ID NO: 655 and CDR-L3 as described in SEQ ID NO: 656;
(32) CDR-H1 as described in SEQ ID NO: 661, CDR-H2 as described in SEQ ID NO: 662, CDR-H3 as described in SEQ ID NO: 663, CDR-L1 as described in SEQ ID NO: 664, CDR-L2 as described in SEQ ID NO: 665 and CDR-L3 as described in SEQ ID NO: 666;
(33) CDR-H1 as described in SEQ ID NO: 671, CDR-H2 as described in SEQ ID NO: 672, CDR-H3 as described in SEQ ID NO: 673, CDR-L1 as described in SEQ ID NO: 674, CDR-L2 as described in SEQ ID NO: 675 and CDR-L3 as described in SEQ ID NO: 676;
(34) CDR-H1 as described in SEQ ID NO: 681, CDR-H2 as described in SEQ ID NO: 682, CDR-H3 as described in SEQ ID NO: 683, CDR-L1 as described in SEQ ID NO: 684, CDR-L2 as described in SEQ ID NO: 685 and CDR-L3 as described in SEQ ID NO: 686;
(35) CDR-H1 as described in SEQ ID NO: 691, CDR-H2 as described in SEQ ID NO: 692, CDR-H3 as described in SEQ ID NO: 693, CDR-L1 as described in SEQ ID NO: 694, CDR-L2 as described in SEQ ID NO: 695 and CDR-L3 as described in SEQ ID NO: 696;
(36) CDR-H1 as described in SEQ ID NO: 701, CDR-H2 as described in SEQ ID NO: 702, CDR-H3 as described in SEQ ID NO: 703, CDR-L1 as described in SEQ ID NO: 704, CDR-L2 as described in SEQ ID NO: 705 and CDR-L3 as described in SEQ ID NO: 706;
(37) CDR-H1 as described in SEQ ID NO: 711, CDR-H2 as described in SEQ ID NO: 712, CDR-H3 as described in SEQ ID NO: 713, CDR-L1 as
ΪΜΡΙ @ ^ 'Μππ * τοΜυοΑΝτ> «SCbcS / í» D * ΙΑ ROFIEDAO is described in SEQ ID NO: 714, CDR-L2 as described in ^ ÉO IDnO ^ l ^ and CDR-L3 as described in SEQ ID NO : 716; '' .....— (38) CDR-H1 as described in SEQ ID NO: 721, CDR-H2 as described in SEQ ID NO: 722, CDR-H3 as described in SEQ ID NO: 723, CDR-L1 as described in SEQ ID NO: 724, CDR-L2 as described in SEQ ID NO: 725 and CDR-L3 as described in SEQ ID NO: 726;
(39) CDR-H1 as described in SEQ ID NO: 731, CDR-H2 as described in SEQ ID NO: 732, CDR-H3 as described in SEQ ID NO: 733, CDR-L1 as described in SEQ ID NO: 734, CDR-L2 as described in SEQ ID NO: 735 and CDR-L3 as described in SEQ ID NO: 736;
(40) CDR-H1 as described in SEQ ID NO: 741, CDR-H2 as described in SEQ ID NO: 742, CDR-H3 as described in SEQ ID NO: 743, CDR-L1 as described in SEQ ID NO: 744, CDR-L2 as described in SEQ ID NO: 745 and CDR-L3 as described in SEQ ID NO: 746;
(41) CDR-H1 as described in SEQ ID NO: 751, CDR-H2 as described in SEQ ID NO: 752, CDR-H3 as described in SEQ ID NO: 753, CDR-L1 as described in SEQ ID NO: 754, CDR-L2 as described in SEQ ID NO: 755 and CDR-L3 as described in SEQ ID NO: 756;
(42) CDR-H1 as described in SEQ ID NO: 761, CDR-H2 as described in SEQ ID NO: 762, CDR-H3 as described in SEQ ID NO: 763, CDR-L1 as described in SEQ ID NO: 764, CDR-L2 as described in SEQ ID NO: 765 and CDR-L3 as described in SEQ ID NO: 766;
(43) CDR-H1 as described in SEQ ID NO: 771, CDR-H2 as described in SEQ ID NO: 772, CDR-H3 as described in SEQ ID NO: 773, CDR-L1 as
IMPI ^ -5 is described in SEQ ID NO: 774, CDR-L2 as described in'í ^ & ílb
CDR-L3 as described in SEQ ID NO: 776; - ---. . _ (44) CDR-H1 as described in SEQ ID NO: 781, CDR-H2 as described in
SEQ ID NO: 782, CDR-H3 as described in SEQ ID NO: 783, CDR-L1 as described in SEQ ID NO: 784, CDR-L2 as described in SEQ ID NO: 785 and CDR-L3 as described described in SEQ ID NO: 786;
(45) CDR-H1 as described in SEQ ID NO: 791, CDR-H2 as described in SEQ ID NO: 792, CDR-H3 as described in SEQ ID NO: 793, CDR-L1 as described in SEQ ID NO: 794, CDR-L2 as described in SEQ ID NO: 795 and CDR-L3 as described in SEQ ID NO: 796;
(46) CDR-H1 as described in SEQ ID NO: 801, CDR-H2 as described in SEQ ID NO: 802, CDR-H3 as described in SEQ ID NO: 803, CDR-L1 as described in SEQ ID NO: 804, CDR-L2 as described in SEQ ID NO: 805 and CDR-L3 as described in SEQ ID NO: 806;
(47) CDR-H1 as described in SEQ ID NO: 811, CDR-H2 as described in SEQ ID NO: 812, CDR-H3 as described in SEQ ID NO: 813, CDR-L1 as described in SEQ ID NO: 814, CDR-L2 as described in SEQ ID NO: 815 and CDR-L3 as described in SEQ ID NO: 816;
(48) CDR-H1 as described in SEQ ID NO: 821, CDR-H2 as described in SEQ ID NO: 822, CDR-H3 as described in SEQ ID NO: 823, CDR-L1 as described in SEQ ID NO: 824, CDR-L2 as described in SEQ ID NO: 825 and CDR-L3 as described in SEQ ID NO: 826;
(49) CDR-H1 as described in SEQ ID NO: 831, CDR-H2 as described in SEQ ID NO: 832, CDR-H3 as described in SEQ ID NO: 833, CDR-L1 as "πττυτο μ" χκ?<sub>αν</sub><
** * PRONidai, is described in SEQ ID NO: 834, CDR-L2 as described ^ SÉQ 1W®M »5 and CDR-L3 as described in SEQ ID NO: 836; · —------ _ (50) CDR-H1 as described in SEQ ID NO: 961, CDR-H2 as described in SEQ ID NO: 962, CDR-H3 as described in SEQ ID NO: 963 , CDR-L1 as described in SEQ ID NO: 964, CDR-L2 as described in SEQ ID NO: 965 and CDR-L3 as described in SEQ ID NO: 966;
(51) CDR-H1 as described in SEQ ID NO: 971, CDR-H2 as described in SEQ ID NO: 972, CDR-H3 as described in SEQ ID NO: 973, CDR-L1 as described in SEQ ID NO: 974, CDR-L2 as described in SEQ ID NO: 975 and CDR-L3 as described in SEQ ID NO: 976;
(52) CDR-H1 as described in SEQ ID NO: 981, CDR-H2 as described in SEQ ID NO: 982, CDR-H3 as described in SEQ ID NO: 983, CDR-L1 as described in SEQ ID NO: 984, CDR-L2 as described in SEQ ID NO: 985 and CDR-L3 as described in SEQ ID NO: 986; and (53) CDR-H1 as described in SEQ ID NO: 991, CDR-H2 as described in SEQ ID NO: 992, CDR-H3 as described in SEQ ID NO: 993, CDR-L1 as described in SEQ ID NO: 994, CDR-L2 as described in SEQ ID NO: 995 and CDR-L3 as described in SEQ ID NO: 996.
In yet another embodiment, the first binding domain of the binding molecule comprises a VH region selected from the group consisting of a VH region as described in SEQ ID NO: 7, SEQ ID NO: 17, SEQ ID NO: 27, SEQ ID NO: 37, SEQ ID NO: 47, SEQ ID NO: 57, SEQ ID NO: 67, SEQ ID NO: 77, SEQ ID NO: 167, SEQ ID NO: 177, SEQ ID NO: 187, SEQ ID NO: 197, SEQ ID NO: 207, SEQ ID NO: 217, SEQ ID NO: 227, SEQ ID NO: 317, SEQ ID NO: 327, SEQ ID NO: 337, SEQ ID NO: 347, SEQ ID NO: 357,
IMPI
SEQ ID NO: 367, SEQ ID NO: 377, SEQ ID NO: 387, SEQ ID NO: 587, SEQ ID NO: 597,
SEQ ID NO: 607, SEQ ID NO: 617, SEQ ID NO: 627, SEQ ID NO: 637, SEQ ID NO: 647,
SEQ ID NO: 657, SEQ ID NO: 667, SEQ ID NO: 677, SEQ ID NO: 687, SEQ ID NO: 697,
SEQ ID NO: 707, SEQ ID NO: 717, SEQ ID NO: 727, SEQ ID NO: 737, SEQ ID NO: 747,
SEQ ID NO: 757, SEQ ID NO: 767, SEQ ID NO: 777, SEQ ID NO: 787, SEQ ID NO: 797,
SEQ ID NO: 807, SEQ ID NO: 817, SEQ ID NO: 827, SEQ ID NO: 837, SEQ ID NO: 967,
SEQ ID NO: 977, SEQ ID NO: 987, and SEQ ID NO: 997.
In another embodiment, the first binding domain of the binding molecule comprises a VL region selected from the group consisting of a VL region as described in SEQ ID in SEQ ID NO: 8, SEQ ID NO: 18, SEQ ID NO: 28, SEQ ID NO: 38, SEQ ID NO: 48, SEQ ID NO: 58, SEQ ID NO: 68, SEQ ID NO: 78, SEQ ID NO: 168, SEQ ID NO: 178, SEQ ID NO: 188, SEQ ID NO: 198, SEQ ID NO: 208, SEQ ID NO: 218, SEQ ID
NO: 228, SEQ ID NO: 318, SEQ ID NO: 328, SEQ ID NO: 338, SEQ ID NO: 348, SEQ ID
NO: 358, SEQ ID NO: 368, SEQ ID NO: 378, SEQ ID NO: 388, SEQ ID NO: 588, SEQ ID
NO: 598, SEQ ID NO: 608, SEQ ID NO: 618, SEQ ID NO: 628, SEQ ID NO: 638, SEQ ID
NO: 648, SEQ ID NO: 658, SEQ ID NO: 668, SEQ ID NO: 678, SEQ ID NO: 688, SEQ ID
NO: 698, SEQ ID NO: 708, SEQ ID NO: 718, SEQ ID NO: 728, SEQ ID NO: 738, SEQ ID
NO: 748, SEQ ID NO: 758, SEQ ID NO: 768, SEQ ID NO: 778, SEQ ID NO: 788, SEQ ID
NO: 798, SEQ ID NO: 808, SEQ ID NO: 818, SEQ ID NO: 828, SEQ ID NO: 838, SEQ ID
NO: 968, SEQ ID NO: 978, SEQ ID NO: 988, and SEQ ID NO: 998.
In one embodiment, the first binding domain of the binding molecule comprises a VH region and a VL region selected from the group consisting of:
IMPIí
Mexican WIiilTO is (1) a VH region as described in SEQ ID NO: 7, and one ^^^^ ion is described in SEQ ID NO: 8; .
(2) a VH region as described in SEQ ID NO: 17, and a VL region as described in SEQ ID NO: 18;
(3) a VH region as described in SEQ ID NO: 27, and a VL region as described in SEQ ID NO: 28;
(4) a VH region as described in SEQ ID NO: 37, and a VL region as described in SEQ ID NO: 38;
(5) a VH region as described in SEQ ID NO: 47, and a VL region as described in SEQ ID NO: 48;
(6) a VH region as described in SEQ ID NO: 57, and a VL region as described in SEQ ID NO: 58;
(7) a VH region as described in SEQ ID NO: 67, and a VL region as described in SEQ ID NO: 68;
(8) a VH region as described in SEQ ID NO: 77, and a VL region as described in SEQ ID NO: 78;
(9) a VH region as described in SEQ ID NO: 167, and a VL region as described in SEQ ID NO: 168;
(10) a VH region as described in SEQ ID NO: 177, and a VL region as described in SEQ ID NO: 178;
(11) a VH region as described in SEQ ID NO: 187, and a VL region as described in SEQ ID NO: 188;
(12) a VH region as described in SEQ ID NO: 197, and a VL region as described in SEQ ID NO: 198;
<img file="MX349396B_D0024.tif" />
IMPI WSTm> TC m »¡c<sub>to</sub>n < <sup>nF</sup> INDUSTRIAL LA ΓΚΟΡΙΕΡΑΩ (13) a VH region as described in SEQ ID NO: 207, and a VL region as described in SEQ ID NO: 208;
(14) a VH region as described in SEQ ID NO: 217, and a VL region as described in SEQ ID NO: 218;
(15) a VH region as described in SEQ ID NO: 227, and a VL region as described in SEQ ID NO: 228;
(16) a VH region as described in SEQ ID NO: 317, and a VL region as described in SEQ ID NO: 318;
(17) a VH region as described in SEQ ID NO: 327, and a VL region as described in SEQ ID NO: 328;
(18) a VH region as described in SEQ ID NO: 337, and a VL region as described in SEQ ID NO: 338;
(19) a VH region as described in SEQ ID NO: 347, and a VL region as described in SEQ ID NO: 348;
(20) a VH region as described in SEQ ID NO: 357, and a VL region as described in SEQ ID NO: 358;
(21) a VH region as described in SEQ ID NO: 367, and a VL region as described in SEQ ID NO: 368;
(22) a VH region as described in SEQ ID NO: 377, and a VL region as described in SEQ ID NO: 378;
(23) a VH region as described in SEQ ID NO: 387, and a VL region as described in SEQ ID NO: 388;
(24) a VH region as described in SEQ ID NO: 587, and a VL region as described in SEQ ID NO: 588;
iwrmrrc müucanc DE LA FBOPIEDAI 'INDUSTRIAL (25) a VH region as described in SEQ ID NO: 597, and a VL region as described in SEQ ID NO: 598;
(26) a VH region as described in SEQ ID NO: 607, and a VL region as described in SEQ ID NO: 608;
(27) a VH region as described in SEQ ID NO: 617, and a VL region as described in SEQ ID NO: 618;
(28) a VH region as described in SEQ ID NO: 627, and a VL region as described in SEQ ID NO: 628;
(29) a VH region as described in SEQ ID NO: 637, and a VL region as described in SEQ ID NO: 638;
(30) a VH region as described in SEQ ID NO: 647, and a VL region as described in SEQ ID NO: 648;
(31) a VH region as described in SEQ ID NO: 657, and a VL region as described in SEQ ID NO: 658;
(32) a VH region as described in SEQ ID NO: 667, and a VL region as described in SEQ ID NO: 668;
(33) a VH region as described in SEQ ID NO: 677, and a VL region as described in SEQ ID NO: 678;
(34) a VH region as described in SEQ ID NO: 687, and a VL region as described in SEQ ID NO: 688;
(35) a VH region as described in SEQ ID NO: 697, and a VL region as described in SEQ ID NO: 698;
(36) a VH region as described in SEQ ID NO: 707, and a VL region as described in SEQ ID NO: 708;
I ΝΕΤΗ Mexican UTO
Ot LA WOHEOAD INDOSTRIA L (37) a VH region as described in SEQ ID NO: 717, and a VL region as described in SEQ ID NO: 718;
(38) a VH region as described in SEQ ID NO: 727, and a VL region as described in SEQ ID NO: 728;
(39) a VH region as described in SEQ ID NO: 737, and a VL region as described in SEQ ID NO: 738;
(40) a VH region as described in SEQ ID NO: 747, and a VL region as described in SEQ ID NO: 748;
(41) a VH region as described in SEQ ID NO: 757, and a VL region as described in SEQ ID NO: 758;
(42) a VH region as described in SEQ ID NO: 767, and a VL region as described in SEQ ID NO: 768;
(43) a VH region as described in SEQ ID NO: 777, and a VL region as described in SEQ ID NO: 778;
(44) a VH region as described in SEQ ID NO: 787, and a VL region as described in SEQ ID NO: 788;
(45) a VH region as described in SEQ ID NO: 797, and a VL region as described in SEQ ID NO: 798;
(46) a VH region as described in SEQ ID NO: 807, and a VL region as described in SEQ ID NO: 808;
(47) a VH region as described in SEQ ID NO: 817, and a VL region as described in SEQ ID NO: 818;
(48) a VH region as described in SEQ ID NO: 827, and a VL region as described in SEQ ID NO: 828;
(49) a VH region as described in SEQ ID N as described in SEQ ID NO: 838;
(50) a VH region as described in SEQ ID NO: 967, and a VL region as described in SEQ ID NO: 968;
(51) a VH region as described in SEQ ID NO: 977, and a VL region as described in SEQ ID NO: 978;
(52) a VH region as described in SEQ ID NO: 987, and a VL region as described in SEQ ID NO: 988; and (53) a VH region as described in SEQ ID NO: 997, and a VL region as described in SEQ ID NO: 998.
In one example, the first binding domain comprises an amino acid sequence selected from the group consisting of SEQ ID NO: 9, SEQ ID NO: 19, SEQ ID NO: 29, SEQ ID NO: 39, SEQ ID NO: 49, SEQ ID NO: 59, SEQ ID NO: 69, SEQ ID NO: 79, SEQ ID NO: 169, SEQ ID NO: 179, SEQ ID NO: 189, SEQ ID NO: 199, SEQ ID NO: 209,
SEQ ID NO: 219, SEQ ID NO: 229, SEQ ID NO: 319, SEQ ID NO: 329, SEQ ID NO: 339,
SEQ ID NO: 349, SEQ ID NO: 359, SEQ ID NO: 369, SEQ ID NO: 379, SEQ ID NO: 389,
SEQ ID NO: 589, SEQ ID NO: 599, SEQ ID NO: 609, SEQ ID NO: 619, SEQ ID NO: 629,
SEQ ID NO: 639, SEQ ID NO: 649, SEQ ID NO: 659, SEQ ID NO: 669, SEQ ID NO: 679,
SEQ ID NO: 689, SEQ ID NO: 699, SEQ ID NO: 709, SEQ ID NO: 719, SEQ ID NO: 729,
SEQ ID NO: 739, SEQ ID NO: 749, SEQ ID NO: 759, SEQ ID NO: 769, SEQ ID NO: 779,
SEQ ID NO: 789, SEQ ID NO: 799, SEQ ID NO: 809, SEQ ID NO: 819, SEQ ID NO: 829,
SEQ ID NO: 839, SEQ ID NO: 969, SEQ ID NO: 979, SEQ ID NO: 989, and SEQ ID
NO: 999.
<img file="MX349396B_D0025.tif" />
It is preferred that a binding molecule of the present invention have a CUR-IT3 region 12 amino acids long, wherein a tyrosine residue (Y) is present at positions 3, 4, and 12. A preferred CDR-H3 is shown. in SEQ ID NOs: 43, 193, 333, 613, 703, 733, 823, or 973. Consequently, a binding molecule of the present invention has in a preferred embodiment a CDR-H3 shown in SEQ ID NOS : 43, 193, 333, 613, 703, 733, 823, or 973
A binding molecule having the amino acid sequence shown in SEQ ID NO: 340 is preferred. A binding molecule having the amino acid sequence shown in or SEQ ID NO: 980 is also preferred.
The binding molecule of the present invention is preferably an isolated binding molecule. Isolated when used to describe the binding molecule described herein, it means a binding molecule that has been identified, separated and / or recovered from a component of its production environment. Preferably, the isolated binding molecule is free of association with all other components of its production environment. Contaminating components from your production environment, such as those resulting from recombinant transfected cells, are materials that would typically interfere with the diagnostic or therapeutic uses of the polypeptide, and may include enzymes, hormones, and other proteinaceous or non-proteinaceous solutes. In preferred embodiments, the binding molecule will be purified (1) to a degree sufficient to obtain at least 15 N-terminal amino acid sequence or internal amino acid sequence residues using a spinning cup sequencer, or (2) to homogeneity by SDS-PAGE under non-reducing or reducing conditions using Coomassie blue or, preferably, silver staining.
<img file="MX349396B_D0026.tif" />
'^' TnTP'lg'ÍCANC CE LA Ρ * ΟΡΙ £ ΠΑΙ 'iwusniAi
Usually, however, an isolated antibody will be prepared by at least one purification step.
Modifications of the amino acid sequence of the binding molecules described herein are contemplated. For example, it may be desirable to improve the binding affinity and / or other biological properties of the antibody. Amino acid sequence variants of the binding molecules are prepared by introducing appropriate nucleotide changes in the nucleic acid of the binding molecules, or by peptide synthesis.
Such modifications include, for example, deletions of, and / or insertions at, and / or substitutions of, residues within the amino acid sequences of the binding molecules. Any combination of deletion, insertion, and substitution is done to arrive at the final construct, as long as the final construct possesses the desired characteristics. Amino acid changes can also alter the post-translational processes of the binding molecules, such as changing the number or position of glycosylation sites. Preferably, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 amino acids can be substituted in a CDR, while 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, or 25 amino acids can be substituted in the framework regions (FR). The substitutions are preferably conservative substitutions as described herein. Additionally or alternatively, 1, 2, 3, 4, 5, or 6 amino acids can be inserted or deleted in each of the CDRs (of course, depending on their length), while 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, or 25 amino acids can be inserted or deleted in each of the FRs.
<img file="MX349396B_D0027.tif" />
<sup>fr</sup> fA KOMSOAH inhustrial
A useful method for identifying certain residues or regions of binding molecules that are preferred locations for mutagenesis is called alanine screening mutagenesis, as described by Cunningham and Wells in Science, 244: 1081-1085 (1989). Here, a residue or group of target residues within the binding molecule is / are identified (for example, charged residues such as Arg, Asp, His, Lys, and Glu) and replaced with a neutral or negatively charged amino acid (which more preferably alanine or polyalanine) to affect the interaction of amino acids with the epitope.
Those amino acid locations that demonstrate functional sensitivity to substitutions are then refined by introducing additional variants or other variants at, or for, the substitution sites. Thus, while the site for introducing an amino acid sequence variation is predetermined, the nature of the mutation per se need not be predetermined. For example, to analyze the performance of a mutation at a given site, Ala screening or random mutagenesis is performed at a target codon or region and expressed variants of the binding molecule are screened for the desired activity.
Preferably, insertions in the amino acid sequence include amino and / or carboxy-terminal fusions ranging in length from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 residues, to polypeptides containing one hundred or more more residues, as well as intrasequence insertions of single or multiple amino acid residues. An insertion variant of the binding molecule includes fusion to the N- or C-terminus of the antibody to an enzyme or a fusion to a polypeptide that increases the serum half-life of the antibody.
IMPI
INSTITUTO MiXIGANC DE LA raOPt £ »AD INDUSTRIAL
Another type of variant is an amino acid substitution variant. These variants preferably have at least 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 amino acid residues in the linker molecule replaced by a different residue. Sites of greatest interest for substitutional mutagenesis include the heavy and / or light chain CDRs, particularly the hypervariable regions, but FR alterations in the heavy and / or light chain are also contemplated.
For example, if a CDR sequence comprises 6 amino acids, it is contemplated that one, two, or three of these amino acids are substituted. Similarly, if a CDR sequence comprises 15 amino acids it is contemplated that one, two, three, four, five or six of these amino acids are substituted.
In general, if the amino acids are substituted in one or more or all of the heavy and / or light chain CDRs, it is preferred that the substituted sequence thus obtained is at least 60%, more preferably 65%, even more preferably 70%, particularly preferably 75%, more particularly preferably 80%, identical to the original CDR sequence. This means that the degree of identity of the substituted sequence depends on the length of the CDR. For example, a CDR that has 5 amino acids is preferably 80% identical to its substituted sequence in order to have at least one substituted amino acid. Accordingly, the CDRs of the binding molecule can have different degrees of identity to their substituted sequences, eg CDRL1 can be 80%, while CDRL3 can be 90%.
Preferred substitutions (or replacements) are conservative substitutions. However, any substitution is contemplated (including non-conservative substitution
ΙΝΤΓΙΠΤΟΜβΙΌΑΝί faíegXi.
or one or more of the example substitutions listed '^ grF ^ a' TablSS ^ below) as long as the binding molecule retains ou -oapQoity to bind BCMA through the first binding domain and CD3 epsilon through of the second binding domain and / or its CDRs have an identity with the then substituted sequence (at least 60%, more preferably 65%, even more preferably 70%, particularly preferably 75%, more particularly preferably 80%, identical to the original CDR sequence).
Conservative substitutions are shown in Table 1 under the heading of preferred substitutions. If such substitutions result in a change in biological activity, then more substantial changes can be introduced, referred to as example substitutions in Table 1, or as described below with reference to the classes of amino acids, and the products examined for a characteristic. desired.
Table 1: Amino Acid Substitutions
<td>Original</td><td>Example Substitutions</td><td>Preferred Substitutions</td>
<td>Wing (A)</td><td>Val, Leu, lie</td><td>Val</td>
<td>Arg (R)</td><td>Lys, Gln, Asn</td><td>Lys</td>
<td>Asn (N)</td><td>Gln, His, Asp, Lys, Arg</td><td>Gln</td>
<td>Asp (D)</td><td>Glu, Asn</td><td>Glu</td>
<td>Cys (C)</td><td>It will be the</td><td>To be</td>
<td>Gln (Q)</td><td>Asn, Glu</td><td>Asn</td>
<td>Glu (E)</td><td>Asp, Gln</td><td>Asp</td>
<td>Gly (G)</td><td>To</td><td>To</td>
<img file="MX349396B_D0028.tif" />
IMPI
INSTITUTO MEXICANO ni ΙΑ ΛΟΜίΟΑΙί iNnumtAi.
<td rowspan="2">His (H)</td><td rowspan="2">Asn, Gln, Lys, Arg</td><td>Arg</td>
<td></td>
<td>He (I)</td><td>Leu, Val, Met, Ala, Phe</td><td>Leu</td>
<td>Leu (L)</td><td>norleucine, lie, Val, Met, Ala</td><td>I have</td>
<td>Lys (K)</td><td>Arg, Gln, Asn</td><td>Arg</td>
<td>Met (M)</td><td>Leu, Phe, He</td><td>Leu</td>
<td>Phe (F)</td><td>Leu, Val, He, Ala, Tyr</td><td>Tyr</td>
<td>Pro (P)</td><td>To</td><td>To</td>
<td>Be (S)</td><td>Thr</td><td>Thr</td>
<td>Thr (T)</td><td>To be</td><td>To be</td>
<td>Trp (W)</td><td>Tyr, Phe</td><td>Tyr</td>
<td>Tyr (Y)</td><td>Trp, Phe, Thr, Ser</td><td>Phe</td>
<td>Val (V)</td><td>lie, Leu, Met, Phe, Ala</td><td>Leu</td>
Substantial modifications in the biological properties of the binding molecule of the present invention are carried out by selecting substitutions that differ significantly in their effect of maintaining (a) the structure of the polypeptide backbone in the area of substitution, for example , as a sheet or helical conformation, (b) the charge or hydrophobicity of the molecule at the target site, or (c) the volume of the side chain. Naturally occurring residues are divided into groups based on common side chain properties: (1) hydrophobic: norleucine, Met, Ala, Val, Leu, lie, (2) neutral hydrophilic: Cys, Ser, Thr; (3) acids: Asp, Glu, (4) basic: Asn, Gln, His, Lys, Arg; (5) residues that influence the orientation of the chain: Gly, Pro; and (6): aromatic: Trp, Tyr, Phe.
<sup>69</sup> IMPI
INSTITUTO MUKUMc OS IA PROCEED! industrial
Non-conservative substitutions will involve exchanging a member of one of these classes for another class. Any cysteine residue not involved in maintaining the proper conformation of the binding molecule can be substituted, generally with serine, to improve the oxidative stability of the molecule and avoid aberrant crosslinking. Conversely, cysteine linkage (s) can be added to the antibody to improve its stability (particularly when the antibody is an antibody fragment such as an Fv fragment).
A particularly preferred type of substitutional variant involves the substitution of one or more residues from the hypervariable region of a parent antibody (eg, a humanized or human antibody). Generally, the resulting variant (s) selected for further development will have improved biological properties relative to the parent antibody from which they are generated. A convenient way to generate such substitutional variants involves affinity maturation using phage display. Briefly, several sites in the hypervariable region (eg, 6-7 sites) are mutated to generate all possible amino acid substitutions at each site. The antibody variants thus generated are presented monovalently from filamentous phage particles in the form of fusions to the M13 gene III product packaged within each particle. Phage-displayed variants are then screened for their biological activity (eg, binding affinity) as described herein. In order to identify candidate hypervariable region sites for modification, alanine screening mutagenesis can be performed to identify hypervariable region residues that contribute significantly to antigen binding. Alternatively, or additionally, it may be beneficial to analyze a crystal structure of the antigen-antibody complex for
<img file="MX349396B_D0029.tif" />
The Mexican institute of the PROEIíDao identify points of contact between the binding domain and, for example, WWIA nCrmSS Such contact residues and neighboring residues are candidates for the use of a guide. the techniques developed in the present. Once those variants are generated, the panel of variants is screened as described herein and antibodies with superior properties in one or more relevant assays can be selected for further development.
Other modifications of the binding molecule are contemplated herein. For example, the binding molecule can be attached to one of a variety of non-protein polymers, eg, polyethylene glycol, polypropylene glycol, polyoxyalkylenes, or copolymers of polyethylene glycol and polypropylene glycol. The binding molecule may also be entrapped in microcapsules prepared, for example, by coacervation techniques or by interfacial polymerization (for example, hydroxymethylcellulose or gelatin microcapsules and poly (methylmethacrylate) microcapsules, respectively), in colloidal delivery systems of drugs (eg, liposomes, albumin microspheres, microemulsions, nanoparticles and nanocapsules) or in macroemulsions. Such techniques are described in Remington's Pharmaceutical Sciences, 16 <sup>to</sup> edition, Oslo, A., Ed., (1980).
The binding molecules described herein can also be formulated as immunoliposomes. A liposome is a small vesicle composed of various types of lipids, phospholipids, and / or surfactants that is useful for the administration of a drug to a mammal. The components of the liposome are commonly arranged in a bilayer formation, similar to the arrangement of lipids in biological membranes. Liposomes containing the antibody are prepared by methods known in <sup>71</sup> iNsmvromuicanc
OF THE INDUSTRIAL PROPERTY technique, such as those described in Epstein et al., Proc. Nati. Acad. Sci. USA, 82: 3688 (1985); Hwang et al. , Proc. Nati. Acad. Sci. USA, 77: 4030 (1980); Patents US 4,485,045 and US 4,544,545, and WO 97/38731 published October 23, 1997. Liposomes with a longer circulation time are described in US Patent 5,013,556. Particularly useful liposomes can be generated by the reverse phase evaporation method with a lipid composition comprising phosphatidylcholine, cholesterol and PEG derivatized phosphatidylethanolamine (PEG-PE). Liposomes are extruded through filters of defined pore size to produce liposomes of the desired diameter. The Fab fragments of the antibody of the present invention can be conjugated to liposomes as described in Martin et al. J. BioL. Chem. 257: 286-288 (1982) by a disulfide exchange reaction. A chemotherapeutic agent is optionally contained within the liposome. See Gabizon et al. J. National Cancer Inst. 81 (19) 1484 (1989).
When using recombinant techniques, the binding molecule can be produced intracellularly, in the periplasmic space, or directly secreted into the medium. If the binding molecule is produced intracellularly, as a first step, particle debris, either host cells or lysed fragments, are removed, for example, by centrifugation or ultrafiltration. Carter et al, Bio / Technology 10: 163-167 (1992) describe a procedure for isolating antibodies that are secreted into the periplasmic space of E. col !.
The binding molecule composition prepared from the cells can be purified using, for example, hydroxyapatite chromatography, gel electrophoresis,
<img file="MX349396B_D0030.tif" />
IMPI
INSTTTUTE MCUCANt · • I LA PRSFIIDAD tNHUSTWlAl dialysis, and affinity chromatography, with affinity chromatography being the preferred purification technique.
In a further aspect, the present invention relates to a nucleic acid sequence encoding a binding molecule of the invention. The term nucleic acid is well known to the person skilled in the art and comprises DNA (such as cDNA) and RNA (such as mRNA). The nucleic acid can be double-stranded and single-stranded, linear and circular. Said nucleic acid molecule is preferably comprised in a vector that is preferably comprised in a host cell. Said host cell is, for example, after transformation or transfection with the nucleic acid sequence of the invention, capable of expressing the binding molecule. For this, the nucleic acid molecule is operatively linked with control sequences.
A vector is a nucleic acid molecule used as a vehicle for transferring (foreign) genetic material within a cell. The term "vector" includes - but is not limited to - plasmids, viruses, cosmids, and artificial chromosomes. In general, designed vectors comprise an origin of replication, a multiple cloning site, and a selectable marker. The vector itself is generally a nucleotide sequence, commonly a DNA sequence, comprising an insert (transgene) and a larger sequence that serves as the backbone of the vector. Modern vectors may include additional features, in addition to the insertion transgene and backbone: promoter, genetic marker, antibiotic resistance, reporter gene, targeting sequence, protein purification tag. Vectors called expression vectors (expression constructs) are specific for the
<img file="MX349396B_D0031.tif" />
expression of the transgene in the target cell, and generally have control sequences such as a promoter sequence that directs the expression of the transgene. Insertion of a vector into the target cell is usually called transformation for bacterial cells, transfection for eukaryotic cells, although insertion of a viral vector is also called transduction.
As used herein, the term "host cell" refers to a cell into which a nucleic acid encoding the binding molecule of the invention was introduced by transformation, transfection, and the like. Such terms should be understood to refer not only to the particular cell being transformed but to the progeny or potential progeny of said cell. Because certain modifications can occur in successive generations due to mutation or environmental influences, such progeny may, in fact, not be identical to the parent cell, but are still included within the scope of the term as used herein.
As used herein, the term "expression" includes any step involved in the production of a binding molecule of the invention including, but not limited to, transcription, post-transcriptional modification, translation, post-translational modification, and secretion. .
The term "control sequences" refers to DNA sequences necessary for the expression of an operably linked coding sequence in a particular host organism. Control sequences that are suitable for prokaryotes, for example, include a promoter, optionally an operator sequence, and a
<img file="MX349396B_D0032.tif" />
IMPI
INSTITUTE MEllCAN.
OF THE MOHEDA! ' INDUSTRY!
binding to the ribosome. Eukaryotic cells are known to use promoters, polyadenylation signals, and enhancers.
A nucleic acid is "operably linked" when it is placed into a functional relationship with another nucleic acid sequence. For example, DNA for a presequence or secretory leader is operably linked to DNA for a polypeptide if it is expressed as a preprotein that participates in the secretion of the polypeptide; a promoter or enhancer is operably linked to a coding sequence if it affects the transcription of the sequence, or a ribosome binding site is operably linked to a coding sequence if it is positioned to facilitate translation. Generally, "operably linked" means that the DNA sequences that are linked are contiguous, and, in the case of a secretory leader, contiguous and in reading phase. However, enhancers do not have to be contiguous. Binding is achieved by ligation at convenient restriction sites. If such sites do not exist, synthetic oligonucleotide adapters or linkers are used in accordance with conventional practice.
The terms "host cell, target cell, or recipient cell" are intended to include any individual cell or cell culture that may be or has been a receptor for vectors or the incorporation of exogenous nucleic acid molecules, polynucleotides and / or proteins. They also include the progeny of a single cell and the progeny may not necessarily be completely identical (in morphology or in genomic or total DNA complement) to the original stem cell due to natural, accidental, or deliberate mutation. Cells can be prokaryotic or eukaryotic, and include, but are not
<img file="MX349396B_D0033.tif" />
IMPI
INSTITUTO MÜBCA NO
RE LA ΝΟΠΕΠΑΓ) INDUSTRIAL limited to bacterial cells, yeast cells, animal cells and mammalian cells, for example, murine, rat, macaque or human.
Suitable host cells include prokaryotic and eukaryotic host cells including yeast, fungi, insect cells, and mammalian cells.
The binding molecule of the invention can be produced in bacteria. After expression, the binding molecule of the invention, preferably the binding molecule is isolated from the E. coli cell paste in a soluble fraction and can be purified by, for example, affinity and / or exclusion chromatography. size. Final purification can be carried out in a similar way to the process for purifying the antibody expressed for example in CHO cells.
In addition to prokaryotes, eukaryotic microbes such as filamentous fungi or yeast are suitable cloning or expression hosts for the binding molecule of the invention. Saccharomyces cerevisiae, or common baker's yeast, is the most commonly used among the lower eukaryotic host microorganisms. However, a number of other genera, species and strains are commonly available and useful, such as Schizosaccharomyces pombe, Kluyveromyces hosts, such as, for example, K. lactis, K. fragilis (ATCC 12424), K. bulgaricus (ATCC 16.045), K. wickeramii (ATCC 24.178), K. waltii (ATCC 56.500), K. drosophilarum (ATCC 36.906), K. thermotolerans, and K. marxianus; yarrowia (EP 402 226); Pichia pastoría (EP 183 070); Candida; Trichhoderma reesia (EP 244 234); Neurospora crassa; Schwanniomyces such as Schwanniomyces occidentalis, and filamentous fungi such et u noeiui *, as, for example, Neurospora, Penicillium, Tolypocladium, and A§pefgmus hosts such as A. nidulans and A. niger.
Suitable host cells for expression of the glycosylated binding molecule of the invention, preferably antibody-derived binding molecules, are derived from multicellular organisms. Examples of invertebrate cells include plant and insect cells. Numerous baculovirus strains and variants and corresponding permissive insect host cells have been identified from hosts such as Spodoptera frugiperda (caterpillar), Aedes aegypti (mosquito), Aedes albopictus (mosquito), Drosophila melanogaster (fruit fly), and Bombyx I died. A variety of viral strains for transfection are publicly available, for example Autographa californica NPV variant L-1 and Bombyx morí NPV strain Bm-5, and such viruses can be used as viruses herein in accordance with the present invention. , particularly for the transfection of Spodoptera frugiperda cells.
Plant cell cultures of cotton, corn, potato, soybean, petunia, tomato, Arabidopsis, and tobacco can also be used as hosts. Cloning and expression vectors useful in the production of proteins in plant cell culture are known to those of skill in the art. See, for example, Hiatt et al., Nature (1989) 342: 76-78, Owen et al. (1992) Bío / Technology 10: 790-794, Artsaenko et al. (1995) The Plant J 8: 745-750, and Fecker et al. (1996) Plant Mol. Biol. 32: 979-986
However, interest has been greatest in vertebrate cells, and propagation in cultured vertebrate cells (tissue culture) has become a routine procedure. Examples of useful mammalian host cell lines are the CV1 line
Impi Gen Virol. 36:59 (1977)); baby hamster kidney cells (BHK, ATCC CCL 10); Chinese hamster ovary cells ADHFR (CHO, Urlaub et al., Proc. Nati. Acad. Sci. USA). 77: 4216 (1980)), mouse Sertoli cells (TM4, Mather, BioL Reprod. 23: 243-251 (1980)), monkey kidney cells (CVI ATCC CCL 70); African green monkey kidney cells (VERO-76, ATCC CRL1587); human cervical carcinoma cells (HELA, ATCC CCL 2), canine kidney cells (MDCK, ATCC CCL 34), buffalo rat liver cells (BRL 3A, ATCC CRL 1442), human lung cells (W138, ATCC CCL 75 ), human liver cells (Hep G2, 1413 8065); mouse mammary tumor (MMT 060562, ATCC CCL5 1); TRI cells (Mather et al., Annals N. And Acad Sci 383: 44-68 (1982)); MRC 5 cells; FS4 cells and a human hepatoma line (Hep G2)
When using recombinant techniques, the binding molecule of the invention can be produced intracellularly, in the periplasmic space, or secreted directly into the environment. If the binding molecule is produced intracellularly, as a first step, particle debris, either host cells or Used fragments, are removed, for example, by centrifugation or ultrafiltration. Carter et al, Bio / Technology 10: 163-167 (1992) describe a procedure for isolating antibodies that are secreted into the periplasmic space of E. coli. Briefly, the cell paste is thawed in the presence of sodium acetate (pH 3.5), EDTA, and phenylmethylsulfonyl fluoride (PMSF) for approximately 30 min. Cell debris can be removed by centrifugation. When the antibody is secreted into the medium, the supernatants of said expression systems are generally concentrated in
<img file="MX349396B_D0034.tif" />
IMPíí
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'NOUSTRial first using a commercially available protein concentration filter eg an Amicon or Millipore Pellicon ultrafiltration unit. A protease inhibitor such as PMSF can be included in any of the above steps to inhibit proteolysis and antibiotics can be included to prevent the growth of adventitious contaminants.
The binding molecule of the invention prepared from host cells can be purified using, for example, hydroxyapatite chromatography, gel electrophoresis, dialysis, and affinity chromatography, with affinity chromatography being the preferred purification technique.
The matrix to which the affinity ligand binds is often agarose, but other matrices are available. Mechanically stable matrices such as controlled pore glass or poly (styrenedivinyl) benzene allow faster flow rates and 15 shorter processing times than can be achieved with agarose. When the binding molecule of the invention comprises a CH3 domain, ABXMresin Bakerbond resin (JT Baker, Phillipsburg, NJ) is useful for purification. Other techniques for protein purification are also available such as fractionation on an ion exchange column, ethanol precipitation, reverse phase HPLC, silica chromatography, heparin chromatography, SEPHAROSE chromatography<sup>mr</sup> on an anion or cation exchange resin (such as a polyaspartic acid column), focus chromatography, SDS-PAGE, and ammonium sulfate precipitation, depending on the antibody to be recovered.
<img file="MX349396B_D0035.tif" />
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In another aspect, processes are provided for the production of binding molecules of the invention, said processes comprising culturing a host cell defined herein under conditions that allow expression of the binding molecule and recovering the produced binding molecule from culture.
The term "cultivar" refers to the in vitro maintenance, differentiation, growth, proliferation and / or propagation of cells under suitable conditions in a medium.
In an alternative embodiment, compositions are provided that comprise a binding molecule of the invention, or produced in accordance with the process of the invention. Preferably, said composition is a pharmaceutical composition.
As used herein, the term "pharmaceutical composition" refers to a composition for administration to a patient, preferably a human patient. The particular preferred pharmaceutical composition of this invention comprises the binding molecule of the invention. Preferably, the pharmaceutical composition comprises suitable formulations of carriers, st abilizers and / or excipients. In a preferred embodiment, the pharmaceutical composition comprises a composition for parenteral, transdermal, intraluminal, intraarterial, intrathecal and / or intranasal administration or by direct injection into tissue. It is contemplated that, in particular, said composition is administered to a patient by infusion or injection. Administration of suitable compositions can be effected in various ways, for example, by intravenous, intraperitoneal, subcutaneous, intramuscular, topical or intradermal administration. In particular, the present invention provides for uninterrupted administration of the suitable composition. As a non-limiting example,
<img file="MX349396B_D0036.tif" />
X f 1 iNsrrrtrro mixicanc Ϊ la moneDAi? For industrial purposes, uninterrupted, that is continuous, administration can be performed by a small pump system worn by the patient to measure the flow of the leiapeuhco-leJhiro agent from the patient's body. The pharmaceutical composition comprising the binding molecule of the invention can be administered using such pump systems. Such pump systems are generally known in the art, and commonly rely on the periodic exchange of cartridges containing the therapeutic agent to be infused. When exchanging the cartridge in a pump system, a temporary interruption of the flow of therapeutic agent, otherwise uninterrupted, in the patient's body can occur. In such a case, the administration phase before cartridge replacement and the administration phase following cartridge replacement are considered to, still within the meaning of the pharmaceutical means and methods of the invention, together constitute an uninterrupted administration of said therapeutic agent.
Continuous or uninterrupted administration of these binding molecules of the invention can be intravenous or subcutaneous by means of a fluid delivery device or small pump system that includes a fluid actuation mechanism for directing fluid out of a reservoir and a drive mechanism to drive the drive mechanism. Pumping systems for subcutaneous administration can include a needle or cannula to penetrate the skin of a patient and provide the appropriate composition in the body of the patient. Such pump systems can be attached or directly attached to the patient's skin independently of a vein, artery or blood vessel, allowing direct contact between the pump system and the patient's skin. The pump system can be attached to the patient's skin for 24 hours to several days. The pump system can be small in size with a LA PBOHEDAf mixing institute for small volumes. As a non-limiting example, the volume of the reservoir for the pharmaceutical composition suitable to be administered is between 0.1 and 50 ml.
Continuous administration can be transdermal by means of a patch worn on the skin and replaced at intervals. One of skill in the art is aware of suitable drug delivery patch systems for this purpose. It is to be noted that transdermal administration is especially suitable for uninterrupted administration, as the exchange of a first spent patch can advantageously be carried out simultaneously with the placement of a new, second patch, for example on the skin surface immediately adjacent to the first spent patch and immediately prior to removal of the first spent patch. They do not arise like this, problems of interruption of flow or failure of batteries.
The compositions of the invention may further comprise a pharmaceutically acceptable carrier. Examples of suitable pharmaceutical carriers are well known in the art and include solutions, for example, phosphate buffered saline solutions, water, emulsions, such as oil / water emulsions, various types of wetting agents, sterile solutions, liposomes, etc. Compositions comprising such carriers can be formulated by well known conventional methods. The formulations can comprise carbohydrates, buffers, amino acids and / or surfactants. The carbohydrates can be non-reducing sugars, preferably trehalose, sucrose, octasulfate, sorbitol, or xylitol. In general, as used herein, "pharmaceutically acceptable carrier" means any and all solvents, dispersion media, coatings, agents.
IMPI IΝΓΓΓΠ ÍTO ΜIXICA NON PE LA PROPERTY antibacterial and antifungal agents, isotonic and retardant agents SW<sup>TO</sup>abseferon, compatible with pharmaceutical administration. The use of tetee media and agents for pharmaceutically active substances is well known in the art. Acceptable carriers, excipients, or stabilizers are non-toxic to recipients at the dosages and concentrations employed, and include: additional buffering agents; preservatives; cosolvents; antioxidants; including ascorbic acid and methionine; chelating agents such as EDTA; metal complexes (eg protein-Zn complexes); biodegradable polymers, such as polyesters; salt-forming counter ions, such as sodium, sugar polyalcohols; amino acids, such as alanine, glycine, asparagine, 2-phenylalanine, and threonine; sugars or sugar alcohols, such as trehalose, sucrose, octasulfate, stachyose, sorbitol, or xylitol, manny, sorbose, xylose, ribose, myoinysitose, galactose, lactitol, ribitol, myoinisitol, galactitol, glycerol, cyclo-inositol (eg, polyethylene glycol) ; sulfur-containing reducing agents, such as glutathione, thioctic acid, sodium thioglycolate, thioglycerol, [alpha] -monothioglycerol, and sodium thiosulfate; low molecular weight proteins, such as human serum albumin, bovine serum albumin, gelatin or other immunoglobulins and hydrophilic polymers, such as polyvinylpyrrolidone. Such formulations can be used for continuous administrations which can be intravenous or subcutaneous with and / or without pump systems. The amino acids can be charged amino acids, preferably Usine, lysine acetate, arginine, glutamate and / or histidine. The surfactants can be detergents, preferably with a molecular weight> 1.2 KD and / or a polyether, preferably with a molecular weight> 3 KD. Non-limiting examples of preferred detergents are Tween 20, Tween 40, Tween 60, Tween 80 or Tween 85. Non-limiting examples of preferred polyethers are PEG 3000, PEG 3350, PEG 4000 or PEG 5000. Buffer systems
<img file="MX349396B_D0037.tif" />
used in the present invention may have an oH. preferred 5 to 9 times to comprise citrate, succinate, phosphate, histidine and acetate.
The compositions of the present invention can be administered to the subject in a suitable dose that can be determined for example, by dose escalation studies by administering increasing doses of the polypeptide of the invention exhibiting cross-species specificity described herein to primates. not chimpanzee, for example macaques. As discussed above, the binding molecule of the invention exhibiting cross-species specificity described herein can advantageously be used identically in preclinical tests in non-chimpanzee primates and as a drug in humans. These compositions can also be administered in combination with other proteinaceous and non-proteinaceous drugs. These drugs can be administered simultaneously with the composition comprising the polypeptide of the invention as defined herein or separately before or after the administration of said polypeptide at defined intervals and doses over time. The dosage regimen will be determined by the attending physician and clinical factors. As is well known in the medical arts, dosages for any patient depend on many factors, including the patient's size, body surface area, age, the particular compound to be administered, sex, time and route of administration, general health. , and other medications that are administered simultaneously.
Preparations for parenteral administration include sterile aqueous or non-aqueous solutions, suspensions, and emulsions. Examples of non-aqueous solvents are
<img file="MX349396B_D0038.tif" />
........,, propylene glycol, pohetylene glycol, vegetable oils such as aca ^ rQ ^ ol ^^^^^ injectable organic peres such as ethyl oleate. Aqueous-pellets include water, alcoholic / aqueous solutions, emulsions or suspensions, including saline and buffered media. Parenteral vehicles include sodium chloride solution, Ringer's dextrose, dextrose and sodium chloride, Ringer's lactate, or fixed oils. Intravenous vehicles include fluid and nutrient replenishers, electrolyte replenishers (such as those based on Ringer's dextrose), and the like. Preservatives and other additives may also be present such as, for example, antimicrobials, antioxidants, chelating agents, inert gases, and the like. Furthermore, the composition of the present invention may comprise proteinaceous carriers, such as, for example, serum albumin or immunoglobulin, preferably of human origin. It is contemplated that the composition of the invention may comprise, in addition to the polypeptide of the invention defined herein, additional biologically active agents, depending on the intended use of the composition. Such agents can be drugs that act on the gastrointestinal system, drugs that act as cytostatics, drugs that prevent hyperuricemia, drugs that inhibit immunoreactions (for example, corticosteroids), drugs that modulate the inflammatory response, drugs that act on the circulatory system and / or agents such as cytokines known in the art. It is also contemplated that the binding molecule of the present invention is applied in a co-therapy, that is, in combination with another anti-cancer drug.
The biological activity of the pharmaceutical composition defined herein can be determined for example by cytotoxicity tests, as described in the following examples, in WO 99/54440 or by Schlereth et al. (Cancer Immunol. Immunother. 20 (2005), 1-12). Efficacy or efficacy in vivo, as used in the
Ι.ΜΡΙ present, refers to the response to treatment by the pharmaceutical composition of the invention, using, for example, standardized NCI response criteria. In vivo success or efficacy of therapy using a pharmaceutical composition of the invention refers to the efficacy of the composition for its intended purpose, that is, the ability of the composition to cause the desired effect, that is, depletion of cells. pathological, for example tumor cells. In vivo efficacy can be monitored by standard methods established for the respective disease entities, including, but not limited to, white blood cell counts, differential, flow cytofluorometry (Fluorescence Activated Cell Sorting), bone marrow aspiration. In addition, various disease-specific clinical chemistry parameters and other established standard methods can be used. In addition, computer-assisted tomography, X-ray, nuclear magnetic resonance tomography (eg, for response assessment based on National Cancer Institute criteria [Cheson BD, Horning SJ, Coiffier B, Shipp MA, Rl Fisher , Connors JM, Lister TA, Vose J, Grillo-López A, Hagenbeek A, Cabanillas F, Klippensten D, Hiddemann W, Castellino R, Harris NL, Armitage JO, Cárter W, Hoppe R, Canellos GP. Report of an international workshop to standardize response criteria by non-Hodgkin lymphomas. NCI Sponsored International Working Group. J Clin Oncol 1999 Apr; 17 (4) 1244]), positron emission tomography, white blood cell count, differential, flow cytofluorometry (Fluorescence Activated Cell Sorting), bone marrow aspiration, lymph node biopsies / histologies, and various clinical chemistry parameters lymphoma-specific (eg, lactate dehydrogenase) and other established standard methods.
Another major challenge in drug development, such as the pharmaceutical composition of the invention is the predictable modulation of pharmacokinetic properties. To this end, a late drug profile can be established.
<img file="MX349396B_D0039.tif" />
candidate, that is, a profile of the pharmacokinetic parameters of a particular drug's ability to treat a given condition. Pharmacokinetic parameters of a drug that influence the ability of the drug to treat a certain disease include, but are not limited to: half-life or half-life, volume of distribution, first-pass hepatic metabolism, and the degree of binding to blood serum. The efficacy of a given drug can be influenced by each of the parameters mentioned above.
"Half-life" means the time that 50% of an administered drug is eliminated through biological processes, eg, metabolism, excretion, etc.
By "first-pass hepatic metabolism" is meant the propensity of a drug to be metabolized on first contact with the liver, that is, during its first pass through the liver.
"Volume of distribution" means the degree of retention of a drug through the various compartments of the body, such as intracellular and extracellular spaces, tissues and organs, and so on. and the distribution of the drug within these compartments.
"Degree of binding to blood serum" means the propensity of a drug to interact with and bind to blood serum proteins, such as albumin, leading to a reduction or loss of the biological activity of the drug.
<img file="MX349396B_D0040.tif" />
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I HEARD THE KCMEDAl? Pharmacokinetic parameters also include b¡od¡spon¡l¡dad,<sup>,</sup>'<sup>,</sup>tWiipo (Tlag), Tmax, absorption rates, plus onset and / or Cmax for a given amount of drug administered. "Bioavailability" means the amount of a drug in the blood compartment. Delay time means the time delay between the administration of the drug and its detection and measurability in blood or plasma.
"Tmax" is the time after which the maximum blood concentration of the drug is reached, and "Cmax" is the maximum blood concentration obtained with a given drug. The time to reach a concentration of the drug in blood or tissue that is required for its biological effect is influenced by all parameters. The pharmacokinetic parameters of bispecific single chain antibodies exhibiting cross-species specificity, which can be determined in preclinical animal tests in non-chimpanzee primates as described above, are also set forth, for example, in the publication by Schlereth et al. (Cancer Immunol. Immunother. 20 (2005), 112).
The term toxicity as used herein refers to the toxic effects of a drug manifested in adverse events or serious adverse events. These secondary events may refer to a lack of tolerance of the drug in general and / or a lack of local tolerance after administration. Toxicity could also include teratogenic or carcinogenic effects caused by the drug.
The terms "safety", "in vivo safety" or "tolerance" as used herein define the administration of a drug without inducing serious adverse effects directly after administration (local tolerance) and during a longer period of drug application. Safety, live safety or tolerance
IMPIAS
MEXICAN INSTITUTE
FROM THE PÍOMEDAl:
they can be evaluated, for example, at regular intervals during the follow-up period. Measures include the eüglrTdüún e.1 ínieo, for example, organic manifestations, and the detection of abnormalities in the laboratory. Clinical evaluation and deviations from normal results can be carried out and recorded / coded according to NCI-CTC and / or MedDRA standards. Organic manifestations can include criteria such as allergy / immunology, bone marrow / blood, cardiac arrhythmia, clotting, and the like, as set forth for example, in Common Terminology Scream for Adverse Events v3.0 (CTCAE). Laboratory parameters that can be tested include, for example, hematology, clinical chemistry, coagulation profile, and urinalysis and examination of other body fluids such as serum, plasma, lymphoid or cerebrospinal fluid, liquor, and the like. Safety can therefore be assessed, for example, by physical examination, imaging techniques (i.e. ultrasound, X-rays, computed tomography, magnetic resonance imaging (MRI), other measurements with technical devices (i.e. electrocardiogram) , vital signs, by measuring laboratory parameters and recording of adverse events. For example, adverse events in non-chimpanzee primates in the uses and methods according to the invention can be examined by histopathological and / or histochemical methods.
The term "effective dose" or "effective dosage" is defined as an amount sufficient to achieve or at least partially achieve the desired effect. The term "therapeutically effective dose" is defined as an amount sufficient to cure or at least partially arrest the disease and its complications in a patient already suffering from the disease. The effective amounts for this use will depend on the severity of the infection and the general state of the immune system itself.<sup>89</sup> Instituto mexícan »r> ^ gj» J5
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INDUSTRIAL • of the subject. The term "patient" includes human subjects and other mammals receiving either prophylactic or therapeutic treatment.
The term "effective and non-toxic dose" as used herein refers to a tolerable dose of a binding molecule of the invention that is high enough to cause depletion of pathological cells, tumor elimination, tumor shrinkage. or the stabilization of the disease with no or essentially no significant toxic effects. Such effective and non-toxic doses can be determined, for example, by dose scale studies described in the art and must be lower than the dose that induces serious adverse side effects (dose limiting toxicity, DLT).
The above expressions are also used, for example, in "Preclinical safety evaluation of biotechnology-derived pharmaceuticals S6; ICH Harmonized Tripartite Guideline ”; ICH Steering Committee meeting July 16, 1997.
The appropriate dosage, or therapeutically effective amount, of the binding molecule of the invention will depend on the condition to be treated, the severity of the condition, the prior therapy, and the patient's medical history and response to the therapeutic agent. The appropriate dose can be adjusted according to the judgment of the attending physician, such that it can be administered to the patient once or during a series of administrations. The pharmaceutical composition can be administered as a single therapeutic agent or in combination with additional therapies such as anticancer therapies, as necessary.
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The pharmaceutical compositions of this invention are particularly useful for parenteral administration, that is, by the subcutaneous, intramuscular, intramuscular, intra-articular and / or intra-synovial routes. Parenteral administration can be by bolus injection or continuous infusion.
If the pharmaceutical composition has been lyophilized, the lyophilized material is first reconstituted in a suitable liquid prior to administration. The lyophilized material can be reconstituted in, for example, bacteriostatic water for injection (BWFI), physiological saline, phosphate buffered saline (PBS), or the same formulation that the protein had been in prior to lyophilization.
Preferably, the binding molecule of the invention or produced by a process of the invention is used in the prevention, treatment or amelioration of a disease selected from a proliferative disease, a tumor disease, or an immune disorder.
An alternative embodiment of the invention provides a method for the prevention, treatment, or amelioration of a disease selected from a proliferative disease, a tumor disease, or an immune disorder comprising the step of administering to a patient in need thereof the molecule of union of the invention or produced by a process of the invention.
The formulations described herein are useful as pharmaceutical compositions in the treatment, amelioration, and / or prevention of pathological medical disease as described herein in a patient in need thereof. The term treatment refers to both therapeutic treatment and
<img file="MX349396B_D0041.tif" />
Treatment includes the application or administration of the fo
<img file="MX349396B_D0042.tif" />
isolated, or cells from a patient who has a disease / disorder, a symptom of a disease / disorder, or a predisposition towards a disease / disorder, for the purpose of curing, healing, alleviating, calming, altering, remedying, improving, overcoming , or affect the disease, disease symptom, or disease predisposition.
Those in need of treatment include those who already have the disorder, as well as those in whom the disorder is to be prevented. The term "disease" is any condition that would benefit from treatment with the protein formulation described herein. This includes chronic and acute disorders or diseases that include those pathological conditions that predispose the mammal to the disease in question. Non-limiting examples of diseases / disorders to be treated herein include proliferative disease, a tumor disease, or an immune disorder.
Preferably, the binding molecule of the invention is for use in the prevention, treatment, or amelioration of B cell disorders that correlate with (over) expression of BCMA, such as plasma cell disorders, and / or autoimmune diseases. The autoimmune disease is, for example, systemic lupus erythematosus or rheumatoid arthritis.
Also provided by the present invention is a method for treating or ameliorating B-cell disorders that correlate with (over) expression of BCMA, such as plasma cell disorders, and / or autoimmune diseases, comprising
IMPI
MSTnUTO MEXICANA DE LA «CPIEDAQ INDUSTRIAL the step of administering to a subject in need thereof the binding molecule of the invention. The autoimmune disease is, for example, systemic lupus erythematosus or rheumatoid arthritis.
In plasma cell disorders, a plasma cell clone multiplies uncontrollably. As a result, this clone produces large amounts of a single (monoclonal) antibody known as the M-protein. In some cases, as with monoclonal gammopathies, the antibody produced is incomplete, consisting of only light chains or heavy chains. These abnormal plasma cells and the antibodies they produce are usually limited to one type. Preferably, the plasma cell disorder is selected from the group consisting of multiple myeloma, plasmacytoma, plasma cell leukemia, macroglobulinemia, amyloidosis, Waldenstrom's macroglobulinemia, solitary bone plasmacytoma, extramedullary plasmacytoma, osteosclerotic myeloma, heavy chain diseases, monoclonal gamopathy of uncertain significance, and smoldering multiple myeloma.
In another aspect, kits are provided comprising a binding molecule of the invention, a nucleic acid molecule of the invention, a vector of the invention, or a host cell of the invention. The kit may comprise one or more vials containing the binding molecule and instructions for use. The kit may also contain means for the administration of the binding molecule of the present invention such as a syringe, pump, infuser or the like, means for reconstitution of the binding molecule of the invention and / or means for diluting the binding molecule. union of the invention.
<img file="MX349396B_D0043.tif" />
INSTITUTO MEXICANO ΓΈ IA PROFIERA! '
Additionally, the present invention relates to the use of the P''nS cluster<sup>TO</sup>tepi
BCMA, preferably human BCMA, for the generation of a binding molecule, preferably an antibody, which is capable of binding BCMA, preferably human BCMA. BCMA epitope cluster 3 preferably corresponds to amino acid residues 24 to 41 of the sequence as depicted in SEQ ID NO: 1002.
Furthermore, the present invention provides a method for the generation of an antibody, preferably a bispecific binding molecule, which is capable of binding to BCMA, preferably human BCMA, which comprises (a) immunizing an animal with a polypeptide comprising the cluster of epitopes 3 of
BCMA, preferably human BCMA, where BCMA epitope cluster 3 corresponds to amino acid residues 24 to 41 of the sequence as represented in SEQ ID NO: 1002, (b) obtain said antibody, and (c) optionally convert said antibody on a bispecific binding molecule that is capable of binding to human BCMA and preferably to the CD3 receptor complex of T cells.
Preferably, step (b) includes that the obtained antibody is tested as follows:
when the respective epitope cluster on the human BCMA protein is exchanged with the respective epitope cluster on a murine BCMA antigen (resulting in a construct comprising human BCMA, wherein the human 3 epitope cluster is replaced with the epitope cluster 3 3 murine; see SEQ ID NO: 1011), there will be a decrease in antibody binding. Said decrease is preferably at least<sup>94</sup> IMPI ^
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10%, 20%, 30%, 40%, 50%, more preferably at least 60%, 70%, 80%, 90%, 95% or even 100% compared to the respective epitope cluster in the BCMA protein human, wherein the binding to the respective epitope cluster in the human BCMA protein is set to 100%. The aforementioned human BCMA / murine BCMA chimeras are contemplated to be expressed in CHO cells. Human BCMA / murine BCMA chimeras are also contemplated to be fused to a transmembrane domain and / or to a cytoplasmic domain of a different membrane-bound protein, such as EpCAM; see Figure 2a.
A method to test this loss of binding due to exchange with the respective epitope cluster of a non-human (eg murine) BCMA antigen is described in the accompanying Examples, in particular in Examples 1-3.
The method may further include testing whether the antibody binds to the human BCMA epitope 3 cluster and is further capable of binding to the macaque BCMA epitope 3 cluster such as BCMA from Macaca mulatta (SEQ ID NO: 1017) or Macaca fascicularís (SEQ ID NO: 1017).
The present invention also provides binding molecules comprising any one of the amino acid sequences shown in SEQ ID NOs: 1-1000 and 1022-1093.
Preferably, a binding molecule comprises three VH CDR sequences (called VH CDR1, VH CDR2, VH CDR3, see 4<sup>ta</sup> column of the accompanying sequence table) of a binding molecule called BCMA- (X), where X is 1-100 (see 2<sup>gives</sup> column of the attached sequence table) and / or three VL CDR sequences (called VL <sup>95</sup>
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CDR1, VH CDR2, VH CDR3, see 4<sup>ta</sup> riflrr column hlti i.Ic. adjunct judgment) of a BCMA-X binding molecule term, where X is 1-100 (see 2<sup>gives</sup> column of the attached sequence table)
Preferably, a binding molecule comprises a VH and / or VL sequence as given in the attached sequence table (see 4<sup>ta</sup> column of the attached sequence table: VH and VL).
Preferably, a binding molecule comprises a scFv sequence as given in the accompanying sequence table (see 4<sup>ta</sup> sequence table column attached: scFv).
Preferably, a binding molecule comprises a bispecific molecule sequence as given in the accompanying sequence table (see 4<sup>ta</sup> column of the attached sequence table: bispecific molecule).
The present invention also relates to a bispecific binding agent comprising at least two binding domains, comprising a first binding domain and a second binding domain, wherein said first binding domain binds to the maturation BCMA antigen of B cells and where said second binding domain binds to CD3 (item 1), also including the following items:
Item 2. The bispecific binding agent of item 1, wherein said first binding domain binds to the extracellular domain of BCMA and said second binding domain binds to the ε chain of CD3
Item 3. A bispecific binding agent of item 1 or 2 that is in the form of a full-length antibody or an antibody fragment.
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Item 4. A bispecific binding agent of item 3 full length, wherein said first BCMA binding domain is derived from mouse and wherein said second CD3 binding domain is derived from rat.
Item 5. A bispecific binding agent of item 3, which is in the form of an antibody fragment in the form of a diabody comprising a heavy chain variable domain connected to a light chain variable domain on the same polypeptide chain so that the two domains do not pair.
Item 6. A bispecific binding agent of item 1 or 2 that is in the form of a bispecific single chain antibody consisting of two scFv molecules connected through a linker peptide or through a human serum albumin molecule.
Item 7. The bispecific binding agent of item 6, the heavy chain (VH) regions, and the corresponding light chain (VL) variable regions are arranged, from N-terminal to C-terminal, in the order
VH (BCMA) -VL (BCMA) -VH (CD3) -VL (CD3),
VH (CD3) -VL (CD3) -VH (BCMA) -VL (BCMA) or
VH CD3) -VL (CD3) -VL (BCMA) -VH (BCMA).
Item 8. A bispecific binding agent of item 1 or 2, which is in the form of a single domain immunoglobulin domain selected from VHHs or VHs.
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Item 9. The bispecific binding agent of item 1 or 2, gm ^ astá ρπ the form of an Fv molecule that has four antibody variable domains with at least two binding domains, wherein at least one binding domain is specific for Human BCMA and at least one binding domain is specific for human CD3
Item 10. A bispecific binding agent of item 1 or 2, which is in the form of a single-chain binding molecule consisting of a first BCMA-specific binding domain, a constant sub-region that is located C terminal to said first binding domain, a scorpion linker located C-terminal to the constant sub-region, and a second CD3-specific binding domain, which is located C-terminal to said constant sub-region.
Item 11. The bispecific binding agent of item 1 or 2, which is in the form of an antibody-like molecule that binds to BCMA through the two heavy chain / light chain Fvs of an antibody or an antibody fragment and that it binds to CD3 through a binding domain that has been modified in the non-CDR loops of the heavy chain or light chain of said antibody or antibody fragment.
Item 12. A bispecific binding agent of item 1 that is in the form of a bispecific ankyrin repeat molecule.
Item 13. A bispecific binding agent of item 1, wherein said first binding domain has a shape selected from the shapes defined in any of items 3 to 12 and wherein said second binding domain has a shape
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different selected from the shapes defined in
12.
Item 14. A bispecific binding agent of item 1 which is a bicyclic peptide.
Item 15. A pharmaceutical composition containing at least one bispecific binding agent from any of items 1 to 14.
Item 16. A bispecific binding agent of any of items 1 to 14 or a pharmaceutical composition of item 14 for the treatment of plasma cell disorders or other B cell disorders that correlate with the expression of BCMA and for the treatment of autoimmune diseases.
Item 17. A bispecific binding agent of any of items 1 to 14 or a pharmaceutical composition of item 15 for the treatment of selected plasma cell disorders of plasmacytoma, plasma cell leukemia, multiple myeloma, macroglobulinemia, amyloidosis, Waldenstrom's macroglobulinemia, bone plasmacytoma solitary, extramedullary plasmacytoma, osteosclerotic myeloma, heavy chain diseases, monoclonal gammopathy of uncertain significance, smoldering multiple myeloma.
Variations of the previous items are derivable from EP 10 191 418.2 which are also included herein.
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It should be understood that the inventions herein are not limited to particular methodology, protocols, or reagents, as these may vary. The discussion and examples provided herein are presented for the sole purpose of describing particular embodiments and are not intended to limit the scope of the present invention, which is defined solely by the claims.
All publications and patents cited either above or below throughout the text of this specification (including all patents, patent applications, scientific publications, manufacturer's specifications, instructions, etc.) are hereby incorporated by reference into its entirety. Nothing herein should be construed as an admission that the invention has no right to backdate such disclosure by virtue of prior invention. To the extent that the material incorporated by reference contradicts or is incompatible with this specification, the specification will take precedence over such material.
The figures show: Figure 1:
Sequence alignment of the extracellular domain (ECD) of human BCMA (amino acid residues 1-54 of the full-length protein) and murine BCMA (amino acid residues 1-49 of the full-length protein). The regions (domains or amino acid residues) that were swapped in the chimeric constructs, as designated for the epitope cluster, are highlighted. Cysteines are shown by black boxes. Disulfide bonds are indicated.
Figure 2a-b:
Epitope mapping of the BCMA constructs. Human and murine BCMA (Figure 2a) as well as seven human-murine chimeric BCMA constructs (Figure 2b)
100 <sup>w</sup> ^ "Industrial PMBDAC expressed on the surface of CHO cells as shown by flow cytometry. The expression of human BCMA on CHO cells was detected with an anti-human BCMA μσ monoclonal arylldUéi. The expression of murine BCMA was detected with a monoclonal anti-murine BCMA antibody. Bound monoclonal antibody was detected with a specific rat anti-IgG-Fc-gamma antibody conjugated to phycoerythrin.
Figure 3:
Examples of binding molecules specific for the E3 epitope cluster, as detected by epitope mapping of chimeric BCMA constructs (see example
3) .
Figure 4:
Determination of the binding constants of bispecific binding molecules (anti BCMA x anti CD3) on human and macaque BCMA using the Biacore system. The antigen was immobilized at a low to intermediate density (100 RU) on a CM5 chip. Binder dilutions were floated on the surface of the chip and the binding was determined using the BiaEval program. The respective dissociation constants and the binding constant (KD) of the respective binders are shown below each graph.
Figure 5:
Cytotoxic Activity of Bispecific BCMA Antibodies Measured in a Release Assay <sup>51</sup> 18 hour chrome. Effector cells: stimulated enriched human CD8 T cells. Target cells: CHO cells transfected with human BCMA
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Effector to target cell ratio (E: T): 10: 1.
Figure 6:
Determination of BCMA / CD3 bispecific antibody binding constants of the E3 epitope cluster on human and macaque BCMA and on human and macaque CD3, using the Biacore system. The antigen was immobilized at low to intermediate density (100-200 RU) on a CM5 chip. Bispecific antibody dilutions were floated on the chip surface and binding was determined using the BiaEval program. The respective association and dissociation constants and the resulting binding constant (KD) of the respective bispecific antibodies are shown below each graph.
Figure 7:
FACS analysis of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster on indicated cell lines: 1) CHO cells transfected with human BCMA, 2) human cell line HBP-ALL of CD3 positive T cells, 3) CHO cells transfected with BCMA macaque, 4) macaque T cell line 4119 LnPx, 5) BCMA-positive human multiple myeloma cell line NCIH929, and 6) non-transfected CHO cells. Negative Controls [1) to 6)]: Antibodies for detection without prior bispecific BCMA / CD3 antibody.
Figure 8:
Scatchard analysis of bispecific antibodies for BCMA / CD3 on cells expressing BCMA. Cells were incubated with increasing concentrations of
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flow cytometry. The triplicate measurement values were plotted as hyperbolic curves and sigmoid curves to demonstrate a valid range of concentration used. Maximum binding was determined using the evaluation of
Scatchard, and the respective KD values were calculated.
Figure 9:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster, measured in a <sup>51</sup> 18 hour chromium against CHO cells transfected with human BCMA. Effector cells: stimulated enriched human CD8 T cells. Effector cell to target ratio (E: T): 10: 1.
Figure 10:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster, measured in a 48 hour FACS-based cytotoxicity assay. Effector cells: unstimulated human PBMC. Target cells: CHO cells transfected with human BCMA. Effector cell to target ratio (E: T): 10: 1.
Figure 11:
FACS analysis of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster on CHO cells transfected with BAFF-R and TACI. Cell lines: 1) CHO cells transfected with human BAFF-R, 2) CHO cells transfected with human TACI 3) multiple myeloma cell line L363; negative controls: antibodies for detection without previous bispecific antibody to BCMA / CD3. Positive controls: BAFF-R detection: goat anti hu BAFF-R (R&D AF1162; 1:20) detected by antibody
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Anti-goat PE (Jackson 705-116-147; 1:50) TACI detection: antibody 8§'tíoneJb3Ete ^
TACI (abcam AB 79023; 1: 100) detected by «^ ¡ri iarpn ~ PP .......... i;
(Sigma P9757; 1:20).
Figure 12:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 measured in a release assay of <sup>51</sup>18 hour chrome. Effector cells: stimulated enriched human CD8 T cells. Target cells: BCMA-positive human multiple myeloma cell line L363 (ie, wild-type expressor). Effector cell to target ratio (E: T): 10: 1.
Figure 13:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 measured in a 48-hour FACS-based cytotoxicity assay. Effector cells: unstimulated human PBMC. Target cells: human multiple myeloma cell line L363 (natural expressor of BCMA). Effector cell to target ratio (E: T): 10: 1.
Figure 14:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 measured in a 48-hour FACS-based cytotoxicity assay. Effector cells: unstimulated human PBMC. Target cells: BCMApositive human multiple myeloma cell line NCI-H929. Effector cell to target ratio (E: T): 10: 1.
Figure 15:
Cytotoxic activity of bispecific antibodies to BCMA / CD3 measured in a 48-hour FACS-based cytotoxicity assay. Effector cells: 4119LnPx line of
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Effector cell to target ratio (E: T): 10: 1.
Figure 16:
Anti-tumor activity of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster in an advanced stage NCI-H929 xenograft model (see Example 16).
Figure 17:
FACS-based cytotoxicity assay using human multiple myeloma cell lines NCI-H929, L-363 and OPM-2 as target cells and human PBMC as elector cells (48h; E: T = 10: 1). The figure shows the levels of cytokine [pg / ml] that were determined for IL-2, IL-6, IL-10, TNF and IFN-gamma at increasing concentrations of the bispecific antibodies to BCMA / CD3 of the E3 epitope cluster ( see Example 22).
Examples:
The following examples illustrate the invention. These examples should not be construed as limiting the scope of this invention. The examples are included for the purposes of illustration, and the present invention is limited only by the claims.
Example 1 Generation of CHO Cells Expressing Chimeric BCMA
For construction of chimeric epitope mapping molecules, the amino acid sequence of the respective epitope domains or individual residues of
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• Human BCMA / murine E1 ECD (SEQ ID NO: 1009)
Extracellular domain of chimeric BCMA: extracellular domain of human BCMA where epitope cluster 1 (amino acid residues 1-7 of SEQ ID NO: 1002 or 1007) is replaced by the respective murine cluster (amino acid residues 1-4 of SEQ ID NO: 1004 or 1008)
- »deletion of amino acid residues 1-3 and G6Q mutation in SEQ ID NO: 1002 or 1007 • ECD of human BCMA / murine E2 (SEQ ID NO: 1010)
Chimeric BCMA extracellular domain: extracellular domain of human BCMA where the epitope cluster 2 (amino acid residues 8-21 of SEQ ID NO: 1002 or 1007) is replaced by the respective murine cluster (amino acid residues 5-18 of SEQ ID NO : 1004 or 1008) S9F, Q10H, and N11S mutations in SEQ ID NO: 1002 or 1007 • Human BCMA / murine E3 ECD (SEQ ID NO: 1011)
Chimeric BCMA extracellular domain: extracellular domain of human BCMA in which the epitope cluster 3 (amino acid residues 24-41 of SEQ ID NO: 1002 or 1007) is replaced by the respective murine cluster (amino acid residues 21-36 of SEQ ID NO : 1004 or 1008) deletion of amino acid residues 31 and 32 and mutation Q25H, S30N, L35A, and R39P in SEQ ID NO: 1002 or 1007
106 • Human BCMA / murine E4 ECD (SEQ ID NO: 1012 ^ -, -
Chimeric BCMA extracellular domain: extracellular domain of human BCMA in which the epitope cluster 4 (amino acid residues 42-54 of SEQ ID NO: 1002 or 1007) is replaced by the respective murine cluster (amino acid residues 37-49 of SEQ ID NO : 1004 or 1008) N42D, A43P, N47S, N53Y and A54T mutations in SEQ ID NO: 1002 or 1007 • Human BCMA / murine E5 ECD (SEQ ID NO: 1013)
Chimeric BCMA extracellular domain: extracellular domain of human BCMA where the amino acid residue at position 22 of SEQ ID NO: 1002 or 1007 (isoleucine) is replaced by its respective murine amino acid residue of SEQ ID NO: 1004 or 1008 (lysine, position 19)
-> I22K mutation in SEQ ID NO: 1002 or 1007. Human BCMA / murine E6 ECD (SEQ ID NO: 1014)
Chimeric BCMA extracellular domain: extracellular domain of human BCMA where the amino acid residue at position 25 of SEQ ID NO: 1002 or 1007 (glutamine) is replaced by its respective murine amino acid residue of SEQ ID NO: 1004 or 1008 (histidine, position 22) Q25H mutation in SEQ ID NO: 1002 or 1007 • Human BCMA / murine E7 ECD (SEQ ID NO: 1015)
Chimeric BCMA extracellular domain: extracellular domain of human BCMA where the amino acid residue at position 39 of SEQ ID NO: 1002 or 1007 (arginine) is
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A) The cDNA constructs were cloned into the mammalian expression vector pEF-DHFR and stably transfected into CHO cells. The expression of human BCMA in CHO cells was verified in a FACS assay using an anti-human BCMA monoclonal antibody. The expression of murine BCMA was demonstrated with an anti-mouse BCMA monoclonal antibody. The concentration of antibodies used
BCMA was 10 pg / ml in PBS / 2% FCS. Bound monoclonal antibodies were detected with an anti-rat IgG-Fcy-PE (1: 100 in PBS / 2% FCS; Jackson-lmmunoResearch # 112-116-071). As a negative control, cells were incubated with PBS / 2% FCS instead of the first antibody. The samples were measured by flow cytometry on a FACSCanto II instrument (Becton Dickinson) and were analyzed with the FlowJo program (Version 7.6). The surface expression of CHO cells transfected with the human-murine BCMA chimeras was analyzed and confirmed in a flow cytometric assay with different anti-BCMA antibodies (Figure 2a-b).
B) For the generation of CHO cells expressing human, macaque, mouse, and chimeric human / mouse BCMA, the coding sequences for human, macaque, mouse, and human-mouse BCMA chimeras (BCMA sequences as published in GenBank, accession numbers NM_001192 [human], NM_011608 [mouse] and XM_001106892 [macaque]) were obtained by gene synthesis according to standard protocols. The gene synthesis fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs and the
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followed in-frame by the coding sequence of the BCMA proteins respectively in the case of chimeras with the respective epitope domains of the human sequence exchanged for the murine sequence.
Except for the human BCMA / murine E4 and human BCMA ECD constructs, the coding sequence for the extracellular domain of the BCMA proteins was followed in-frame by the coding sequence for an artificial Ser1-Gly4-Ser1 linker followed by the extracellular domain of human EpCAM (amino acids 226-314; sequence as published in GenBank accession number NM_002354).
All coding sequences were followed by a stop codon. The gene synthesis fragments were designed to introduce suitable restriction sites. The gene synthesis fragments were cloned into a plasmid designated pEF-DHFR (pEF-DHFR is described in Raum et al. Cancer Immunol Immunother 50 (2001) 141150). All the aforementioned procedures were carried out according to standard protocols (Sambrook, Molecular Cloning; A Laboratory Manual, 3rd edition, Coid Spring Harbor Laboratory Press, Coid Spring Harbor, New York (2001)). For each antigen, a sequence-verified nucleotide clone was transfected into DHFR-deficient CHO cells for eukaryotic expression of the constructs. Eukaryotic protein expression in DHFR deficient CHO cells was carried out as described in Kaufman RJ (1990) Methods Enzymol. 185, 537566. Gene amplification of the constructs was induced by increasing concentrations of methotrexate (MTX) to a final concentration of up to 20 nM MTX.
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Example 2 2.1 Transient expression in HEK 293 cells
Clones of the expression plasmids with sequence verified nucleotide sequences were used for transfection and protein expression in the FreeStyle 293 Expression System (Invitrogen GmbH, Karlsruhe, Germany) according to the manufacturer's protocol. Supernatants containing the expressed proteins were obtained, the cells were removed by centrifugation and the supernatants were stored at -20 C.
2.2 Stable expression in CHO cells
Clones of the expression plasmids were transfected with sequence-verified nucleotide sequences into DHFR-deficient CHO cells for eukaryotic expression of the constructs. Eukaryotic protein expression in DHFR deficient CHO cells was carried out as described in Kaufman RJ (1990) Methods Enzymol. 185, 537-566. Gene amplification of the constructs was induced by increasing concentrations of methotrexate (M TX) to a final concentration of 20 nM MTX. After two passages of stationary culture, the cells were grown in spinner bottles with liquid soybean medium for CHO with nucleoside-free HyQ PF (with 4.0 mM LGlutamine with 0.1% Pluronic F-68; HyClone) for 7 days before harvesting. The cells were removed by centrifugation and the supernatant containing the expressed protein was stored at -20 C.
2.3 Protein purification
The purification of soluble BCMA proteins was carried out as follows: the Akta® Explorer system (GE Healthcare) and the Unicom® program for chromatography were used. I know<sup>110</sup> iNSTnvro mejucamf ___ de la ριορτιολγ
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Stage 1: 10% buffer B in 6 column volumes
Stage 2: 100% buffer B in 6 column volumes
The protein fractions eluted from step 2 were pooled for further purification. All chemical agents were research grade and purchased from Sigma (Deisenhofen) or Merck (Darmstadt).
Gel filtration chromatography was carried out on a HiLoad 16/60 Superdex 200 preparative grade column (GE / Amersham) equilibrated with Equi-buffer (10 mM citrate, 25 mM lysine-HCl, pH 7.2 for expressed proteins in HEK cells and PBS pH 7.4 for proteins expressed in CHO cells). Eluted protein samples (flow rate 1 ml / min) were subjected to SDS-PAGE and standard Western Blot for detection. Protein concentrations were determined using OD280 nm.
The proteins obtained via transient expression in HEK 293 cells were used for immunizations. Proteins obtained via stable expression in CHO cells were used for selection of binders and for binding measurement.
Example 3
Epitope cluster formation of murmos scFv fragments
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Cells transfected with human or murine BCMA or chimeric corTTITOlétula ^ BEíScMA were stained with crOTfFStTTTITtaii7-eoR ^^ periplasmic extract that binds human / macaque BCMA. Bound scFvs were detected with 1 pg / ml of an anti-FLAG antibody (Sigma F1804) and an R-PE-labeled anti-mouse gamma-specific Fe antibody (1: 100; Dianova # 115-116-071). All antibodies were diluted in PBS with 2% FCS. As a negative control, cells were incubated with PBS / 2% FCS instead of the periplasmic extract. The samples were measured by flow cytometry on a FACSCanto II instrument (Becton Dickinson) and were analyzed using the FlowJo program (Version 7.6); see Figure 3.
Example 4
Obtaining different recombinant forms of human BCMA and soluble macaque
A) The coding sequences for human and rhesus BCMA (as published in GenBank, accession numbers NM_001192 [human], XM_001106892 [rhesus]), coding sequences for human albumin, human Fcy1 and murine albumin were used for the construction of sequences. of artificial cDNAs that encode soluble fusion proteins of human BCMA and macaque respectively, and human albumin, human IgG1 Fe and murine albumin respectively, as well as soluble proteins that comprise only the extracellular domains of BCMA. To generate the constructs for expression of soluble macaque and human BCMA proteins, cDNA fragments were obtained by PCR mutagenesis of the full-length BCMA cDNAs described above and molecular cloning according to standard protocols.
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For human albumin fusions, the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs followed by the coding sequence of the human BCMA and rhesus (or Macaca mulatta) proteins respectively, which comprise amino acids 1 a 54 and 1 to 53 corresponding to the extracellular domain of human and rhesus BCMA, respectively, followed in frame by the coding sequence of an artificial linker Ser1-Gly4-Ser1, followed in frame by the coding sequence for human serum albumin, followed in frame by the coding sequence for a Flag tag, followed in frame by the coding sequence for a modified histidine tag (SGHHGGHHGGHH) and a stop codon.
For the IgGImurin fusions, the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs followed by the coding sequence of the human and macaque BCMA proteins respectively, comprising amino acids 1 to 54 and 1 to 53 corresponding to the extracellular domain of human BCMA and rhesus, respectively, followed in frame by the coding sequence of an artificial linker Ser1-Gly4-Ser1, followed in frame by the coding sequence for the hinge and Fe gamma portion of human IgG1, followed in frame by the coding sequence for a hexahistidine tag and a stop codon.
For the murine albumin fusions, the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs followed by the coding sequence for the human and macaque BCMA proteins respectively, comprising amino acids 1 to 54 and 1 to 53 corresponding to the extracellular domain of human BCMA and rhesus, respectively, followed in frame by the coding sequence of an artificial linker Ser1-Gly4-Ser1, followed in frame by the coding sequence for murine serum albumin, followed in
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For the soluble extracellular domain constructs, the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs followed by the coding sequence for the human and macaque BCMA proteins respectively, comprising amino acids 1 to 54 and 1 to 53 corresponding to the extracellular domain of human BCMA and rhesus, respectively, followed in frame by the coding sequence of an artificial linker Ser1-Gly1, followed in frame by the coding sequence for a Flag tag, followed in frame by the coding sequence for a modified histidine tag (SGHHGGHHGGHH) and a stop codon.
The cDNA fragments were also designed to introduce restriction sites at the beginning and end of the fragments. The introduced restriction sites, EcoRI at the 5 'end and Exit at the 3' end, were used in the following cloning procedures. The cDNA fragments were cloned via EcoRI and Sali into a plasmid designated pEF-DHFR (pEF-DHFR is described in Raum et al. Cancer Immunol Immunother 50 (2001) 141-150). The aforementioned procedures were all carried out according to standard protocols (Sambrook, Molecular Cloning; A Laboratory Manual, 3rd edition, Coid Spring Harbor Laboratory Press, Coid Spring Harbor, New York (2001)).
B) The coding sequences for human and macaque BCMA as described above and the coding sequences for human albumin, human Fcy1, murine Fcy1, murine Fcy2a, murine albumin, rat albumin, rat Fcy1 and rat Fcy2b were used to the construction of artificial cDNA sequences encoding soluble fusion proteins of human BCMA and macaque, respectively, and human albumin, human IgG1 Fe, murine IgG1 Fe, murine IgG2a Fe, murine albumin, Rat IgG1 Fe, rat IgG2b, and rat albumin, respectively, as well as soluble proteins comprising only the extracellular domains of BCMA. To generate constructs for expression of soluble human and macaque BCMA proteins, cDNA fragments were obtained by PCR mutagenesis of full-length BCMA cDNAs described above and molecular cloning according to standard protocols.
For the albumin fusions the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs and the coding sequence for a 19 amino acid immunoglobulin leader peptide, followed in frame by the coding sequence for the extracellular domain of the respective BCMA protein followed in frame by the coding sequence of an artificial linker Ser1-Gly4Ser1, followed in frame by the coding sequence for the respective serum albumin, followed in frame by the coding sequence for a Flag tag, followed in frame by the coding sequence for a modified histidine tag (SGHHGGHHGGHH) and a stop codon.
For the IgG Fes fusions the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs and the coding sequence for a 19 amino acid immunoglobulin leader peptide, followed in frame by the coding sequence for the extracellular domain of the respective BCMA protein followed in frame by the coding sequence of an artificial linker Ser1-Gly4Ser1, except for human Fe IgG1 where an artificial linker Ser1-Gly1 was used, followed in frame by the coding sequence of the hinge and the Fe gamma portion of the IgG
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respective, followed in frame by the coding sequence for a Flag tag, followed in frame by the coding sequence for a modified histidine tag (SGHHGGHHGGHH) and a stop codon.
For soluble extracellular domains constructs the modified cDNA fragments were designed to first contain a Kozak site for eukaryotic expression of the constructs and the coding sequence for a 19 amino acid immunoglobulin leader peptide, followed in frame by the coding sequence for the extracellular domain of the respective BCMA protein followed in frame by the coding sequence of an artificial linker Ser1-Gly1, followed in frame by the coding sequence for a Flag tag, followed in frame by the coding sequence for a modified histidine tag (SGHHGGHHGGHH) and a stop codon.
For the cloning of the constructs, suitable restriction sites were introduced. The cDNA fragments were all cloned into a plasmid designated pEF-DHFR (pEFDHFR is described in Raum et al. 2001). The aforementioned procedures were all carried out according to standard protocols (Sambrook, 2001).
The following constructs were designed to allow searching directed at different epitopes. The coding sequence of murine-human BCMA chimeras and murine-macaque BCMA chimeras (sequences of mouse, human and macaque BCMA as described above) and the coding sequences of murine albumin and murine Fcy1 were used for the construction of artificial sequences of CDNAs encoding soluble fusion proteins of murine-human and murine-macaque BCMA chimeras respectively and murine IgG1 Fe and murine albumin, respectively. To generate the constructs for the expression of the soluble murine-human and murinemacac BCMA chimeras, fragments of murine BCMA cDNA (amino acids 1-49) were obtained with the
<img file="MX349396B_D0054.tif" />
116 respective domains of epitopes mutated to respectively, by gene synthesis of
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the human and macaque sequence according to standard protocols. The cloning of constructs was carried out as described above and according to standard protocols (Sambrook, 2001).
The following molecules were constructed:
• human amino acids 1-4, lgG1 murine Fe • human amino acids 1-4, murine albumin • amino acids 1-4 rhesus, lgG1 murine Fe • amino acids 1-4 rhesus, murine albumin • amino acids 5-18 human, lgG1 murine Fe • amino acids Human 5-18, murine albumin • amino acids 5-18 rhesus, lgG1 murine Fe • amino acids 5-18 rhesus, murine albumin • amino acids 37-49 human, lgG1 murine Fe • amino acids 37-49 human, murine albumin • amino acids 37-49 rhesus, IgG 1 murine Fe • amino acids 37-49 rhesus, murine albumin
Example 5
5.1 Determination on the basis of Biacore of affinity of bispecific antibody for
BCMA and human and macaque CD3
Biacore assay experiments were carried out using recombinant BCMA fusion proteins with human serum albumin (ALB) to determine BCMA target binding. For CD3 affinity measurements, recombinant fusion proteins having the N-terminal 27 amino acids of CD3 epsilon (CD3e) fused to the
117 iNsrmrro mexicanc
OF THE PROPERTY vSe ^ SLSr. ,.<sub>±</sub>. . „R-. _ ... ___x JNDUmiAL FC portion of human antibody. This recombinant protein exists in a human version CD3e1-27 and in a crab macaque CÜ3e version, both of which contain the epitope of the CD3 binder on bispecific antibodies.
In detail, CM5 sensor chips (GE Healthcare) were immobilized with approximately 100 to 150 RU of the respective recombinant antigen using acetate buffer pH 4.5 according to the manufacturer's manual. Bispecific antibody samples were loaded in five concentrations: 50 nM, 25 nM, 12.5 nM, 6.25 nM and 3.13 nM diluted in HBS-EP running buffer (GE Healthcare). The flow rate was 30 to 35 μΙ / min for 3 min, then HBS-EP running buffer was applied for 8 min again at a flow rate of 30 to 35 μΙ / min. Chip regeneration was carried out using 10 mM glycine, 0.5 M NaCl pH 2.45. The data sets were analyzed using the BiaEval Program (see Figure 4). In general, two independent experiments were carried out.
5.2 Human and macaque BCMA binding affinity
Bispecific antibody binding affinities for BCMA / CD3 to human and macaque BCMA were determined by Biacore analysis using recombinant BCMA fusion proteins with mouse albumin (ALB).
In detail, CM5 sensor chips (GE Healthcare) were immobilized with approximately 150 to 200 RU of the respective recombinant antigen using acetate buffer pH 4.5 according to the manufacturer's manual. Bispecific antibody samples were loaded in five concentrations: 50 nM, 25 nM, 12.5 nM, 6.25 nM and 3.13 nM diluted in HBS-EP running buffer (GE Healthcare). For BCMA affinity determinations, the flow rate was 35 µΙ / min for 3 min, then HBS-EP running buffer was applied for 10, 30 or 60 min again at a flow rate of 35 µΙ / min. The
<img file="MX349396B_D0055.tif" />
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<img file="MX349396B_D0056.tif" />
iirrrrRrro muicaw <LA PtOPlEDAC INDU.THtlAl chip regeneration was carried out using a hi iffar-gi ir mnaistR of a 1: 1 mixture of 10 mM glycine, 0.5 M NaCl pH 1.5 and 6M guanidine chloride solution . The data sets were analyzed using the BiaEval Program (see Figure 6). In general, two independent experiments were carried out.
Confirmatory binding of human and macaque epsilon CD3 was carried out in individual experiments using the same concentrations applied to BCMA binding; the determination of the dissociation rate was carried out for a dissociation time of 10 min.
All bispecific antibodies to BCMA / CD3 from the E3 epitope cluster showed high affinities for human BCMA in the sub-nanomolar range to the 1-digit picomolar range. Binding to macaque BCMA was balanced, also showing affinities in the 1-digit nanomolar to sub-nanomolar range. The affinities and affinity differences of bispecific antibodies for BCMA / CD3 are shown in Table 2.
Table 2: Bispecific antibody affinities for BCMA / CD3 of the E3 epitope cluster to human and macaque BCMA, determined by Biacore analysis, and calculated affinity differences (ma BCMA: hu BCMA).
<td>bispecific antibody for BCMA / CD3</td><td>hu BCMA [nM]</td><td>ma BCMA [nM]</td><td>Affinity difference ma BCMA: hu BCMA</td>
<td>BCMA-83</td><td> 0,031</td><td> 0,077</td><td> 2,5</td>
<img file="MX349396B_D0057.tif" />
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<td>BCMA-98</td><td> 0,025</td><td> 0,087 ______</td><td></td>
<td>BCMA-71</td><td> 0,60</td><td> 2,2</td><td> 3,7</td>
<td>BCMA-34</td><td> 0,051</td><td> 0,047</td><td> 1 : 1,1</td>
<td>BCMA-74</td><td> 0,088</td><td> 0,12</td><td> 1,4</td>
<td>BCMA-20</td><td> 0,0085</td><td> 0,016</td><td> 1,9</td>
5.3 Biacore-based determination of bispecific antibody affinity for human and macaque BCMA
Bispecific antibody affinities for BCMA / CD3 for soluble recombinant BCMA on CM5 chips in Biacore measurements were repeated to reconfirm KDs and especially dissociation constants using longer dissociation periods (60 min instead of 10 min, as used in the previous experiment). All BCMA / CD3 bispecific antibodies tested were subjected to two<sup>15</sup> Independent affinity measurements with five different concentrations each.
The affinities of the bispecific antibodies for BCMA / CD3 of the E3 epitope cluster were clearly sub-nanomolar to 1 digit picomolar, see examples in Table 3.
Table 3: Affinity (KD) of Bispecific Antibodies to BCMA / CD3 of the E3 epitope cluster from Biacore experiments using extended dissociation times (two independent experiments each).
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<img file="MX349396B_D0058.tif" />
ίΝτππιτο
<td>bispecific antibody for BCMA / CD3</td><td>KD [nM] human BCMA</td><td>KD [nM] BCMA of macaque</td>
<td>BCMA-83</td><td> 0,053 ±0.017</td><td> 0,062 ±0.011</td>
<td>BCMA-98</td><td> 0,025 ± 0.003</td><td> 0,060 ±0.001</td>
<td>BCMA-71</td><td> 0,242 ± 0.007</td><td> 0,720 ± 0.028</td>
<td>BCMA-34</td><td> 0,089 ±0.019</td><td> 0,056 ± 0.003</td>
<td>BCMA-74</td><td> 0,076 ± 0.002</td><td> 0,134 ±0.010</td>
<td>BCMA-20</td><td> 0,0095 ± 0.0050</td><td> 0,0060 ± 0.0038</td>
Example 6 Bispecific binding and interspecies cross-reactivity
For confirmation of binding to human and macaque BCMA and CD3, bispecific antibodies were assayed by flow cytometry using CHO cells transfected with human and macaque BCMA, respectively, the human multiple myeloma cell line NCIH929 expressing native human BCMA, the CD3-expressing human T-cell leukemia cell line HPB-ALL (DSMZ, Braunschweíg, ACC483) and the CD3-expressing macaque T-cell cell line 4119LnPx (Knappe A, et al., Blood, 2000, 95, 3256-3261). In addition, non-transfected CHO cells were used as a negative control.
For flow cytometry, 200,000 cells of the respective cell lines were incubated for 30 min on ice with 50 μΙ of purified bispecific antibody at a
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IMPI concentration of 5 pg / ml. The cells were washed twice in PBS / 2% FCS and binding of the constructs was detected with a murine PentaHis antibody (Qiagen; diluted 1:20 in 50 µΙ of PBS / 2% FCS). After washing, the bound PentaHis antibodies were detected with a Fe gamma-specific antibody (Dianova) conjugated to phycoerythrin, diluted 1: 100 in PBS / 2% FCS. The samples were measured by flow cytometry on a FACSCanto II instrument and were analyzed using a FACSDiva program (both from Becton Dickinson).
Bispecific antibodies to BCMA / CD3 from the E3 epitope cluster stained CHO cells transfected with human and macaque BCMA, the human multiple myeloma cell line NCI-H929 expressing human BCMA as well as human and macaque T cells. Furthermore, there was no staining of non-transfected CHO cells (see Figure 7).
Example 7
Scatchard-based determination of bispecific antibody affinity to human and macaque BCMA
For Scatchard analysis, saturation binding experiments are performed using a monovalent detection system developed by Micromet (anti-His Fab / Alexa 488) to accurately determine the monovalent binding of bispecific antibodies to the respective cell line.
Incubate 2 x 10<sup>4</sup> cells of the respective cell line (CHO cell line expressing
Recombinant human BCMA, CHO cell line that expresses macaque BCMA recombinantly) with every 50 μΙ of a triplet dilution series (eight 1: 2 dilutions) of the respective bispecific BCMA antibody starting at 100 <sup>122</sup> WICKED
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OF THE EROHEDAr AwJSSLjgW industrial nM followed by 16 h incubation at 4 ° C under shaking and. a residual wash atana The cells are then incubated for an additional 30 min with 30 µΙ of an anti-His Fab / Alexa488 solution (Micromet; 30 pg / ml). After a washing step, the cells are resuspended in 150 μΙ of FACS buffer containing 3.5% formaldehyde, incubated for an additional 15 min, centrifuged, resuspended in FACS buffer and analyzed using a Cantoll FACS machine and a FACS Diva program. . The data are generated from two sets of independent experiments. The values are plotted as hyperbolic junction curves. The respective Scatchard analysis is calculated to extrapolate the maximum binding (Bmax). The bispecific antibody concentrations at the mean maximum binding are determined by reflecting the respective KDs. Triplicate measurement values are plotted as hyperbolic curves. Maximum binding is determined using the Scatchard evaluation and the respective KDs are calculated.
The affinities of bispecific BCMA / CD3 antibodies to CHO cells transfected with human or macaque BCMA were determined by Scatchard analysis as the most reliable method to measure potential affinity differences between human and macaque BCMA.
Cells expressing the BCMA antigen were incubated with increasing concentrations of the respective monomeric BCMA / CD3 bispecific antibodies until saturation was reached (16 h). Bound bispecific antibodies were detected by flow cytometry. The concentrations of the bispecific antibodies to BCMA / CD3 at mean maximum binding were determined by reflecting the respective KDs.
<img file="MX349396B_D0059.tif" />
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The triplicate measurement values were plotted as hyperbolic curves and as S-shaped curves to demonstrate the appropriate concentration ranges from minimal to optimal binding. Maximum binding (Bmax) was determined (Figure 8) using Scatchard evaluation and the respective KDs were calculated. The values shown in Table 4 were derived from two independent experiments per bispecific antibody to BCMA / CD3.
Cellular analysis based on Scatchard confirmed that the bispecific antibodies to BCMA / CD3 of the E3 epitope cluster are sub-nanomolar in affinity to human BCMA and have a small inter-species BCMA affinity difference of less than five.
Table 4: Affinity (KD) of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster from Scatchard cell analysis (two independent experiments each) with the calculated macaque BCMA KD / human BCMA KD affinity difference calculated.
<td>bispecific antibody for BCMA / CD3</td><td>KD [nM] Human BCMA</td><td>KD [nM] Macaque BCMA</td><td>difference of order "x" in KD KD BCMA ma vs. KD BCMA hu</td>
<td>BCMA-83</td><td> 0,40 ±0,13</td><td> 1,22 ±0,25</td><td> 3,1</td>
<td>BCMA-98</td><td> 0,74 ± 0,02</td><td> 1,15 ±0,64</td><td> 1,6</td>
<td>BCMA-71</td><td> 0,78 ± 0,07</td><td> 3,12 ±0,26</td><td> 4,0</td>
<td>BCMA-34</td><td> 0,77 ±0,11</td><td> 0,97 ± 0,33</td><td> 1,3</td>
<img file="MX349396B_D0060.tif" />
<td>BCMA-74</td><td> 0,67 ± 0,03</td><td> 0,95 ± 0,06</td><td> 1,4 _____</td>
<td>BCMA-20</td><td> 0,78 ±0,10</td><td> 0,85 ±0,01</td><td> 1,1</td>
Example 8 Cytotoxic activity
8.1 Chromium release assay with stimulated human T cells
Stimulated T cells enriched in CD8 T cells<sup>+</sup> were obtained as described below.
A Petri dish (145 mm diameter, Greiner bio-one GmbH, Kremsmünster) was coated with a commercially available anti-CD3 specific antibody (OKT3, Orthoclone) at a final concentration of 1 pg / ml for 1 hour at 37 ° C. . Unbound protein was removed by a PBS wash step. 3-5 x 10 added<sup>7 </sup>Human PBMC to Petri dish pre-coated in 120 ml of RPMI1640 with stabilized glutamine / 10% FCS / 20 U / ml IL-2 (Proleukin®, Chiron) and were stimulated for days. On the third day, cells were harvested and washed once with RPM11640. IL-2 was added to a final concentration of 20 U / ml and the cells were cultured again for one day in the same culture medium as before.
CD8 cytotoxic T lymphocytes enriched<sup>+</sup> (CTLs) by depletion of CD4 T cells<sup>+</sup> and NK CD56 cells<sup>+</sup> using Dynal-Beads according to the manufacturer's protocol.
Target CHO cells transfected with macaque or human BCMA were washed twice with PBS and labeled with <sup>51</sup>Cr of 11.1 MBq in a final volume of 100 μl of RPMI with -
FCS 50% for 60 minutes at 37 ° C. Subsequently, the labeled target cells were washed 3 times with 5 ml of RPMI and then used in the assay of
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<img file="MX349396B_D0061.tif" />
cytotoxicity. The assay was carried out in a 96-well plate in a total volume of 200 µI of RPMI supplemented with an E: T ratio of 10: 1. An initial concentration of 0.01 -1 pg / ml of purified bispecific antibody and dilutions to one third of it were used. The incubation time for the assay was 18 hours. Cytotoxicity was determined as relative values of chromium released in the supernatant in relation to the difference of maximum lysis (Triton-X addition) and spontaneous lysis (without effector cells). All measurements were carried out in quadruplicate. Chromium activity measurement in the supernatants was carried out in a gamma Wizard 3 "counter (Perkin Elmer Life Sciences GmbH, Koln, Germany). The analysis of the results was carried out with Prism 5 for Windows (version 5.0, GraphPad Software Inc., San Diego, California, USA). EC values<sub>50</sub> Calculated by the analysis program from the sigmoid dose response curves were used for comparison of cytotoxic activity (see Figure 5).
8.2 Retargeting potency of stimulated human effector T cells against CHO cells transfected with human BCMA
The cytotoxic activity of bispecific antibodies to BCMA / CD3 was analyzed in a chromium 51 release cytotoxicity assay (<sup>51</sup>Cr) using CHO cells transfected with human BCMA as target cells, and stimulated enriched human CD8 T cells as effector cells. The experiment was carried out as described in Example 8.1.
All bispecific antibodies to BCMA / CD3 of the E3 epitope cluster showed very potent cytotoxic activity against CHO cells transfected with human BCMA, with EC values<sub>50</sub> in the range of 1 digit of pg / ml or even lower (Figure
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and Table 5). Thus, the E3 epitope cluster exhibits a very favorable epitope activity ratio supporting a very potent bispecific antibody-mediated cytotoxic activity.
Table 5: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster analyzed in a chromium 51 release cytotoxicity assay (<sup>51</sup>Cr) using CHO cells transfected with human BCMA as target cells, and stimulated enriched human CD8 T cells as effector cells.
<td>bispecific antibody for BCMA / CD3</td><td>ECm [pg / ml]</td><td>R-squared value</td>
<td>BCMA-83</td><td> 0,38</td><td> 0,79</td>
<td>BCMA-98</td><td> 0,27</td><td> 0,85</td>
<td>BCMA-71</td><td> 3,2</td><td> 0,85</td>
<td>BCMA-34</td><td> 3,4</td><td> 0,81</td>
<td>BCMA-74</td><td> 0,73</td><td> 0,80</td>
<td>BCMA-20</td><td> 0,83</td><td> 0,82</td>
8.3 FACS-based cytotoxicity assay with unstimulated human PBMC Isolation of effector cells
Human Peripheral Blood Mononuclear Cells (PBMC) were prepared by Ficoll density gradient centrifugation from enriched lymphocyte (buffy coat) preparations, a by-product of blood banks that
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<img file="MX349396B_D0063.tif" />
They collect blood for transfusions. Buffy coats were provided by a local blood bank and PBMC were prepared on the same day as blood collection. After density centrifugation with Ficoll and extensive washes with Dulbecco PBS (Gibco), the remaining erythrocytes were removed from the PBMC via incubation with erythrocyte lysis buffer (NH<sub>4</sub>155 mM IC, KHCO<sub>3</sub>10 mM,
EDTA 100 μΜ). Platelets were removed via the supernatant with PBMC centrifugation at 100 x g. The remaining lymphocytes comprised mainly B and T lymphocytes, NK cells and monocytes. The PBMC were kept in culture at 37 ° C / 5% CO<sub>2</sub> in RPMI medium (Gibco) with 10% FCS (Gibco).
CD14 cell depletion<sup>+</sup>and CD56 *
For depletion of CD14 cells<sup>+</sup>, Human CD14 MicroBeads (Milteny Biotec, MACS, # 130-050-201) were used for depletion of human CD56 MicroBeads NK cells (MACS, # 130-050-401). The PBMC were counted and centrifuged for 10 min at room temperature with 300 x g. The supernatant was discarded and the cell pellet was resuspended in MACS isolation buffer [80 μΙ / 10<sup>7</sup> cells; PBS (Invitrogen, # 20012-043), 0.5% (v / v) FBS (Gibco, # 10270-106), 2 mM EDTA (SigmaAldrich, # E-6511)]. MicroBeads CD14 and MicroBeads CD56 (20 μΙ / 10<sup>7 </sup>cells) and incubated for 15 min at 4-8 ° C. Cells were washed with MACS isolation buffer (1-2 ml / 10<sup>7</sup> cells). After centrifugation (see above), the supernatant was discarded and the cells were resuspended in MACS isolation buffer (500 μΙ / 10<sup>8</sup> cells). CD14 / CD56 negative cells were then isolated using LS Columns (Miltenyi Biotec, # 130-042-401). PBMC without CD14 + / CD56 + cells were cultured in complete RPM medium, that is RPMI1640 (Biochrom AG, # FG1215) supplemented with 10% FBS (Biochrom AG, # S0115), 1x of non-essential amino acids (Biochrom AG, # K0293), 10 mM Hepes buffer (Biochrom AG, # L1613),
<img file="MX349396B_D0064.tif" />
1 mM sodium pyruvate (Biochrom AG, # L0473) and 100 U / ml penicillin / streptomycin (Biochrom AG, # A2213) at 37 ° C in an incubator until needed.
Target cell marking
For the analysis of cell lysis in flow cytometry assays, the fluorescent membrane dye D¡OC was used.<sub>18</sub> (DiO) (Molecular Probes, # V22886) to label CHO cells transfected with human BCMA or macaque BCMA, as target cells, and to distinguish them from effector cells. Briefly, cells were harvested, washed once with PBS, and adjusted to 10<sup>6</sup> cells / ml in PBS containing 2% (v / v) of FBS and the membrane stain DiO (5 μΙ / 10<sup>6</sup> cells). After incubation for 3 min at 37 ° C, the cells were washed twice in complete RPMI medium and the number of cells was adjusted to 1.25 x 10<sup>5</sup> cells / ml. Cell vitality was determined using 0.5% (v / v) isotonic EosinG solution (Roth, # 45380).
Analysis based on flow cytometry
This assay was designed to quantify the lysis of CHO cells transfected with macaque or human BCMA in the presence of serial dilutions of bispecific BCMA antibodies.
Equal volumes of DiO-labeled target cells and effector cells (i.e. PBMC without CD14 cells<sup>+</sup>), resulting in an E: T cell ratio of 10: 1. 160 µΙ of this suspension was transferred to each well of a 96-well plate. 40 µΙ of serial dilutions of the BCMA bispecific antibodies and a negative bispecific control (a CD3-based bispecific antibody that recognizes an irrelevant target antigen) or complete RPMI medium were added as an additional negative control. The bispecific antibody-mediated cytotoxic reaction proceeded for 48 hours in a humidified incubator with 7% CO<sub>2</sub>. The cells were then transferred to a new 96-well plate and the loss of target cell membrane integrity was
INSTITUTO MSX1CAHO DE LA KCMSDAÍ 'industrial monitored by adding propidium iodide (Pl) at a final concentration of 1 pg / ml. Pl is an impermeable membrane dye that is normally excluded from viable cells, while dead cells take it up and become identifiable by fluorescent emission.
Samples were measured by flow cytometry on a FACSCanto II instrument and analyzed with a FACSDiva program (both from Becton Dickinson).
Target cells were identified as DiO positive cells. Negative target cells were classified as live target cells. The percentage of cytotoxicity was calculated according to the following formula:
Cytotoxicity [%] = <sub>x</sub> 1<sub>00</sub> n target cells n = number of events
The percent cytotoxicity is plotted against the corresponding bispecific antibody concentrations using the GraphPad Prism 5 program (Graph Pad Software, San Diego). Dose response curves were analyzed with the four parametric logistic regression models for evaluation of sigmoid dose response curves with adjusted Hill slope and the EC values were calculated.<sub>S0</sub>.
8.4 Unstimulated human PBMC against target cells transfected with human BCMA
The cytotoxic activity of bispecific antibodies to BCMA / CD3 was analyzed in a FACS-based cytotoxicity assay using BCMA-transfected CHO cells.
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INSTITUTO MEXICAN, DE LA MOHEDAL INDUSTRIAL human as target cells, and unstimulated human PBMC as elector cells. The test was carried out as described above (Example 8.3).
The results of the cytotoxicity assay based on FACSs with unstimulated human PBMC as effector cells and CHO cells transfected with human BCMA as target cells are shown in Figure 10 and Table 6.
Table 6: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster measured in a 48 hour FACS-based cytotoxicity assay with unstimulated human PBMC as effector cells and CHO cells transfected with human BCMA as target cells.
<td>bispecific antibody for BCMA / CD3</td><td>EC<sub>50</sub> [pg / ml]</td><td>R-squared value</td>
<td>BCMA-83</td><td> 212</td><td> 0,97</td>
<td>BCMA-7</td><td> 102</td><td> 0,97</td>
<td>BCMA-5</td><td> 58,4</td><td> 0,94</td>
<td>BCMA-98</td><td> 53,4</td><td> 0,95</td>
<td>BCMA-71</td><td> 208</td><td> 0,94</td>
<td>BCMA-34</td><td> 149</td><td> 0,94</td>
<td>BCMA-74</td><td> 125</td><td> 0,97</td>
<td>BCMA-20</td><td> 176</td><td> 0.98</td>
Example 9
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9.1 Exclusion of cross-reactivity with INTOITUAL BAFF receptor
For flow cytometry, 200,000 cells from the active cell lines were incubated for 30 min on ice with 50 µΙ of purified bispecific molecules at a concentration of 5 pg / ml. The cells were washed twice in PBS with 2% FCS and the binding of the constructs was detected with a murine PentaHis antibody (Qiagen; diluted 1:20 in 50 µΙ of PBS with 2% FCS). After washing, bound PentaHis antibodies were detected with a Fe gamma-specific antibody (Díanova) conjugated to phycoerythrin, diluted 1: 100 in PBS with 2% FCS. Samples were measured by flow cytometry on a FACSCanto II instrument and analyzed using the FACSDiva program (both from Becton Dickinson). The bispecific binders were not shown to have cross-reactivity with the BAFF receptor.
9.2 Exclusion of cross-reactivity of bispecific antibody for BCMA / CD3 with human BAFF receptor (BAFF-R) and TACI
For exclusion of binding to human BAFF-R and TACI, bispecific antibodies to BCMA / CD3 were assayed by flow cytometry using CHO cells transfected with human BAFF-R and TACI, respectively. In addition, multiple myeloma L363 cells were used as a positive control for binding to human BCMA. The expression of BAFF-R and TACI antigens on CHO cells was confirmed by two positive control antibodies. Flow cytometry was carried out as described in the previous example.
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Flow cytomethane analysis confirmed that none of the bispfeefrtcüs antibodies to BCMA / CD3 in the E3 epitope cluster have human cross-reactivity to ~ cCTfTΒΑΓΓR ~ or human TACI (see Figure 11).
Example 10 Cytotoxic Activity
Human-type BCMA bispecific antibodies are tested for potency in targeting effector T cells against BCMA-expressing target cells in five additional in vitro cytotoxicity assays:
1. The potency of BCMA bispecific antibodies to redirect stimulated human effector T cells against a BCMApositive (human) tumor cell line was measured in a chromium-51 release assay.
2. The potency of bispecific BCMA antibodies to redirect T cells in unstimulated human PBMC against CHO cells transfected with human BCMA was measured in a FACS-based cytotoxicity assay.
3. The potency of BCMA bispecific antibodies to redirect T cells in unstimulated human PBMC against a BCMA-positive (human) tumor cell line was measured in a FACS-based cytotoxicity assay.
Four. To confirm whether the bispecific antibodies to cross-reactive BCMA are capable of redirecting macaque T cells against CHO cells transfected with macaque BCMA, a FACS-based cytotoxicity assay is performed with a macaque T cell line as effector T cells.
5. The difference in potency between the monomeric and dimeric forms of bispecific antibodies to BCMA is determined in a chromium-51 release assay.
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INSTITUTO MEXICANO Oí LA HlOMEDAti INDUSTRIAL using CHO cells transfected with human BCMA ran target cells and stimulated human T cells as effector cells.
Example 11
Human T cells stimulated against the BCMA-positive human multiple myeloma cell line L363
The cytotoxic activity of bispecific antibodies to BCMA / CD3 was analyzed in a chromium-51 release assay (<sup>51</sup>Cr) using the BCMA-positive human multiple myeloma cell line L363 (DSMZ No. ACC49) as a source of target cells, and stimulated enriched human CD8 T cells as effector cells. The test was carried out as described in Example 8.1.
Based on the results of chromium-51 release assays with stimulated enriched human CD8 T cells as effector cells and CHO cells transfected with human BCMA as targets, bispecific antibodies to BCMA / CD3 from the E3 epitope cluster are very potent in cytotoxic activity (Figure 12 and Table 7).
Another group of antibodies was identified during epitope clustering (see Examples 1 and 3), which is capable of binding to BCMA epitope clusters 1 and 4 ("E1 / E4"). Unexpectedly, bispecific antibodies to BCMA / CD3 of the E1 / E4 epitope cluster - despite being potent in cytotoxic activity against CHO cells transfected with human BCMA - were shown to be rather weakly cytotoxic against the human multiple myeloma cell line L363 expressing Low native BCMA
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<img file="MX349396B_D0067.tif" />
IMPI «τπντρ MEXICAN <sup>P!</sup> LA MOHEDA D 'ndustuial density on the cell surface (Figure 12 and Table 7). Without wishing to be bound by theory, the inventors understand that the BCMA humai'iü BCMA E1 / E4 epitope may be less accessible on natural BCMA expressors than on BCMA-transfected cells.
Table 7: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 from epitope clusters E1 / E4 (rows 1 and 2) and E3 (rows 3 to 8) analyzed in a chromium-51 release cytotoxicity assay (<sup>51</sup>Cr) of 18 hours with the BCMA-positive human multiple myeloma cell line L363 as the source of target cells, and stimulated enriched human CD8 T cells as effector cells.
<td></td><td>bispecific antibody to BCMA / CD3</td><td>EC<sub>50</sub> [pg / ml]</td><td>R-squared value</td>
<td> 1</td><td>BCMA-54</td><td> 685</td><td> 0,84</td>
<td> 2</td><td>BCMA-53</td><td> 1107</td><td> 0,82</td>
<td> 3</td><td>BCMA-83</td><td> 28</td><td> 0,83</td>
<td> 4</td><td>BCMA-98</td><td> 10</td><td> 0,81</td>
<td> 5</td><td>BCMA-71</td><td> 125</td><td> 0,86</td>
<td> 6</td><td>BCMA-34</td><td> 42</td><td> 0,81</td>
<td> 7</td><td>BCMA-74</td><td> 73</td><td> 0,79</td>
<td> 8</td><td>BCMA-20</td><td> 21</td><td> 0,85</td>
Example 12
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Unstimulated human PBMC against myelo cell line L363
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BCMA-positive human
The cytotoxic activity of bispecific antibodies to BCMA / CD3 was further analyzed in a FACS-based cytotoxicity assay using the BCMA-positive human multiple myeloma cell line L363 (DSMZ, ACC49) - showing the weakest surface expression of native BCMA from all T cell lines tested - as source of target cells and unstimulated human PBMC as effector cells. The test was carried out as described above (Example 8.3).
As seen in the chromium-51 release assay with enriched human CD8 T lymphocytes stimulated against the human multiple myeloma cell line L363, bispecific antibodies to BCMA / CD3 from the E1 / E4 epitope cluster - in contrast to their potent cytotoxic activity against CHO cells transfected with human BCMA - were again shown to be less potent in redirecting the cytotoxic activity of unstimulated PBMC against the L363 cell line of human multiple myeloma expressing native BCMA at low density on the cell surface. This is in line with the theory provided hereinabove, that is, that the human BCMA E1 / E4 epitope may be less accessible on natural expressers of BCMA than on cells transfected with BCMA. Bispecific antibodies to BCMA / CD3 of the E3 epitope cluster presented EC values<sub>50</sub> 3-digit pg / ml in this assay (see Figure 13 and Table 8).
Table 8: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 of epitope clusters E1 / E4 (rows 1 and 2) and E3 (rows 3 to 8) measured in an assay of
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<td></td><td>bispecific antibody for BCMA / CD3</td><td>EC<sub>50</sub>[pg / ml]</td><td>R-squared value</td>
<td> 1</td><td>BCMA-54</td><td> 3162</td><td> 0,99</td>
<td> 2</td><td>BCMA-53</td><td> 2284</td><td> 0,98</td>
<td> 3</td><td>BCMA-83</td><td> 241</td><td> 0,99</td>
<td> 4</td><td>BCMA-98</td><td> 311</td><td> 0,99</td>
<td> 5</td><td>BCMA-71</td><td> 284</td><td> 0,99</td>
<td> 6</td><td>BCMA-34</td><td> 194</td><td> 0,99</td>
<td> 7</td><td>BCMA-74</td><td> 185</td><td> 0,99</td>
<td> 8</td><td>BCMA-20</td><td> 191</td><td> 0,99</td>
As expected, the EC values<sub>50</sub> they were higher in cytotoxicity assays with unstimulated PBMC as effector cells than in cytotoxicity assays using enriched stimulated human CD8 T cells.
Example 13
0 Unstimulated human PBMC against the BCMA-positive human multiple myeloma cell line NCI-H929
The cytotoxic activity of bispecific antibodies to BCMA / CD3 was analyzed in a FACS-based cytotoxicity assay using the cell line NCI-H929 (ATCC CRL137
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9068) of BCMA-positive human multiple myeloma as the source of target cells and unstimulated human PBMC as effector cells. The test was carried out as described above (Example 8.3).
The results of this assay with another human multiple myeloma cell line (NCIH929) expressing native BCMA on the cell surface confirm those obtained with the human multiple myeloma cell line L363. Again, bispecific antibodies to BCMA / CD3 of the E1 / E4 epitope cluster - in contrast to their potent cytotoxic activity against CHO cells transfected with human BCMA were shown to be less potent in redirecting the cytotoxic activity of unstimulated PBMCs against human multiple myeloma cells, confirming the theory that the human BCMA E1 / E4 epitope may be less accessible on natural expressers of BCMA than on cells transfected with BCMA. Such a difference in activity between target cells transfected with BCMA and natural expressors as seen for E1 / E4 binders was not found for E3. Bispecific antibodies to BCMA / CD3 of the E3 epitope cluster presented EC values<sub>50</sub> 2 to 3 digits pg / ml and thus redirected unstimulated PBMC against NCI-H929 target cells with very good EC values<sub>50</sub> (see Figure 14 and Table 9).
Table 9: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 from epitope clusters E1 / E4 (rows 1 and 2) and E3 (rows 3 to 8) measured in a 48-hour FACS-based cytotoxicity assay with human PBMCs unstimulated as effector cells and the human multiple myeloma cell line NCI-H929 as the source of target cells.
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<td></td><td>bispecific antibody for BCMA / CD3</td><td>ECso [pg / mlj '</td><td>-mfrr ° '' • Treasury</td>
<td> 1</td><td>BCMA-54</td><td> 2604</td><td> 0,99</td>
<td> 2</td><td>BCMA-53</td><td> 2474</td><td> 0,99</td>
<td> 3</td><td>BCMA-83</td><td> 154</td><td> 0,93</td>
<td> 4</td><td>BCMA-98</td><td> 67,6</td><td> 0,87</td>
<td> 5</td><td>BCMA-71</td><td> 50,7</td><td> 0,96</td>
<td> 6</td><td>BCMA-34</td><td> 227</td><td> 0,99</td>
<td> 7</td><td>BCMA-74</td><td> 103</td><td> 0,97</td>
<td> 8</td><td>BCMA-20</td><td> 123</td><td> 0,97</td>
As expected, the EC values<sub>50</sub> they were inferior with the human multiple myeloma cell line NCI-H929, which expresses high levels of BCMA on the cell surface compared to L363. Example 14 Macaque T cells versus macaque BCMA-expressing target cells
Finally, the cytotoxic activity of bispecific BCMA / CD3 antibodies was analyzed in a FACS-based cytotoxicity assay using CHO cells transfected with macaque BCMA as target cells, and a macaque T cell line as the source of effector cells.
The macaque T cell line 4119LnPx (Knappe et al. Blood 95: 3256-61 (2000)) was used as the source of effector cells. Target cell labeling of CHO cells
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Transfected with macaque BCMA and the analysis of cytotoxic activity based on flow cytometry, were carried out as described above.
Macaque T cells of the 4119LnPx cell line were induced to efficiently kill CHO cells transfected with macaque BCMA by bispecific antibodies to BCMA / CD3 of the E3 epitope cluster. The antibodies presented very strong EC values<sub>50</sub> with 1 digit to 2 digit low pg / ml in this assay, confirming that these antibodies are very active in the macaque system. On the other hand, bispecific antibodies to BCMA / CD3 from the E1 / E4 epitope cluster showed significantly weaker potency with EC values<sub>50</sub> in the range of 2 digits to 3 digits of pg / ml (see Figure 15 and Table 10). E3-specific antibodies are therefore approximately 3 to almost 100 times more potent in the macaque system.
Table 10: EC values<sub>50</sub> [pg / ml] of bispecific antibodies to BCMA / CD3 from epitope clusters E1 / E4 (rows 1 and 2) and E3 (rows 3 to 8) measured in a 48-hour FACS-based cytotoxicity assay with the line 4119LnPx cell of macaque T cells as effector cells and CHO cells transfected with macaque BCMA as target cells.
<td></td><td>bispecific antibody for BCMA / CD3</td><td>EC<sub>50</sub> [pg / ml]</td><td>R-squared value</td>
<td> 1</td><td>BCMA-54</td><td> 78,5</td><td> 0,98</td>
<td> 2</td><td>BCMA-53</td><td> 183</td><td> 0,96</td>
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<td> 3</td><td>BCMA-83</td><td> 10,9</td><td> 0,97</td>
<td> 4</td><td>BCMA-98</td><td> 2,5</td><td> 0,89</td>
<td> 5</td><td>BCMA-71</td><td> 3,2</td><td> 0,97</td>
<td> 6</td><td>BCMA-34</td><td> 2,1</td><td> 0,95</td>
<td> 7</td><td>BCMA-74</td><td> 2,0</td><td> 0,95</td>
<td> 8</td><td>BCMA-20</td><td> 26</td><td> 0,98</td>
Example 15
Potency difference between monomer and dimer of bispecific antibody for
BCMA / CD3
In order to determine the difference in cytotoxic activity between the monomeric and dimeric forms of individual BCMA / CD3 bispecific antibodies (termed the potency difference), a chromium 51 release cytotoxicity assay was carried out as described above in the present (Example 8.1) with purified BCMA / CD3 bispecific antibody monomer and dimer. The difference in power was calculated as the relationship between the EC values<sub>50</sub> of the monomer and dimer of the bispecific antibody. Differences in potency of bispecific antibodies to BCMA / CD3 of the E3 epitope cluster tested were between 0.03 and 1.2. Therefore, there is substantially no more active dimer compared to its respective monomer.
Example 16
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Conversion from monomer to dim after three freeze / thaw cycles
The bispecific antibody monomer to BCMA / CD3 was subjected to three freeze / thaw cycles followed by high performance SEC to determine the percentage of initially monomeric antibody, which had been converted to antibody dimer.
15 pg of monomeric antibody were adjusted to a concentration of 250 pg / ml with generic buffer and then frozen at -80 ° C for 30 min followed by thawing for 30 min at room temperature. After three freeze / thaw cycles, the dimer content was determined by HPSEC. For this purpose, 15 pg aliquots of the monomeric isoforms of the antibodies were thawed and equalized at a concentration of 250 pg / ml in the original SEC buffer (10 mM citric acid- 75 mM lysine HCI- 4% trehalose - pH 7.2) followed by incubation at 37 ° C for 7 days. A high resolution SEC TSK Gel G3000 SWXL Column (Tosoh, Tokyo-Japan) was connected to an Ákta 10 FPLC purifier (GE Lifesciences) equipped with an A905 Autosampler autosampler. Column equilibration and run buffer consisted of KH<sub>2</sub>PO<sub>4</sub> 100 mM20 Na<sub>2</sub>SW<sub>4</sub> 200 mM adjusted to pH 6.6. After 7 days of incubation, the antibody solution (15 pg protein) was applied to the equilibrated column and elution was carried out at a flow rate of 0.75 ml / min at a maximum pressure of 7 MPa. The entire run was monitored at 280, 254 and 210 nm optical absorbance. The analysis was carried out by integrating peaks of the signal at 210 nm recorded on an evaluation sheet.<sup>142</sup> IMPI ^ iiwrrruTt μϊχκλνι: € - * <* - *
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INDUSTRY! <sup>w</sup> run of the Ákta Unicom program. The dimer content was calculated by dividing the area of the dimer peak by the total area of the monomer plus dimer peak.
Bispecific antibodies to BCMA / CD3 from the E3 epitope cluster showed dimer percentages of 0.7 to 1.1% after three freeze / thaw cycles, which is considered good. However, the BCMA / CD3 bispecific antibody dimer conversion rates of the E1 / E4 epitope cluster reached unfavorably high values, exceeding the threshold at disadvantageous dimer values of> 2.5% (4.7% and 3, 8%, respectively), see Table 11.
Table 11: Percentage of bispecific antibodies to BCMA / CD3 of the monomeric versus dimeric E1 / E4 epitope clusters (rows 1 and 2) and E3 (rows 3 to 8) after three freeze / thaw cycles determined by Molecular Exclusion Chromatography High Performance (HP-SEC).
<td></td><td>bispecific antibody for BCMA / CD3</td><td>Monomer [%]</td><td>Dimer [%]</td>
<td> 1</td><td>BCMA-54</td><td> 95,3</td><td> 4,7</td>
<td> 2</td><td>BCMA-53</td><td> 96,2</td><td> 3,8</td>
<td> 3</td><td>BCMA-83</td><td> 99,1</td><td> 0,9</td>
<td> 4</td><td>BCMA-98</td><td> 99,1</td><td> 0,9</td>
<td> 5</td><td>BCMA-71</td><td> 99,1</td><td> 0,9</td>
<td> 6</td><td>BCMA-34</td><td> 98,9</td><td> 1,1</td>
<td> 7</td><td>BCMA-74</td><td> 99,3</td><td> 0,7</td>
<td> 8</td><td>BCMA-20</td><td> 99,2</td><td> 0,8</td>
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Example 17
Thermostability
Melting temperature curves were determined by Differential Scanning Calorimetry (DSC) to determine the intrinsic biophysical protein stabilities of bispecific antibodies to BCMA / CD3. These experiments were carried out using a MicroCal LLC (Northampton, MA, USA) VPDSC device. The energy consumption of a sample containing bispecific antibody for BCMA / CD3 was recorded from 20 to 90 ° C compared to a sample that only contained the antibody formulation buffer.
In detail, the bispecific antibodies for BCMA / CD3 were adjusted to a final concentration of 250 pg / ml in storage buffer. 300 µl of the prepared protein solutions were transferred to a deep well plate and placed in position on the cooled autosampler shelf of the DSC device. Additional wells were filled with SEC run buffer as reference material for measurement. For the measurement process, the protein solution was transferred by the autosampler to a capillary. An additional capillary was filled with the SEC run buffer as a reference. Heating and recording of the heating energy required to heat both capillaries to the same temperature in the range of 20 to 90 ° C was carried out for all samples.
To record the respective melting curve, the overall temperature of the sample was increased stepwise. The energy consumption of the sample and the reference formulation buffer was recorded at each temperature T. The difference in energy consumption Cp (kcal / mol / ° C) of the sample minus the reference was plotted against the
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All BCMA / CD3 bispecific antibodies of the E3 epitope cluster tested showed favorable thermostability with melting temperatures above 60 ° C, more precisely between 61.62 ° C and 63.05 ° C.
Example 18 Exclusion of plasma interference by flow cytometry
To determine the potential interaction of bispecific BCMA / CD3 antibodies with human plasma proteins, a plasma interference assay was established. To this end, 10pg / ml of the respective bispecific antibodies for BCMA / CD3 were incubated for one hour at 37 ° C in 90% human plasma. Subsequently, binding to CHO cells expressing human BCMA was determined by flow cytometry.
For flow cytometry, 200,000 cells from the respective cell lines were incubated for 30 min on ice with 50 µl of purified antibody at a concentration of 5 pg / ml. The cells were washed twice in PBS / 2% FCS and binding of the constructs was detected with a murine PentaHis antibody (Qiagen; diluted 1:20 in 50 µl of PBS / 2% FCS). After washing, bound PentaHis antibodies were detected with a Fe gamma-specific antibody (Dianova) conjugated to phycoerythrin, diluted 1: 100 in PBS / 2% FCS. The samples were measured by flow cytometry in
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a FACSCanto II instrument and were analyzed using the Becton Dickinson program 'F / ^ toiva gimióos). * '' '........
The data obtained were compared with a control test using PBS instead of human plasma. The relative union was calculated as follows:
(PBS sample signal / signal without detection agent) / (plasma sample signal / signal without detection agent).
In this experiment, it was obvious that there was no significant reduction in target binding of the respective bispecific antibodies to BCMA / CD3 of the plasma protein-mediated E3 epitope cluster. The relative plasma interference value was below a value of 2 in all cases, more precisely between 1.29 ± 0.25 and 1.70 ± 0.26 (a value of “2” being considered as the lower threshold for interference signals).
Example 19
Therapeutic efficacy of bispecific antibodies to BCMA / CD3 in xenograft models of human tumors
On day 1 of the study, 5x10 were injected subcutaneously.<sup>6</sup> cells of the human cancer cell line NCI-H929 in the right dorsal flank of female NOD / SCID mice.
On day 9, when the mean tumor volume had reached approximately 100 mm<sup>3</sup>, CD3 T cells were transplanted<sup>+</sup> human multiplied in vitro to mice by injection of approximately 2x10<sup>7</sup> cells within the peritoneal cavity of animals. Mice in the vehicle 1 control group (n = 5) received no effector cells and were used as a non-transplanted control for comparison with the
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OE LA ¡> K »ISDAb INDUSTRIAL vehicle 2 control group (n = 10, receiving effector cells) to monitor the impact of T cells alone on tumor growth.
Antibody treatment began on day 13, when the mean tumor volume had reached approximately 200 mm<sup>3</sup>. The mean tumor size of each treatment group on the day of treatment start was not statistically different from any other group (analysis of variance). Mice were treated with 0.5 mg / kg / day of the bispecific antibodies for BCMA / CD3 BCMA-98 x CD3 (group 3, n = 7) or BCMA-34 x CD3 (group 4, n = 6) by intravenous injection in bolus for 17 days.
Tumors were gauged during the study and progress was assessed by intergroup comparison of tumor volumes (TV). T / C tumor growth inhibition [%] was determined by calculating TV as T / C% = 100 x (mean TV of the analyzed group) / (mean TV of the control group 2). The results are shown in Table 12 and Figure 16.
Table 12: Mean tumor volume (TV) and tumor growth inhibition (T / C) at days 13 to 30.
<td>Group dose</td><td>Data</td><td>d13</td><td>d14</td><td>d15</td><td>d16</td><td>d18</td><td>d19</td><td>d21</td><td>d23</td><td>d26</td><td>d28</td><td>d30</td>
<td rowspan="2">1 Vehicle cell-free control T</td><td>TV med. [mm<sup>3</sup>]</td><td> 238</td><td> 288</td><td> 395</td><td> 425</td><td> 543</td><td> 632</td><td> 863</td><td> 1067</td><td> 1116</td><td> 1396</td><td> 2023</td>
<td>T / C [%]</td><td> 120</td><td> 123</td><td> 127</td><td> 118</td><td> 104</td><td> 114</td><td> 122</td><td> 113</td><td> 87</td><td> 85</td><td> 110</td>
<td> 2</td><td>TV</td><td> 198</td><td> 235</td><td> 310</td><td> 361</td><td> 525</td><td> 553</td><td> 706</td><td> 942</td><td> 1290</td><td> 1636</td><td> 1839</td>
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<td rowspan="3">Vehicle control</td><td rowspan="2">med. [mm<sup>3</sup>]</td><td rowspan="2"></td><td rowspan="2"></td><td rowspan="2"></td><td rowspan="2"></td><td rowspan="2"></td><td rowspan="2"></td><td></td><td></td><td></td><td></td><td></td>
<td></td><td></td><td></td><td></td><td></td>
<td>T / C [%]</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td>
<td rowspan="2">3 BCMA- 98</td><td>TV med. [mm<sup>3</sup>]</td><td> 207</td><td> 243</td><td> 248</td><td> 235</td><td> 164</td><td> 137</td><td> 93,5</td><td> 46,2</td><td> 21,2</td><td> 0,0</td><td> 0,0</td>
<td>T / C [%]</td><td> 105</td><td> 104</td><td> 79,7</td><td> 65,0</td><td> 31,2</td><td> 24,7</td><td> 13,2</td><td> 4,9</td><td> 1,6</td><td> 0,0</td><td> 0,0</td>
<td rowspan="2">4 BCMA- 3. 4</td><td>TV med. [mm<sup>3</sup>]</td><td> 206</td><td> 233</td><td> 212</td><td> 189</td><td> 154</td><td> 119</td><td> 56,5</td><td> 17,4</td><td> 0,0</td><td> 0,0</td><td> 0,0</td>
<td>T / C [%]</td><td> 104</td><td> 99,2</td><td> 68,2</td><td> 52,3</td><td> 29,4</td><td> 21,5</td><td> 8,0</td><td> 1,8</td><td> 0,0</td><td> 0,0</td><td> 0,0</td>
Example 20 Exclusion of lysis of negative target cells
An in vitro lysis assay was carried out using the BCMA-positive human multiple myeloma cell line NCI-H929 and purified T cells at an effector cell to target cell ratio of 5: 1 and with an incubation time of 24 hours. . Bispecific antibodies to BCMA / CD3 of the E3 epitope cluster (BCMA-34 and BCMA-98) showed high potency and efficiency in the lysis of NCI-H929. However, no lysis was detected in the BCMA negative cell lines HL60 (AML / myeloblast morphology), MES-SA (uterine sarcoma, myeloblast morphology), and SNU-16 (stomach carcinoma, epithelial morphology) for up to 500 nM of the respective antibody.
Example 21
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Induction of T-cell activation of different PBMC subsets
A FACS-based cytotoxicity assay (48h; E: T = 10: 1) was carried out using human multiple myeloma cell lines NCI-H929, L-363 and OPM-2 as target cells and different subsets of human PBMC (CD4<sup>+</sup> / CD8<sup>+</sup> / CD25<sup>+</sup> / CD69<sup>+</sup>) as effector cells. The results (see Table 13) show that the degree of activation, measured as the EC value<sub>50</sub>, is essentially in the same range for the different subsets of PBMC analyzed.
Table 13: EC values<sub>50</sub> [ng / ml] of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster measured in a 48-hour FACS-based cytotoxicity assay with different subsets of human PBMC as effector cells and different human multiple myeloma cell lines as target cells .
<td colspan="2"></td><td colspan="2">EC<sub>50</sub> [ng / ml]</td>
<td>Cellphone line</td><td>PBMC</td><td>BCMA-98 x CD3</td><td>BCMA-34xCD3</td>
<td rowspan="4">NCI-H929</td><td>CD4<sup>+</sup> / CD25<sup>+</sup></td><td> 1,46</td><td> 1,20</td>
<td>CD8<sup>+</sup> / CD25<sup>+</sup></td><td> 0,53</td><td> 0,49</td>
<td>CD4<sup>+</sup> / CD69<sup>+</sup></td><td> 0,59</td><td> 0,47</td>
<td>CD8<sup>+</sup> / CD69<sup>+</sup></td><td> 0,21</td><td> 0,21</td>
<td rowspan="3">OPM-2</td><td>CD4<sup>+</sup> / CD25<sup>+</sup></td><td> 2,52</td><td> 4,88</td>
<td>CD8 * / CD25 *</td><td> 1,00</td><td> 1,20</td>
<td>CD4<sup>+</sup> 1 CD69<sup>+</sup></td><td> 1,65</td><td> 2,27</td>
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<td></td><td>CD8<sup>+</sup> / CD69 *</td><td> 0,48</td><td> 0,42</td>
<td rowspan="4">L-363</td><td>CD4<sup>+</sup> / CD25<sup>+</sup></td><td> 0,54</td><td> 0,62</td>
<td>CD8<sup>+</sup> / CD25<sup>+</sup></td><td> 0,24</td><td> 0,28</td>
<td>CD4<sup>+</sup> / CD69<sup>+</sup></td><td> 0,35</td><td> 0,34</td>
<td>CD8 * / CD69<sup>+</sup></td><td> 0,12</td><td> 0,11</td>
Example 22 Induction of cytokine release
A FACS-based cytotoxicity assay (48h; E: T = 10: 1) was carried out using human multiple myeloma cell lines NCI-H929, L-363 and OPM-2 as target cells and human PBMC as effector cells. . Cytokine release levels [pg / ml] were determined at increasing concentrations of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster. The following cytokines were analyzed: IL-2, IL-6, IL-10, TNF, and IFN-gamma. The results are shown in Table 14 and in Figure 17.
Table 14: Release of IL-2, IL-6, IL-10, TNF and IFN-gamma [pg / ml] induced by 2.5 pg / ml of bispecific antibodies to BCMA / CD3 from the E3 epitope cluster (BCMA- 98 and BCMA-34) in a 48-hour FACS-based cytotoxicity assay with human PBMC as effector cells and different human multiple myeloma cell lines as target cells (E: T = 10: 1).
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<td rowspan="2"></td><td colspan="5"></td>
<td>IL-2</td><td>IL-6</td><td>IL-10</td><td>TNF</td><td>IFN-gamma</td>
<td>BCMA-98</td><td> 1357</td><td> 699</td><td> 2798</td><td> 10828</td><td> 73910</td>
<td>BCMA-34</td><td> 1327</td><td> 631</td><td> 3439</td><td> 6675</td><td> 77042</td>
<td rowspan="2"></td><td colspan="5">OPM-2</td>
<td>IL-2</td><td>IL-6</td><td>IL-10</td><td>TNF</td><td>IFN-gamma</td>
<td>BCMA-98</td><td> 41</td><td> 118</td><td> 990</td><td> 5793</td><td> 33302</td>
<td>BCMA-34</td><td> 28</td><td> 109</td><td> 801</td><td> 4913</td><td> 23214</td>
<td rowspan="2"></td><td colspan="5">L-363</td>
<td>IL-2</td><td>IL-6</td><td>IL-10</td><td>TNF</td><td>IFN-gamma</td>
<td>BCMA-98</td><td> 97</td><td> 314</td><td> 2433</td><td> 5397</td><td> 64981</td>
<td>BCMA-34</td><td> 168</td><td> 347</td><td> 2080</td><td> 5930</td><td> 75681</td>
<td></td><td>SEQ ID NO</td><td>Designation</td><td>Designation</td><td>Format / font</td><td>Kind</td><td>Sequence</td><td></td><td></td>
<td></td><td> 1</td><td>BCMA-1</td><td>BC 5G9 91- C7-B10</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td></td><td></td>
<td></td><td> 2</td><td>BCMA-1</td><td>BC 5G9 91- C7-B10</td><td>VH CDR2</td><td>aa</td><td>SIITSGDATYYRDSVKG</td><td></td><td></td>
<td rowspan="2"> 5</td><td> 3</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td></td><td></td>
<td> 4</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>VLCDR1</td><td>aa</td><td>KASQSVGINVD</td><td></td><td></td>
<td></td><td> 5</td><td>BCMA-1</td><td>BC 5G9 91- C7-B10</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td><td></td>
<td></td><td> 6</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td></td><td></td>
<td> 10</td><td> 7</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>VH</td><td>aa</td><td colspan="2">0ν0ΕνΕ3σθ6λΑ70ΡΟΝ3ΕΡΕ30ΑΑ3αΡΤΡ3ΝΥϋΜΑΝνΡ0ΆΡσΚΟΕΕΝνΑ3ΙΙΤ3σθΑΤΥΥΡΏ3νκσΡ FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td><td></td>
<td></td><td> 8</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 15</td><td> 9</td><td>BCMA-1</td><td>BC 5G9 91C7-B10</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td> 151</td>
<td> 20</td><td> 10</td><td>BCMA-1 HL x CD3 HL</td><td>BC 5G9 91C7-B10 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>ΟνΟΕνΕΒΟσσννΟΡΟΝΞΕΕΕεϋΑΑΕΘΡΤΡΒΝΥϋΜΑΝνΕΟΑΡσΚΟΕΕΝνΑΒΙΙΤΒαΏΑΤ ^ FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGS GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINAZDWYQQKPGQAPRLLIYGASNRHTC GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGI LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSI NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTW ': PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGG1 QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td><sup>r</sup>YRDSVKGR GGGGSGGG IPARFSGS VQPGGajfe · NTAYIjá ^ Nj QEPSJ5§Zg 7 \ AL1§j¿rv</td><td> 4</td>
<td></td><td> 11</td><td>BCMA-2</td><td>BC 5G9 91- C7-D8</td><td>VHCDR1</td><td>aa</td><td>NYDMA</td><td>/Saw</td><td></td>
<td></td><td> 12</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VH CDR2</td><td>aa</td><td>SIITSGDMTYYRDSVKG</td><td>'IS6'</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td> 13</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VH CDR3</td><td>aa</td><td colspan="2">HDYYDGSYGFAY</td>
<td> 14</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VLCDR1</td><td>aa</td><td colspan="2">KASQSVGINVD</td>
<td> 15</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASNRHT</td>
<td> 16</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VL CDR3</td><td>aa</td><td colspan="2">LQYGSIPFT</td>
<td> 17</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 18</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 19</td><td>BCMA-2</td><td>BC 5G9 91C7-D8</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 20</td><td>BCMA-2 HL x CD3 HL</td><td>BC 5G9 91C7-D8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">0ν0Ε · νΕ3ααθνν0ΡαΗ3ΕΕΕ3εΑΑ3σΡΤΡ3ΝΥΟΜΑΜνΗ0ΑΡΟΚ6ΕΕΝνΑ3ΙΙΤεσΏΜΤΥΥΗϋ3νΚΟΗ FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 21</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td></td>
<td> 22</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VH CDR2</td><td>aa</td><td>SIITSGDATYYRDSVKG</td><td>2 u</td>
<td> 23</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td></td>
<td> 24</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VLCDR1</td><td>aa</td><td>KASQSVGINVD</td><td>MKXIC PROHt NDUST</td>
<td> 25</td><td>BCMA-3</td><td>BC 5G9 91- E4-B10</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td>
<td> 26</td><td>BCMA-3</td><td>BC 5G9 91-</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td>rf 9</td>
in
IMPI
<td></td><td></td><td>E4-B10</td><td></td><td></td><td></td><td rowspan="12"></td>
<td> 27</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VH</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 28</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>VL</td><td>aa</td><td>EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 29</td><td>BCMA-3</td><td>BC 5G9 91E4-B10</td><td>scFv</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 30</td><td>BCMA-3 HL x CD3 HL</td><td>BC 5G9 91E4-B10 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ΡαστνΤ1.Ταα33ΤΘΑνΤ3αΝΥΡΝΝν02ΚΡΟ0ΑΡΡαΐ.ΙΰΟΤΚΡΕΑΡαΤΡΑΕΡ3α3Ι.ΕΟΰΚΑΑΕΤΕ3αν QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 31</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td>
<td> 32</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VH CDR2</td><td>aa</td><td>SIITSGDMTYYRDSVKG</td>
<td> 33</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td>
<td> 34</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VL CDR1</td><td>aa</td><td>KASQSVGINVD</td>
<td> 35</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td>
<td> 36</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT i</td>
<td> 37</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VH</td><td>aa</td><td>qvqlvesgggwqpgrslrlscaasgftfsnydmawvrqapgkglewvasiitsgdmtyyrdsvkgW 1 FTISRDNSKNTL · YL · QMNSL · RSΞDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS 1</td>
<td> 38</td><td>BCMA-4</td><td>BC 5G9 91E4-D8</td><td>VL</td><td>aa</td><td>EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIP ^ RFSG ^^ »· GTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK I 333 ^ ·</td><td></td>
<td> 39</td><td>BCMA-4</td><td>BC 5G9 91-</td><td>scFv</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYJ'RDsVRál ^ '</td><td> 1</td>
<img file="MX349396B_D0081.tif" />
<img file="MX349396B_D0082.tif" />
E4-D8
FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHEYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG
<td></td><td></td><td></td><td></td><td></td><td>GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 40</td><td>BCMA-4 HL x CD3 HL</td><td>BC 5G9 91E4-D8 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYEMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 41</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td></td>
<td> 42</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VH CDR2</td><td>aa</td><td>SIITSGDATYYRDSVKG</td><td></td>
<td> 43</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td></td>
<td> 44</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VL CDR1</td><td>aa</td><td>KASQSVGINVD</td><td></td>
<td> 45</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td>
<td> 46</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td> 154</td>
<td> 47</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>VH</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGD ATYYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHEYYEGSYGFAYWGQGTLVTVSS</td><td></td>
<td> 48</td><td>BCMA-5</td><td>BC 5G9 91- D2-B10</td><td>VL</td><td>aa</td><td>EIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 49</td><td>BCMA-5</td><td>BC 5G9 91D2-B10</td><td>scFv</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYEMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGG <3SGGG GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK] <</td><td> 3</td>
<td> 50</td><td>BCMA-5 HL x CD3 HL</td><td>BC 5G9 91D2-B10 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDEVKGB FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGCSGG ^ ^ ^ GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIP FSGSS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQ ^ ^ GGSLK</td><td>ÍPD</td>
<td></td><td></td><td></td><td></td><td></td><td>1 il</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td colspan="2">LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ρσστντΒτσσΞΞταΑντΞσΝΥΡΝΝνοςκρσοΑΡκσΕίοοτκΕΏΑΡατΡΆΚΡεσεΒΕσοκΑΑΏτηεον QPEDEAEYYCVLWYSNRWVFGGGTKLTVL ·</td>
<td> 51</td><td>BCMA-6</td><td>BC 5G9 91D2-D8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 52</td><td>BCMA-6</td><td>BC 5G9 91D2-D8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SIITSGDMTYYRDSVKG</td>
<td> 53</td><td>BCMA-6</td><td>BC 5G9 91D2-D8</td><td>VH CDR3</td><td>aa</td><td colspan="2">HDYYDGSYGFAY</td>
<td> 54</td><td>BCMA-6</td><td>BC 5G9 91- D2-D8</td><td>VLCDR1</td><td>aa</td><td colspan="2">KASQSVGINVD</td>
<td> 55</td><td>BCMA-6</td><td>BC 5G9 91D2-D8</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASNRHT</td>
<td> 56</td><td>BCMA-6</td><td>BC 5G9 91- D2-D8</td><td>VL CDR3</td><td>aa</td><td colspan="2">LQYGSIPFT</td>
<td> 57</td><td>BCMA-6</td><td>BC 5G9 91- D2-D8</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 58</td><td>BCMA-6</td><td>BC 5G9 91D2-D8</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 59</td><td>BCMA-6</td><td>BC 5G9 91- D2-D8</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 60</td><td>BCMA-6 HL x CD3 HL</td><td>BC 5G9 91- D2-D8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVE GGGWQ PGR S S S CAASG LRL NYDMAWVRQAPGKGLEWVASIITSGDMT FS FT ^ FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGS GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTC GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGL LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSB NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTW1 PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGB QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>-yrdsvkgr GGGGSGGG .IPARFSGS VQPGGSLK NTAYL (J®F QEPSLW * 3 AALTjSp¡2</td>
<td> 61</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td> ***</td>
ί,
155
<td></td><td> 62</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VH CDR2</td><td>aa</td><td>SIITSGDATYYRDSVKG</td><td></td><td></td>
<td></td><td> 63</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td></td><td></td>
<td></td><td> 64</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VL CDR1</td><td>aa</td><td>KASQSVGINVD</td><td></td><td></td>
<td></td><td> 65</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td><td></td>
<td> 5</td><td> 66</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td></td><td></td>
<td></td><td> 67</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td><td></td>
<td></td><td> 68</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 10</td><td> 69</td><td>BCMA-7</td><td>BC 5G9 92E10-B10</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 15</td><td> 70</td><td>BCMA-7 HL x CD3 HL</td><td>BC 5G9 92E10B10HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDATYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td rowspan="2"> 20</td><td> 71</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td> 5</td><td></td>
<td> 72</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>VH CDR2</td><td>aa</td><td>SIITSGDMTYYRDSVKG</td><td>□ i</td><td></td>
<td></td><td> 73</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td>11 CM »A PtCF INDU!</td><td></td>
<td></td><td> 74</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>VL CDR1</td><td>aa</td><td>KASQSVGINVD</td><td>i Cano IKDAl TRIAL</td><td> 1</td>
<td></td><td> 75</td><td>BCMA-8</td><td>BC 5G9 92-</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td><td></td>
156
<td></td><td></td><td>E10-D8</td><td></td><td></td><td colspan="2"></td>
<td> 76</td><td>BCMA-8</td><td>BC 5G9 92- E10-D8</td><td>VL CDR3</td><td>aa</td><td colspan="2">LQYGSIPFT</td>
<td> 77</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 78</td><td>BCMA-8</td><td>BC 5G9 92- E10-D8</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTE FTLTIS S LQAEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 79</td><td>BCMA-8</td><td>BC 5G9 92E10-D8</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTVSRDNSKNTL · · RAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS YLQMNSL GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 80</td><td>BCMA-8 HL x CD3 HL</td><td>BC 5G9 92E10-D8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGDMTYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ροστντΒτοσΒετσΑντεοΝΥΡΝΝνοοκρσοΑΡΡσηισοτκΡΕΑΡστΡΑΡΡεσΞΓΕσσκΑΑΕΤΒδσν QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 81</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYWIH</td>
<td> 82</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VH CDR2</td><td>aa</td><td colspan="2">AIYPGNSDTHYNQKFQG</td>
<td> 83</td><td>BCMA-9</td><td>BC H1 38- D2-A4</td><td>VH CDR3</td><td>aa</td><td colspan="2">SSYYYDGSLFAS</td>
<td> 84</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VL CDR1</td><td>aa</td><td>RSSQSIVHSNGNTYLY</td><td></td>
<td> 85</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VL CDR2</td><td>aa</td><td>RVSNRFS</td><td>nsttp OF</td>
<td> 86</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VL CDR3</td><td>aa</td><td>FQGSTLPFT</td><td></td>
<td> 87</td><td>BCMA-9</td><td>BC H1 38- D2-A4</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYlVTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td><td>BKFq ^ í</td>
<td> 88</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>VL</td><td>aa</td><td>ΠίνΜΤΟΤΡΤΒΕΞνΒΡσΟΡΑΕΙΞσΡΒΞΟείνΗΞΝσΝΤΥΒΥΝΥΕΟΚΡΟΟΡΡΟΒΕΙΥΡνΞΝΡΓί</td><td><sup>GVPI</sup>^</td>
157
<td></td><td></td><td></td><td></td><td></td><td>SGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td></td><td></td>
<td> 89</td><td>BCMA-9</td><td>BC H1 38D2-A4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK νΤΙΤΕΌΤ3Α3ΤΑΥΜΕΒ35ΒΤ3ΕΌΤΆνΥΥΟΤΕ33ΥΥΎΟΘ3ΕΡΑ3ΝαθΟΤΕντν53ααθΘ3ασΘ03ασα GSDIVMTQTPLSLSVSPGQPASISCESSQSIVHSNGNTYLYWYLQKPGQPPQLLIYEVSNEFSGVPD EFSGSGSGTDFTLKISEVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td></td>
<td> 90</td><td>BCMA-9 HL x CD3 HL</td><td>BC H1 38D2-A4 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG GSDIVMTQTPLSLSVSPGQPASISCESSQSIVHSNGNTYLYWYLQKPGQPPQLLIYEVSNEFSGVPD ΕΡ3σ3σ3ΘΤΌΡΤΕΚΙ3ΕνΕΑΕθνσνΥΥαΡ0σ3ΤΕΡΡΤΡΟ0στΚΕΕΙΚ3σσσσ3Εν0ΕνΕ3θασΕν0Ρ GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTA YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAAL TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 91</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VH CDR1</td><td>aa</td><td>NYWIH</td><td></td><td></td>
<td> 92</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VH CDR2</td><td>aa</td><td>AIYPGNSDTHYNQKFQG</td><td></td><td></td>
<td> 93</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VH CDR3</td><td>aa</td><td>SSYYYDGSLFAS</td><td></td><td></td>
<td> 94</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VLCDR1</td><td>aa</td><td>RSSQSIVHSNGNTYLY</td><td></td><td></td>
<td> 95</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VL CDR2</td><td>aa</td><td>RVSNRFS</td><td></td><td></td>
<td> 96</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VL CDR3</td><td>aa</td><td>FQGSHLPFT</td><td></td><td></td>
<td> 97</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTH VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td><td>YNQKFQGK</td><td>-J</td>
<td> 98</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVSPGQPASΙ3αΕ3303ΐνΗ3ΝσΝΤΥΕΥΜΥΕ0ΚΡσ0ΡΡ0ΕΕΙΥΕν3ΝΕ SGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK</td><td>ω II hj VI 3QJ OlfU ^ Y ÍATj</td><td></td>
<td> 99</td><td>BCMA-10</td><td>BC H1 38D2-F12</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTE νΤΙΤΕΌΤ3Α3ΤΑΥΜΞΕ33ΕΤ3ΕΟΤΑνΥΥΟΤΕ33ΥΥΥΌσ3ΕΕΑ3ΝσθβΤΕντν33σσθσε σ3ϋΐνΜΤΟΤΡΕ3Ε3ν3Ρα0ΡΑ3Ι3ΟΕ3303ΐνΗ3ΝΘΝΤΥΕΥΜΥΕ0ΚΡ6ΟΡΡ0ΕΕΙΥΕν3 RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK</td><td>ÍNQKl ^ fc 3GGGS | & G '^ RFSGVí> faith "</td><td> 3</td>
<td></td><td></td><td></td><td></td><td></td><td></td><td>rf «W</td><td></td>
158
<td> 100</td><td>BCMA-10HL x CD3 HL</td><td>BC H1 38D2-F12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG GSDIVMTQTPLSLSVSPGQPASISCRSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVSNRFSGVPD RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIKSGGGGSEVQLVESGGGLVQP GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTA YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAAL TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 101</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYWIH</td>
<td> 102</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VH CDR2</td><td>aa</td><td colspan="2">AIYPGNSDTHYNQKFQG</td>
<td> 103</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VH CDR3</td><td>aa</td><td colspan="2">SSYYYDGSLFAS</td>
<td> 104</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VLCDR1</td><td>aa</td><td colspan="2">KS S QSIVHSNGNTYLY</td>
<td> 105</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VL CDR2</td><td>aa</td><td colspan="2">RVSNRFS</td>
<td> 106</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VL CDR3</td><td>aa</td><td colspan="2">FQGSTLPFT</td>
<td> 107</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td>
<td> 108</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQQASISCKSSQSlVHSNGNTYLYWYLiQKPGQPPQLLIYRVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCFQGS TLPFTFGQGTKLEIK</td>
<td> 109</td><td>BCMA-11</td><td>BC H1 38C1-A4</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDT νΤΙΤΕΟΤ3Α3ΤΑΥΜΕΕ33ΕΤ3ΕΏΤΑνΥΥ0ΤΡ35ΥΥΥϋσ3ΕΕΑ3Ν60σΤΕντν33σσσσ GSDIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLIjIYRX RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td>HYNQKFQGK SGGGGSGGG SNRFSGVPD</td>
<td> 110</td><td>BCMA-11 HL x CD3 HL</td><td>BC H1 38C1-A4HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDl VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGG GSDIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRV ΕΡ3Ο3Ο3ΟΤΟΡΤΕΚΙ3ΕνΕΑΕΌνθνΥΥΟΕ0σ3ΤΕΡΡΤΕΟ0σΤΚΕΕΙΚ3ασσθ3Εν0Εν GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTI ΥΕ0ΜΝΝΕΚΤΕϋΤΑνΥΥ0νΗΗσΝΡΟΝΞΥΙ3ΥΜΑΥνΐα0σΤΕντν336αασ3αθθα8Ο6θα SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSG</td><td>hynqkS® ^ F SNRFgpr ^ m SSGG'á & ^ QE *<sup>1 </sup>3RDD§ ^ F ^ K " 3LLG ^^) ^ [|</td>
159
<img file="MX349396B_D0083.tif" />
<td></td><td></td><td></td><td></td><td></td><td>TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td><td></td>
<td> 111</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VH CDR1</td><td>aa</td><td>NYWIH</td><td></td><td></td>
<td> 112</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VH CDR2</td><td>aa</td><td>AIYPGNSDTHYNQKFQG</td><td></td><td></td>
<td> 113</td><td>BCMA-12</td><td>BC H1 38- C1-F12</td><td>VH CDR3</td><td>aa</td><td>SSYYYDGSLFAS</td><td></td><td></td>
<td> 114</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VLCDR1</td><td>aa</td><td>KSSQSIVHSNGNTYLY</td><td></td><td></td>
<td> 115</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VLCDR2</td><td>aa</td><td>RVSNRFS</td><td></td><td></td>
<td> 116</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VLCDR3</td><td>aa</td><td>FQGSHLPFT</td><td></td><td></td>
<td> 117</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td><td></td>
<td> 118</td><td>BCMA-12</td><td>BC H1 38- C1-F12</td><td>VL</td><td>aa</td><td colspan="2">ϋΐνΜΤ0ΤΡΕ3Ε3νΤΡ600Α3Ι3εΚ3303ΐνΗ3ΝΟΝΤΥΕΥΝΥΒ0ΚΡσ0ΡΡ0ΕΕΙΥΕν3ΝΕΡ3θνΡΟΕΡ SGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK</td><td></td>
<td> 119</td><td>BCMA-12</td><td>BC H1 38C1-F12</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGK VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG GSDIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVSNRFSGVPD RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK</td><td> 160</td>
<td> 120</td><td>BCMA-12 HL x CD3 HL</td><td>BC H1 38C1-F12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWIGAIYPGNSDTH VTITRDTSASTAYMELSSLTSEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGS GSDIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVS RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIKSGGGGSEVQLVE GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTIS YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGS SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGS TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>YNQKFQGK GGGGSGGG NRFSGVPD SGGGLVQP RDDSKNTA QTWTQEP □ LGGKAAL</td><td></td>
<td> 121</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VH CDR1</td><td>aa</td><td>NYWIH</td><td>II viaa oiau UT</td><td rowspan="3"></td>
<td> 122</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VH CDR2</td><td>aa</td><td>AIYPGNSDTHYNQKFQG</td><td></td>
<td> 123</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VH CDR3</td><td>aa</td><td>SSYYYDGSLFAS</td><td>JV ( ON<sup>1</sup>Lr</td>
<td> 124</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VL CDR1</td><td>aa</td><td>KS S QSI VHSNGNTYLY</td><td></td><td></td>
<td> 125</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VL CDR2</td><td>aa</td><td>RVSNRFS</td><td></td><td></td>
<td> 126</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VL CDR3</td><td>aa</td><td>FQGSTLPFT</td><td></td><td></td>
<td> 127</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAWAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDTHYNQKFQGR VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td><td></td>
<td> 128</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>VL</td><td>aa</td><td colspan="2">οινΜτςτΡΒΕΕεντρσοοΑειεοκεβοεινΗεΝσΝΤΥΕΥΝΥΒΟΚΡαορρροΕΕίΥΕνΞΝΕΡΞσνΡΌΕΡ SGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td></td>
<td> 129</td><td>BCMA-13</td><td>BC H1 39B2-A4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAWAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDTHYNQKFQGR VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG GSDIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVSNRFSGVPD RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td></td>
<td> 130</td><td>BCMA-13 HL x CD3 HL</td><td>BC H1 39B2-A4 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAWAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDTHYNQKFQGR VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG 03ΌΐνΜΤ0ΤΡΗ3Η3νΤΡσ00Α3Ι3αΚ3Ξ03ΐνΗ3ΝΟΝΤΥΗΥΗΥΗ0ΚΡα0ΡΡ0ΗΏΙΥΕν3ΝΕΡ3σνΡΟ RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIKSGGGGSEVQLVESGGGLVQP GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTA YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAAL TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td> 161</td>
<td> 131</td><td>BCMA-14</td><td>BC H1 39- B2-F12</td><td>VH CDR1</td><td>aa</td><td>NYWIH</td><td></td><td></td>
<td> 132</td><td>BCMA-14</td><td>BC H1 39B2-F12</td><td>VH CDR2</td><td>aa</td><td>AIYPGNSDTHYNQKFQG</td><td></td><td> |</td>
<td> 133</td><td>BCMA-14</td><td>BC H1 39B2-F12</td><td>VH CDR3</td><td>aa</td><td>SSYYYDGSLFAS</td><td>Λ! □ 3 H ·?</td><td></td>
<td> 134</td><td>BCMA-14</td><td>BC H1 39- B2-F12</td><td>VLCDR1</td><td>aa</td><td>KSSQSIVHSNGNTYLY</td><td>DGMI nw o. II</td><td></td>
<td> 135</td><td>BCMA-14</td><td>BC H1 39- B2-F12</td><td>VL CDR2</td><td>aa</td><td>RVSNRFS</td><td>n ICANC 1KDAP pTMIAL ¡ i</td><td>I</td>
<td> 136</td><td>BCMA-14</td><td>BC H1 39B2-F12</td><td>VL CDR3</td><td>aa</td><td>FQGSHLPFT</td><td></td><td></td>
<td> 137</td><td>BCMA-14</td><td>BC H1 39-</td><td>VH</td><td>aa</td><td>QVQLVQSGAWAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDT]</td><td>YNQ]</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td></td><td></td><td>B2-F12</td><td></td><td></td><td colspan="2">VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSS</td>
<td> 138</td><td>BCMA-14</td><td>BC H1 39B2-F12</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQQASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK</td>
<td> 139</td><td>BCMA-14</td><td>BC H1 39B2-F12</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAVVAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDTHYNQKFQGR VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG SVTPGQQASISCKSSQSIVHSNGNTYL GSDIVMTQTPL · SL · · · QKPGQPPQLLIYRVSNRFSGVPD RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK YWYL</td>
<td> 140</td><td>BCMA-14 HL x CD3 HL</td><td>BC H1 39B2-F12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAWAKPGASVKVSCKASGYTFTNYWIHWVKQAPGQRLEWMGAIYPGNSDTHYNQKFQGR VTLTTDTSASTAYMELSSLRNEDTAVYYCTRSSYYYDGSLFASWGQGTLVTVSSGGGGSGGGGSGGG SVTPGQQASISCKSSQSIλ7HSNGNTYLYWYL GSDIVMTQTPL · SL · · · IYRVSNRFSGVPD ΕρεοεαεΘΤΏΡΤΒκίδΕνΕΑΕονσνγγαΡοαΒΗΕΡΡΤΕσοστκΕΕίκΞσαοσΞΞνοΓνΕεσασΕνορ QKPGQPPQLL GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTA YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAAL · TLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 141</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VH CDR1</td><td>aa</td><td colspan="2">SYWIH</td>
<td> 142</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VH CDR2</td><td>aa</td><td colspan="2">AIYPGNSDTHYNQKFQG</td>
<td> 143</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VH CDR3</td><td>aa</td><td colspan="2">SSYYYDGSLFAD</td>
<td> 144</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VLCDR1</td><td>aa</td><td colspan="2">KSSQSIVHSNGNTYLY</td>
<td> 145</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VL CDR2</td><td>aa</td><td colspan="2">RVSNRFS</td>
<td> 146</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VL CDR3</td><td>aa</td><td>FQGSTLPFT</td><td></td>
<td> 147</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRLEWIGAIYPGNSD VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGQGTLVTVSS</td><td>TOYNQKg ^ G ^</td>
<td> 148</td><td>BCMA-15</td><td>BC H1 39- C9-A4</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVTPGQPASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQIjIjIYRVS SGSGSGTDFTLKISRVEAEDVGVYYCFQGSTLPFTFGQGTKLEIK</td><td>T the</td>
<td> 149</td><td>BCMA-15</td><td>BC H1 39C9-A4</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRLEWIGAIYPGNSE VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGQGTLVSIVSGGQG GSDIVMQASQLSQLPNGQSQLSQLPNGSQLPGTYPIVQSQLSQLPNGCTYPGSQVYYCTRSSYYYDGSLFADWGQGTLVSIVSGQG</td><td>ΓΗΥΝ ^ ίβ ^ ΒΙ GSGGGGgGGG</td>
162
<img file="MX349396B_D0084.tif" />
<td></td><td></td><td></td><td></td><td></td><td>ΕΡεοεσεΘΤΟΓΤΕΚΙΒΕνΕΑΕϋνονΥΥΟΡΟΟΒΤΕΡΡΤΡΟΟατΚΕΕΙΚ</td>
<td> 150</td><td>BCMA-15HL x CD3 HL</td><td>BC H1 39C9-A4 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGR VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGQGTLVTVSSGGGGSGGGGSGGG σ3ϋΐνΜΤ0ΤΡΕ5Ε3νΤΡσ0ΡΑ3ΐε0Κ3303ΐνΗ3ΝσΝΤΥΕΥΝΥΕ0ΚΡσ0ΡΡ0ΕΕΙΥΡν3ΝΡΡ3θνΡΟ ρρεΘεσεστυρτΕκιερνΕΑΕυνσνγγοΡοσετΏΡΡΤΡσοστκΕΕίκεσσσσεΕνοΕνΕεσσαΕνορ GGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTA YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAAL TLS GVQP EDEAEYYCVLWYS NRWVFGGGTKLTVL <sup>1</sup></td>
<td> 151</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VH CDR1</td><td>aa</td><td>SYWIH</td>
<td> 152</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VH CDR2</td><td>aa</td><td>AIYPGNSDTHYNQKFQG</td>
<td> 153</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VH CDR3</td><td>aa</td><td>SSYYYDGSLFAD</td>
<td> 154</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VLCDR1</td><td>aa</td><td>KSSQSIVHSNGNTYLY</td>
<td> 155</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VL CDR2</td><td>aa</td><td>RVSNRFS</td>
<td> 156</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VL CDR3</td><td>aa</td><td>FQGSHLPFT</td>
<td> 157</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGR VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGQGTLVTVSS</td>
<td> 158</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVTPGQPASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYRVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYC FQGS HLP FTFGQGTKLEIK</td>
<td> 159</td><td>BCMA-16</td><td>BC H1 39C9-F12</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRLEWIGAIYPGNSDTHYNQKFQGR VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGOGTLVTVSSGGGGSGGG & SGGG GSDIVMTQTPLSLSVTPGQPASISCKSSQSI \ ^^^ 7HSNGNTYLYWYLQKPGQPPQL.LIY¿VSNR TO RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIK t.-S ________________________________________________________________________________________________________i_______<sup>></sup> SnrP *</td>
<td> 160</td><td>BCMA-16 HL x CD3 HL</td><td>BC H1 39C9-F12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQL · · EWIGAIYPGNSpTHYS§gK¡gR VTLTRDTSASTAYMELSSLRSEDSAVYYCTRSSYYYDGSLFADWGQGTLVTVSSGGGGSGtígCsÓeb VQSGAEVKKPGTSVKVSCKASGYTFTSYWIHWVKQAPGQRL GSDIVMTQTPLSLSVTPGQPASISCKSSQSIVHSNGNTYLYWYLQKPGQPPQLLIYpVSN Ílfe'Wfc ^) ^ & aWQP RFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHLPFTFGQGTKLEIKSGGGGSEVqLVES GGSLKLSC7kASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYZlDSVKDRqTISI ^^^ ÍA</td>
163
<td></td><td></td><td></td><td></td><td></td><td colspan="2">YLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEP SLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRFS APRGLGGTPFSGSI<sub>J</sub>LGGKAAL TLS GVQ PE DEΑΞYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 161</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 162</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGADHAIYADSVKG</td>
<td> 163</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 164</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNYLN</td>
<td> 165</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 166</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQYDISSYT</td>
<td> 167</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 168</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK</td>
<td> 169</td><td>BCMA-17</td><td>BC C3 33D7-E6</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK</td>
<td> 170</td><td>BCMA-17 HL x CD3 HL</td><td>BC C3 33D7-E6 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>Εν0ΕνΕ3σσαΕν0Ρσθ3ΕΕΕ5εΑΑ3σΕΤΕ3ΝΕΌΜΑΝνΕζ2ΑΡσκσΐ, νΗν33ΙΤΤαΑϋΗΑΙΥ FTISRDNAKNTLYIjQMDSIjRAEDTAVYYCVRHGYYDGYHLFDYWGQGTIjVTVSSGGGGSG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGV GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLV LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKN ΝΕκτΕΏΤΑνγγονΕΗαΝΡαΝδΥϊΕΥΧΑΥΝαοστΕντνεεασοσΕβσασΕοασσΞοτνντο ρσστντΕτοαΕΞτσΑντΕσΝΥΡΝΝνοοκΡΟΟΑΡΡαΕίσστκΓΕΑΡστΡΆΕΡΕσΕΕί, σσκΑ QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>ADSVKGR GGGSGGG PSRFSGS QPGGSLK TAYLQMN IPSLTVS j kLTLSen |</td>
<td> 171</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td>KUÍXJ -BU OI to go</td>
<td> 172</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VH CDR2</td><td>aa</td><td>SITTGADHAIYADSVKG</td><td>>> í Lj</td>
164
173
VH CDR3
BCMA-18
HGYYDGYHLFDY aa
BC C3 33D7-E6B1
<td> 174</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VL CDR1</td><td>aa</td><td>RASQGISNYLN</td><td></td><td></td>
<td> 175</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 176</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td><td></td><td></td>
<td> 177</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGL · VQPGGSL · RL · SC / \ ASGFTFSNFDMAWVRQAPGKGL · VWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYTVWGQSGTLV</td><td></td>
<td> 178</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td> 179</td><td>BCMA-18</td><td>BC C3 33D7-E6B1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td> 180</td><td>BCMA-18 HL X CD3 HL</td><td>BC C3 33D7-E6B1 HLxCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td> 165</td>
<td> 181</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td> 182</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VH CDR2</td><td>aa</td><td>SITTGADHAIYADSVKG</td><td> | 1 5</td><td rowspan="2"></td>
<td> 183</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td>- - STmn OF I - ™</td>
<td> 184</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VLCDR1</td><td>aa</td><td>RASQGISNYLN</td><td> * <sup>Λ </sup>0 MEX AMOf ΙΝΕΠΓ</td><td rowspan="2"></td>
<td> 185</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td>A 'CANO IEDad TBIAt</td>
<td> 186</td><td>BCMA-19</td><td>BC C3 33-</td><td>VLCDR3</td><td>aa</td><td>QQYDISSYT</td><td></td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td>i</td><td></td>
<td></td><td></td><td>F8-E6</td><td></td><td></td><td></td><td></td><td></td>
<td> 187</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGIjVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td></td>
<td> 188</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK</td><td></td>
<td> 189</td><td>BCMA-19</td><td>BC C3 33F8-E6</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK</td><td></td>
<td> 190</td><td>BCMA-19HL x CD3 HL</td><td>BC C3 33F8-E6 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR ftisrdnakntlylqmnsIjRAEdtavyycvrhgyydgyhlfdywgqgtlvtvssggggsggggsggg GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 191</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td> 192</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VH CDR2</td><td>aa</td><td>SITTGADHAIYADSVKG</td><td></td><td>σ></td>
<td> 193</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td><td></td>
<td> 194</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VLCDR1</td><td>aa</td><td>RASQGISNYLN</td><td></td><td></td>
<td> 195</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VLCDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 196</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td><td>5 u</td><td></td>
<td> 197</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VH</td><td>aa</td><td>ΕνθΕνΕ3θσαΕν0Ρσα3ΕΡΕ3σΑΑ8αΡΤΡεΝΡϋΜΑΝνΡ0ΑΡ6ΚσΕνΝν33ΙΤΤΟΑϋΗΑΙΥΑ FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHL FDYWGQGTLVTVS 3</td><td>JSVKG ^^ Yes!</td><td>m:</td>
<td> 198</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSR] GTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td>ω 0 w</td><td>HO<sub>t</sub> TO</td>
<td> 199</td><td>BCMA-20</td><td>BC C3 33F8-E6B1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTIS SLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td>
<td> 200</td><td>BCMA-20 HL x CD3 HL</td><td>BC C3 33F8-E6B1 HLxCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ρσστντΕτασΞεταΑντεσΝΥΡΝΜνοοκρσςΑΡΡσΕίσστκΕΕΑΡΟΤΡΑΗΓεσεΕΕσσκΑΑΕΤΒεσν QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 201</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 202</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGADHAIYADSVKG</td>
<td> 203</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 204</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASQGISNYLN</td>
<td> 205</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 206</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQYDISSYT</td>
<td> 207</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 208</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPS ^ FSGSGS GTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK I 2I</td>
<td> 209</td><td>BCMA-21</td><td>BC C3 33F9-E6</td><td>scFv</td><td>aa</td><td>EVQLVE S GGGLVQ PGGs LRLSCAASGFTFSNFDMAWVRQAPGKGLVWVS SITTGADHAIY ^ FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGd GSDIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVI GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIK</td><td>DS VKCB§ GGSCYES ^ SRF ^^ X □></td>
<td> 210</td><td>BCMA-21 HL x CD3 HL</td><td>BC C3 33F9-E6 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIY.? FTISRDNAKNTL · YL · QMDSLRSEDTAVYYCVRHGYYDGYHL · FDYWGQGTLVTVSSGGGGSGC</td><td>DSVKG & s GGSG ^ Í</td>
167
<img file="MX349396B_D0085.tif" />
<td></td><td></td><td>x CD3 HL</td><td>AC</td><td></td><td>GSDIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYDISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ΡσθΤνΤΕΤ0σ33ΤσΑνΤ3σΝΥΡΝΝν00ΚΡα0ΑΡΕσΕΐσσΤΚΡΕΑΡσΤΡΑΕΡ3α3ΕΕσθΚΑΑΕΤΕ3σν QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td rowspan="10"> 168</td>
<td> 211</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td>
<td> 212</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VH CDR2</td><td>aa</td><td>SITTGADHAIYAESVKG</td>
<td> 213</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td>
<td> 214</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VLCDR1</td><td>aa</td><td>RASQGISNYLN</td>
<td> 215</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td>
<td> 216</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td>
<td> 217</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYAESVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 218</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCMGQTI33YTFGQGTKLEIK</td>
<td> 219</td><td>BCMA-22</td><td>BC C3 33F9-E6B1-E</td><td>scFv</td><td>aa</td><td>EVQL VESGGGL · · · RLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYAESVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG VQPGGSL GSDIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td>
220
BCMA-22 HL x CD3 HL
<td>BC C3 33-</td><td>molecule</td><td></td>
<td>F9-E6B1-E</td><td>bispecific</td><td>aa</td>
<td>HL x CD3 HL</td><td>AC</td><td></td>
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGADHAIYAESVKGR ΡΤίεΕΟΝΑΚΝΤΕΥΕΟΜΟΒΕΚΒΕΟΤΑνΥΥΟνΕΗΟγΥΌσΥΗΕΡΟΥΝσοσΤΕντνεεσαοσΒίΙσσΟΞΟσΟ GSDIVRQAPGKGLVWVSSITTGADHAIYAESVKGR ΡΤίεΕΟΝΑΚΝΤΕΥΕΟΜΟΒΕΚΒΕΟΤΑνΥΥΟνΕΗΟγΥΌσΥΗΕΡΟΥΝσοσΤΕντνεεσαοσΒίΙσσΟΞΟσΟ GSDINQMTQSAPKPSLTISLSASVGTSNQWGFSQR
GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGL \ QPGG LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKhTAYL NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTC EPSL í · PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLí QPEDEAEYYCVLWYSNRWVFGGGTKLTVL
<img file="MX349396B_D0086.tif" />
<td></td><td> 221</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td></td><td> 222</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VH CDR2</td><td>aa</td><td>SITTGADHAIYADSVKG</td><td></td><td></td>
<td></td><td> 223</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td><td></td>
<td></td><td> 224</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VL CDR1</td><td>aa</td><td>RASQGISNYLN</td><td></td><td></td>
<td> 5</td><td> 225</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td></td><td> 226</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td><td></td><td></td>
<td></td><td> 227</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGADHAIYADSVKGR FTIΒΡϋΝΑΚΝΤΕΥΕΟΜΝΒΕΡΑΕΌΤΑνΥΥσνΡΗΟΥΥΟαΥΗΕΡΌΥνίΟΟσΤΏντνεS</td><td></td>
<td> 10</td><td> 228</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td></td><td> 229</td><td>BCMA-23</td><td>BC C3 33F10-E6B1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td>in</td>
<td> 15 20</td><td> 230</td><td>BCMA-23 HL x CD3 HL</td><td>BC C3 33F10-E6B1 HLxCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGADHAIYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVS SGGGGS GGGGSGGGGS QTWTQE PS LTVs PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKÁALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL 1 1 ni></td><td></td>
<td></td><td> 231</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VH CDR1</td><td>aa</td><td>DYYIN I</td><td>(ΙΛΗ IM</td><td></td>
<td></td><td> 232</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG |</td><td>Pl</td><td></td>
<td></td><td> 233</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV 1</td><td></td><td></td>
<td></td><td> 234</td><td>BCMA-24</td><td>BC B6 64-</td><td>VLCDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td><td></td><td></td>
<img file="MX349396B_D0087.tif" />
<td></td><td></td><td>H5-A4</td><td></td><td></td><td colspan="2"></td>
<td> 235</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 236</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VL CDR3</td><td>aa</td><td colspan="2">AETSHVPWT</td>
<td> 237</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVEQAPGQGLEWMGWIYFASGNSEYNQKFTGE VTMTEDTSSSTAYMELSSLESEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 238</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNEFSGVPDEF SGSGSGTDFTLKINEVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td>
<td> 239</td><td>BCMA-24</td><td>BC B6 64H5-A4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTEDTSSSTAYMELSSLESEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNEFSGVPDEF SGSGSGTDFTLKINEVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td>
<td> 240</td><td>BCMA-24 HL x CD3 HL</td><td>BC B6 64H5-A4 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVEQAPGQGLEWMGWIYFASGNSEYNQKFTGE VTMTEDTSSSTAYMELSSLESEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNEFSGVPDEF SGSGSGTDFTLKINEVEAEDVGVYYCAETSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVEQAPGKGLEWVAEIESKYNNYATYYADSVKDEFTISEDDSKNTAYL QMNNLKTEDTAVYYCVEHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPEGLIGGTKFLAPGTPAEFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNEWVFGGGTKLTVL</td>
<td> 241</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 242</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 243</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td>
<td> 244</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VLCDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td><td></td>
<td> 245</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VL CDR2</td><td>aa</td><td>KVSNEFS</td><td>2 HE</td>
<td> 246</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VL CDR3</td><td>aa</td><td>LTTSHVPWT</td><td>L 11 licanc FIEDAE STRIAÍ</td>
<td> 247</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VH</td><td>aa</td><td>QVQLVQS GAEVKKPGASVKVSCKASGYSFPDYYINWVEQAPGQGLEWMGWIYFASGNS E: VTMTEDTS SS TAYMELS SLESEDTAVYFCASLYDYDWYFDVWGQGTMVTVS S</td><td>nqkftg ^ ¡</td>
170
<td> 248</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>VL</td><td>aa</td><td colspan="2">ΟΐνΜΤ0ΤΡΕ3Ε5νΤΡ60ΡΑ3Ι3αΚ3303ΕνΗ3ΝΘΝΤΥΏΗ «ΥΕ0ΚΡΘ03Ρ0ΙιΙ.ΙΥΚν3ΝΕΕ3σνΡΟΕΡ SGSGSGTDFTLKINRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK</td>
<td> 249</td><td>BCMA-25</td><td>BC B6 64H5-H9</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKINRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK</td>
<td> 250</td><td>BCMA-25 HL x CD3 HL</td><td>BC B6 64H5-H9 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKINRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 251</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 252</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 253</td><td>BCMA-26</td><td>BC B6 65- B5-A4</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV</td>
<td> 254</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VLCDR1</td><td>aa</td><td colspan="2">KSSQSLVHSNGNTYLH</td>
<td> 255</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 256</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VL CDR3</td><td>aa</td><td>AETSHVPWT</td><td></td>
<td> 257</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYN VTMTRDT SSS TAYMELS 3 LR S EDTAVYF CAS LYDYDWYFDVWGQGTMVTVSS</td><td>Ω isa LU1I.WI</td>
<td> 258</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFS SGSGSGTDFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td><td>JVPD ^ gl ΗμΓ</td>
<td> 259</td><td>BCMA-26</td><td>BC B6 65B5-A4</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYN VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGG DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLiLIYKVSNRFS SGSGSGTDFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td><td>__> Í3) KFTGK GGGGET</td>
<td> 260</td><td>BCMA-26 HL x CD3 HL</td><td>BC B6 65B5-A4 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVS CKASGYS FPDYYINWVRQAPGQGLEWMGWIYFASGNS EYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF sgsgsgtdftlkisrveaedvgvyycaetshvpwtfgqgtkleiksggggsevqlvesggglvqpgg SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 261</td><td>BCMA-27</td><td>BC B6 65- B5-H9</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td>
<td> 262</td><td>BCMA-27</td><td>BC B6 65B5-H9</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td>
<td> 263</td><td>BCMA-27</td><td>BC B6 65- B5-H9</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td>
<td> 264</td><td>BCMA-27</td><td>BC B6 65B5-H9</td><td>VLCDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td>
<td> 265</td><td>BCMA-27</td><td>BC B6 65B5-H9</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td>
<td> 266</td><td>BCMA-27</td><td>BC B6 65B5-H9</td><td>VL CDR3</td><td>aa</td><td>LTTSHVPWT</td>
267
BCMA-27
BC B6 65B5-H9
VH aa
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTS S STAYMEL S SLRS EDTAVYFCASLYDYDWYFDVWGQGTMVTVS S
268
BCMA-27
BC B6 65B5-H9
VL aa
SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK
<td> 269</td><td>BCMA-27</td><td>BC B6 65B5-H9</td><td>scFv</td><td>aa</td>
<td> 270</td><td>BCMA-27 HL XCD3HL</td><td>BC B6 65B5-H9 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td>
DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRF SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEl ·! ST <VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGG3, DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRfβι SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIKSGGGGSEVQLVESGqG:
OH gv:
SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDISKNl | ^ Au4 = - <QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQT \ VTQEPSL TVS PGGTVTLTCGS STGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLCG
<img file="MX349396B_D0088.tif" />
<td></td><td></td><td></td><td></td><td></td><td>SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td><td></td>
<td> 271</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td><td></td><td></td>
<td> 272</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td><td></td>
<td> 273</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
<td> 274</td><td>BCMA-28</td><td>BC B6 65- H7-A4</td><td>VL CDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td><td></td><td></td>
<td> 275</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td></td><td></td>
<td> 276</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VL CDR3</td><td>aa</td><td>AETSHVPWT</td><td></td><td></td>
<td> 277</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td><td></td>
<td> 278</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td><td></td>
<td> 279</td><td>BCMA-28</td><td>BC B6 65H7-A4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td><td> 173</td>
<td> 280</td><td>BCMA-28 HL XCD3HL</td><td>BC B6 65H7-A4 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISREpSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQlLvTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLl | 3GKAAL 'l? SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL | S |</td><td></td>
<td> 281</td><td>BCMA-29</td><td>BC B6 65H7-H9</td><td>VH CDR1</td><td>aa</td><td>DYYIN 1</td><td>Π3Μ <XI</td><td></td>
<td> 282</td><td>BCMA-29</td><td>BC B6 65H7-H9</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td><td></td>
<td> 283</td><td>BCMA-29</td><td>BC B6 65H7-H9</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
Y
<td> 284</td><td>BCMA-29</td><td>BC B6 65H7-H9</td>
<td> 285</td><td>BCMA-29</td><td>BC B6 65H7-H9</td>
<td> 286</td><td>BCMA-29</td><td>BC B6 65H7-H9</td>
<td> 287</td><td>BCMA-29</td><td>BC B6 65H7-H9</td>
<td> 288</td><td>BCMA-29</td><td>BC B6 65- H7-H9</td>
<td> 289</td><td>BCMA-29</td><td>BC B6 65H7-H9</td>
VL CDR1
VL CDR2
VL CDR3
VH
VL scFv aa aa aa aa aa aa
KSSQSLVHSNGNTYLH
KVSNRFS
LTTSHVPWT
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS
DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYL · QKPGQSPQLL · IYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK
<td> 290</td><td>BCMA-29 HL x CD3 HL</td><td>BC B6 65H7-H9 HL x CD3 HL</td>
<td> 291</td><td>BCMA-30</td><td>BC B6 65H8-A4</td>
<td> 292</td><td>BCMA-30</td><td>BC B6 65- H8-A4</td>
<td> 293</td><td>BCMA-30</td><td>BC B6 65H8-A4</td>
<td> 294</td><td>BCMA-30</td><td>BC B6 65H8-A4</td>
<td> 295</td><td>BCMA-30</td><td>BC B6 65H8-A4</td>
<td> 296</td><td>BCMA-30</td><td>BC B6 65H8-A4</td>
<td> 297</td><td>BCMA-30</td><td>BC B6 65-</td>
bispecific molecule
VHCDR1
VH CDR2
VH CDR3
VLCDR1
VL CDR2
VL CDR3
VH
<img file="MX349396B_D0089.tif" />
aa aa aa aa aa aa aa
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQIjLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL Τν3ΡσστνΤΒΤσθ33ΤαΑνΤ3ΟΝΥΡΝΗν00ΚΡΟ0ΑΡΕΰΗΐσσΤΚΡΗΑΡατΡΑΚΡ3Ο3ΕΗΟΰΚΆΑΗΤΕ SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL
DYYIN
WIYFASGNSEYNQKFTG
LYDYDWYFDV
KSSQSLVHSNGNTYLH
KVSNRFS
AETSHVPWT
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSE fNQ
<img file="MX349396B_D0090.tif" />
WW
7^
<td></td><td></td><td>H8-A4</td><td></td><td></td><td colspan="2">VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 298</td><td>BCMA-30</td><td>BC B6 65H8-A4</td><td>VL</td><td>aa</td><td colspan="2">ΌΐνΜΤ0ΤΡΕ3ΕΞνΤΡσΕΡΑ3Ι3σΚ3303ΕνΗ3ΝΟΝΤΥΕΗΝΥΕ0ΚΡΟ (25Ρ0ΕΕΙΥΚν3ΝΕΡ3σνΡϋΕΡ SGSGSGADFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td>
<td> 299</td><td>BCMA-30</td><td>BC B6 65H8-A4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPL · SLSVTPGEPASISCKSSQSLVHSNGNTYL · HWYLQKPGQSPQL·LIYKVSNRFSGVPDRF SGSGSGADFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIK</td>
<td> 300</td><td>BCMA-30 HL xCD3HL</td><td>BC B6 65H8-A4 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS ΓίνΜτοτρΕεΕεντρσΕΡΑειεοκεεοεΕνΗεΝσΝΤΥΕΗΝΥΕοκρσοεροΒΕίΥκνεΝΕΡεσνΡΌΕΡ SGSGSGADFTLKISRVEAEDVGVYYCAETSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 301</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 302</td><td>BCMA-31</td><td>BC B6 65- H8-H9</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 303</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV</td>
<td> 304</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VL CDR1</td><td>aa</td><td colspan="2">KS S QSLVHSNGNTYLH</td>
<td> 305</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 306</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VL CDR3</td><td>aa</td><td colspan="2">LTTSHVPWT í i -k — J</td>
<td> 307</td><td>BCMA-31</td><td>BC B6 65- H8-H9</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNS VTMTRDT S SSTAYMEL SSLRS EDTAVYFCASLYDYDWYFDVWGQGTMVTVS S</td><td>EYNQI ^ qet ^</td>
<td> 308</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVTPGEPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVS1 SGSGSGADFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK</td><td>ω ΐνίΗχβΰΙ ivmiapH •) NV3Ü3> Id</td>
<td> 309</td><td>BCMA-31</td><td>BC B6 65H8-H9</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNE VTMTRDTS SS TAYMELS SLRS EDTAVYFCASLYDYDWYFDVWGQGTMVTVS SGGGGSC DIVMTKSQTQLSLSQLSQLSQLSNGlCVHSTPQLSLSQLSQLSNGLPVMTKSQTPLSLSQLSQLSNGL</td><td><sup>EYNQ</sup>* ^^ £ \ GGGSfflS ^ lj RFsqü ^ pio</td>
<td></td><td></td><td></td><td></td><td></td><td colspan="2">SGSGSGADFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIK</td>
<td> 310</td><td>BCMA-31 HL XCD3HL</td><td>BC B6 65H8-H9 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPL · SL · VHSNGNTYL SVTPGEPASISCKSSQSL · · · QKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGADFTLKISRVEAEDVGVYYCLTTSHVPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG Hwyl SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 311</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VH CDR1</td><td>aa</td><td colspan="2">NHIIH</td>
<td> 312</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VH CDR2</td><td>aa</td><td colspan="2">YINPYPGYHAYNEKFQG</td>
<td> 313</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYYRDTDVLDY</td>
<td> 314</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VL CDR1</td><td>aa</td><td colspan="2">QASQDISNYLN</td>
<td> 315</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHT</td>
<td> 316</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQGNTLPWT</td>
<td> 317</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYHAYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSS</td>
<td> 318</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>VL</td><td>aha</td><td colspan="2">DIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGSGS GTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 319</td><td>BCMA-32</td><td>BC A7 27A6-G7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYHAYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHtGVPSREFlGS, GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK I 1 η -1 U—. j</td>
<td> 320</td><td>BCMA-32 HL XCD3HL</td><td>BC A7 27A6-G7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYI ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGYGCGPSYQMTNSQTCDLPGCPSYQMTNSQTCDLPGCPSVYQMTNSQTCDVLDKPSVYQMTNSQTCDLPGCPSYQMTNSQTCDLPGCPSYQMTNSQRL<sup>r </sup>οεστοΡτρτιεεΕΟΟΕΟίΑΤΥΥσοοσΝΤΓΡκτρσοατκνΕίκεοσοσεΕνουνΕεσσί L8CAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYAD8VKDRFTISRDD</td><td>one SGGCJ ^^ 'GVP ^ BS ^ © IKNTAY ^ P ^</td>
176 'Ό.
NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS
<td></td><td></td><td></td><td></td><td></td><td>pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td rowspan="10"> 177</td>
<td> 321</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VH CDR1</td><td>aa</td><td>NHIIH</td>
<td> 322</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VH CDR2</td><td>aa</td><td>YINPYDGWGDYNEKFQG</td>
<td> 323</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VH CDR3</td><td>aa</td><td>DGYYRDADVLDY</td>
<td> 324</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VLCDR1</td><td>aa</td><td>QASQDISNYLN</td>
<td> 325</td><td>BCMA-33</td><td>BC A7 27- A6-H11</td><td>VL CDR2</td><td>aa</td><td>YTSRLHT</td>
<td> 326</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td>
<td> 327</td><td>BCMA-33</td><td>BC A7 27A6-H11</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSS</td>
<td> 328</td><td>BCMA-33</td><td>BC A7 27- A6-H11</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGSGS GTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 329</td><td>BCMA-33</td><td>BC A7 27- A6-H11</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGS GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSGGGGSWGQGTLVTVSGGGGSWGQGTLVTVSGGGGS
<td> 330</td><td>BCMA-33 HL x CD3 HL</td><td>BC A7 27A6-H11 HL x CD3 HL</td>
<td> 331</td><td>BCMA-34</td><td>BC A7 27C4-G7</td>
<td> 332</td><td>BCMA-34</td><td>BC A7 27C4-G7</td>
bispecific molecule aa
VH CDR1 aa
VH CDR2 aa
GSDIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTG 'GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGL' LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSK nlktedtavyycvrhgnfgnsyisywaywgqgtlvtvssggggsggggsggggsqtwti PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGK QPEDEAEYYCVLWYSNRWVFGGGTKLTVL
NHIIH
YINPYPGYHAYNEKFQG 'SRFSG £> PGGSLÍ' AYL
<img file="MX349396B_D0091.tif" />
.LTL
<td> 333</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYYRDTDVLDY</td>
<td> 334</td><td>BCMA-34</td><td>BC A7 27- C4-G7</td><td>VLCDR1</td><td>aa</td><td colspan="2">QASQDISNYLN</td>
<td> 335</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHT</td>
<td> 336</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQGNTLPWT</td>
<td> 337</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYHAYNEKFQGR ATMT SDTS TSTVYMELS SLRSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVS S</td>
<td> 338</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>VL</td><td>aa</td><td colspan="2">diqmtqspsslsasvgdrvtitcqasqdisnylnwyqqkpgkapklliyytsrlhtgvpsrfsgsgs GTDFTFTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 339</td><td>BCMA-34</td><td>BC A7 27C4-G7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYHAYNEKFQGR atmtsdtststvymelsslrsedtavyyc ardgyyrdtdvldywgqgtlvtvssggggsggggsggg gsdiqmtqspsslsasvgdrvtitcqasqdisnylnwyqqkpgkapklliyytsrlhtgvpsrfsgs GSGTDFTFTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 340</td><td>BCMA-34 HL XCD3 HL</td><td>BC A7 27C4-G7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYPGYHAYNEKFQGR ATMTSDTS TSTVYMELS SLRSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSS GGGGSGGGG S GGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGS GSGTDFTFTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 341</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VH CDR1</td><td>aa</td><td colspan="2">NHIIH</td>
<td> 342</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VH CDR2</td><td>aa</td><td>YINPYDGWGDYNEKFQG</td><td> £ 1=</td>
<td> 343</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VH CDR3</td><td>aa</td><td>DGYYRDADVLDY</td><td>3 L</td>
<td> 344</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VL CDR1</td><td>aa</td><td>QASQDISNYLN</td><td>l FROP1 INDUS</td>
<td> 345</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VL CDR2</td><td>aa</td><td>YTSRLHT</td><td>IVIMJ CIVQ3 owv: T</td>
<td> 346</td><td>BCMA-35</td><td>BC A7 27-</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td><td></td>
178
<td></td><td></td><td>C4-H11</td><td></td><td></td><td colspan="2"></td>
<td> 347</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSS</td>
<td> 348</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGSGS GTDFTFTISS LEPEDIATYYCQQGNTLPWT FGQGTKVEIK</td>
<td> 349</td><td>BCMA-35</td><td>BC A7 27C4-H11</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGS GSGTDFTFTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 350</td><td>BCMA-35 HL x CD3 HL</td><td>BC A7 27C4-H11 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYTFTNHIIHWVRQAPGQGLEWMGYINPYDGWGDYNEKFQGR ATMTSDTSTSTVYMELSSLRSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGS gsgtdftftisslepediatyycqqgntlpwtfgqgtkveiksggggsevqlvesggglvqpggslk LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 351</td><td>BCMA-36</td><td>BC A7 15- H2-G7</td><td>VH CDR1</td><td>aa</td><td colspan="2">NHIIH</td>
<td> 352</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VH CDR2</td><td>aa</td><td colspan="2">YINPYPGYHAYNQKFQG</td>
<td> 353</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYYRDTDVLDY</td>
<td> 354</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VL CDR1</td><td>aa</td><td colspan="2">QASQDISNYLN</td>
<td> 355</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VL CDR2</td><td>aa</td><td>YTSRLHT</td><td></td>
<td> 356</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td><td>2 h</td>
<td> 357</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VH</td><td>aa</td><td>QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYPGYHA VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSS</td><td>rNQKFSaiE -lili</td>
<td> 358</td><td>BCMA-36</td><td>BC A7 15H2-G7</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLLIYYTSRLHTGVP, GTDYSFTISSLQPEDIATYYCQQGNTLPWTFGQGTKVEIK</td><td>! RFS <5lfÍ ^ _</td>
179
QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYPGYHAYNQKFQGR
<td> 359</td><td>BCMA-36</td><td>BC A7 15- H2-G7</td><td>scFv</td><td>aa</td><td colspan="2">VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGGGSGGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLEDGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLEDGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLEDLFATIYVQKPGRAPKLEDLFTSIYVQKPGRAPKLEDLFTSIYVQKPGRAPKLEDLFTSGFSGFSP</td><td></td>
<td> 360</td><td>BCMA-36 HL x CD3 HL</td><td>BC A7 15H2-G7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYPGYHAYNQKFQGR VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLLIYYTSRLHTGVPSRFSGS GSGTDYSFTISSLQPEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 361</td><td>BCMA-37</td><td>BC A7 15- H2-H11</td><td>VH CDR1</td><td>aa</td><td>NHIIH</td><td></td><td></td>
<td> 362</td><td>BCMA-37</td><td>BC A7 15- H2-H11</td><td>VH CDR2</td><td>aa</td><td>YINPYDGWGDYNQKFQG</td><td></td><td></td>
<td> 363</td><td>BCMA-37</td><td>BC A7 15H2-H11</td><td>VH CDR3</td><td>aa</td><td>DGYYRDADVLDY</td><td></td><td></td>
<td> 364</td><td>BCMA-37</td><td>BC A7 15- H2-H11</td><td>VL CDR1</td><td>aa</td><td>QASQDISNYLN</td><td></td><td rowspan="2"> 180</td>
<td> 365</td><td>BCMA-37</td><td>BC A7 15- H2-H11</td><td>VL CDR2</td><td>aa</td><td>YTSRLHT</td><td></td>
<td> 366</td><td>BCMA-37</td><td>BC A7 15H2-H11</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td><td></td><td></td>
<td> 367</td><td>BCMA-37</td><td>BC A7 15H2-H11</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYDGWGDYNQKFQGR VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSS</td><td></td>
<td> 368</td><td>BCMA-37</td><td>BC A7 15- H2-H11</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLLIYYTSRLHTGVPS GTDYSFTISS LQPEDIATYYCQQGNTLPWT FGQGTKVEIK</td><td>RFSGSGS</td><td>Ber |</td>
<td> 369</td><td>BCMA-37</td><td>BC A7 15H2-H11</td><td>scFv</td><td>aa</td><td>QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYDGWGDY VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSSGGGGSG GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLLIYYTSRLHTGV GSGTDYSFTISSLQPEDIATYYCQQGNTLPWTFGQGTKVEIK</td><td>IV we hm fe «Otó OO w</td><td> 03^</td>
<td> 370</td><td>BCMA-37 HL x CD3 HL</td><td>BC A7 15- H2-H11 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAKVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWMGYINPYDGWGDY VTMTRDKSTSTVYMELSSLTSEDTAVYYCARDGYYRDADVLDYWGQGTLVTVSSGGGGSG</td><td>ÜQKFQGB-- 3GGS ^^</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td></td><td></td><td>xCD3HL</td><td>AC</td><td></td><td colspan="2">GSDIQMTQSPSSLSASVGDRVTITCQASQDISNYLNWYQQKPGRAPKLLIYYTSRLHTGVPSRFSGS GSGTDYSFTISSLQPEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td rowspan="11"><sup>181</sup></td>
<td> 371</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>VH CDR1</td><td>aa</td><td colspan="2">NHIIH</td>
<td> 372</td><td>BCMA-38</td><td>BC A7 15- H8-G7</td><td>VH CDR2</td><td>aa</td><td colspan="2">YINPYPGYHAYNQKFQG</td>
<td> 373</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYYRDTDVLDY</td>
<td> 374</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>VL CDR1</td><td>aa</td><td colspan="2">QASQDISNYLN</td>
<td> 375</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHT</td>
<td> 376</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQGNTLPWT</td>
<td> 377</td><td>BCMA-38</td><td>BC A7 15- H8-G7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWIGYINPYPGYHAYNQKFQGK VTMTRDTS TS TVYMEL SS LT SEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVS S</td>
<td> 378</td><td>BCMA-38</td><td>BC A7 15- H8-G7</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGSGS GTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 379</td><td>BCMA-38</td><td>BC A7 15H8-G7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWIGYINPYPGYHAYNQKFQGK VTMTRDTSTSTVYMELSSLTSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGVPSRFSGS GSGTDFTFTIS SLQQEDTATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 380</td><td>BCMA-38 HL x CD3 HL</td><td>BC A7 15H8-G7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWIGYINPYPGYHAY VTMTRDTSTSTVYMELSSLTSEDTAVYYCARDGYYRDTDVLDYWGQGTLVTVSSGGGGSG GSDIQMTQSPSSLSASLGDRVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSRLHTGV GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLV LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKK NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTC PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKS QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>STQKFQGK 3GGSGG§I psrfsbI * DPGGsÉi ^ rAYLgí ^ L EPSláf ^ altlS ^ · ^</td>
<td> 381</td><td>BCMA-39</td><td>BC A7 15- H8-H11</td><td>VH CDR1</td><td>aa</td><td>NHIIH</td>
<td> 382</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VH CDR2</td><td>aa</td><td>YINPYDGWGDYNQKFQG</td>
<td> 383</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VH CDR3</td><td>aa</td><td>DGYYEDADVLDY</td>
<td> 384</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VL CDR1</td><td>aa</td><td>QASQDISNYLN</td>
<td> 385</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VL CDR2</td><td>aa</td><td>YTSRLHT</td>
<td> 386</td><td>BCMA-39</td><td>BC A7 15- H8-H11</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td>
<td> 387</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVIKPGASVKVSCKASGYTFTNHIIHWVRQKPGQGLEWIGYINPYDGWGDYNQKFQGK VTMTEDTSTSTVYMELSSLTSEDTAVYYCAEDGYYEDADVLDYWGQGTLVTVSS</td>
<td> 388</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASLGDEVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSELHTGVPSEFSGSGS GTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 389</td><td>BCMA-39</td><td>BC A7 15H8-H11</td><td>scFv</td><td>aa</td><td>QVQLVQ3GAEVIKPGASVKVSCKASGYTFTNHIIHWVEQKPGQGLEWIGYINPYDGWGDYNQKFQGK VTMTEDTSTSTVYMELSSLTSEDTAVYYCAEDGYYEDADVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDEVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSELHTGVPSEFSGS GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVETK</td>
<td> 390</td><td>BCMA-39 HL x CD3 HL</td><td>BC A7 15- H8-H11 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVIKPGASVKVSCKASGYTFTNHIIHWVEQKPGQGLEWIGYINPYDGWGDYNQKFQGK VTMTEDTSTSTVYMELSSLTSEDTAVYYCAEDGYYEDADVLDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDEVTITCQASQDISNYLNWYQQKPGKAPKLLIYYTSELHTGVPSEFSGS GSGTDFTFTISSLQQEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVEQAPGKGLEWVAEIESKYNNYATYYADSVKDEFTISEDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPeLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPEGLIGGTKFLAPGTPARFSGSLLGGKAAIITLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL: I! 1 34</td>
<td> 391</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VH CDR1</td><td>aa</td><td>DYYIN 1</td>
<td> 392</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VH CDR2</td><td>aa</td><td>1 sis WIYFASGNSEYNQKFTG i</td>
<td> 393</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VH CDR3</td><td>aa</td><td>i ^ 55 LYDYDWYFDV 1 _</td>
<td> 394</td><td>BCMA-40</td><td>BC 7A4 96-</td><td>VLCDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH í ΐΙτΛ __________________________________________________________________________________i ag '</td>
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<img file="MX349396B_D0092.tif" />
<img file="MX349396B_D0093.tif" />
<td></td><td></td><td>D4-A12</td><td></td><td></td><td colspan="2"></td>
<td> 395</td><td>BCMA-40</td><td>BC 7A4 96- D4-A12</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 396</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VL CDR3</td><td>aa</td><td colspan="2">SQSSTAPWT</td>
<td> 397</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 398</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>VL</td><td>aa</td><td colspan="2">ΌΐνΜΤ0ΤΡΕΞΕΡνΤΕσ0ΡΑ3Ι3σΚ3303ΕνΗ3ΝσΝΤΥΕΗΜΥΕζ2ΚΡσ0ΞΡ0ΕΕΙΥΚν5ΝΡΡ3σνΡϋΕΡ SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK</td>
<td> 399</td><td>BCMA-40</td><td>BC 7A4 96D4-A12</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK</td>
<td> 400</td><td>BCMA-40 HL x CD3 HL</td><td>BC 7A4 96D4-A12HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYIjHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 401</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 402</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 403</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV '-। (</td>
<td> 404</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VL CDR1</td><td>aa</td><td colspan="2">KSSQSLVHSNGNTYLH i 23 ^ * . . .___________________________</td>
<td> 405</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td>z- JI * ' 0? ^</td>
<td> 406</td><td>BCMA-41</td><td>BC 7A4 96- D4-D7</td><td>VL CDR3</td><td>aa</td><td>SQSSIYPWT</td><td>»And> <sup>v</sup></td>
<td> 407</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGK VTMTRDTSIS TAYMELS SLRS EDTAVYFCASLYDYDWYFDVWGQGTMVTVS S</td><td>SEYNC ^^ fa</td>
<td> 408</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIK</td>
<td> 409</td><td>BCMA-41</td><td>BC 7A4 96D4-D7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQS SIYPWTFGQGTKLEIK</td>
<td> 410</td><td>BCMA-41 HL XCD3HL</td><td>BC 7A4 96D4-D7 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 411</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 412</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 413</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV</td>
<td> 414</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VL CDR1</td><td>aa</td><td colspan="2">KSSQSLVHSNGNTYLH</td>
<td> 415</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 416</td><td>BCMA-42</td><td>BC 7A4 96- D4-E7</td><td>VL CDR3</td><td>aa</td><td>SQSTYPEFT</td><td></td>
<td> 417</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASG1 VTMTRDT SISTAYMELS SLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td><td>SEYNOI^TG^ —</td>
<td> 418</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVÍ SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td><td>NRFSd^^S·</td>
<td> 419</td><td>BCMA-42</td><td>BC 7A4 96D4-E7</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGl VTMTRDTSIS TAYMELS SLR SEDTAVYFCASLYDYDWYFDVWGQGTMVTVS SGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVS SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td><td>sEYú¡dmes$ GGGGSGG^QS NRFSi^to®^</td>
184
<td> 420</td><td>BCMA-42 HL x CD3 HL</td><td>BC 7A4 96D4-E7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLPVTLGQPASISCKSSQSLjVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF δΰεαεατϋΕΤΕΚιεΗνΕΑΕϋνονγγσβοετγρΕΡΤΡσοστκΕΕίκεσσσσεΕνοΕνΕΞοσσΒνοροο SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 421</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td><td></td><td></td>
<td> 422</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td><td></td>
<td> 423</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
<td> 424</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VL CDR1</td><td>aa</td><td>KS S QS LVHSNGNTYLH</td><td></td><td></td>
<td> 425</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td></td><td></td>
<td> 426</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VL CDR3</td><td>aa</td><td>SQSSTAPWT</td><td></td><td></td>
<td> 427</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td><td></td>
<td> 428</td><td>BCMA-43</td><td>BC 7A4 96F4-A12</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK</td><td></td>
<td> 429</td><td>BCMA-43</td><td>BC 7A4 96- F4-A12</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNiFSGVPDRF^ SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK | |</td><td> 1</td>
<td> 430</td><td>BCMA-43 HL x CD3 HL</td><td>BC 7A4 96F4-A12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNsá VTMTRDTSIS TAYMELS S LRSEDTAVYFCAS LYDYDWYFDVWGQGTMVTVS SGGGGSGC DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLIiIYKVSNr 8σ3σ36ΤϋΡΤΕΚΙ3ΕνΕΑΕθνθνΥΥΟ3033ΤΑΡΝΤΡΘ0σΤΚΕΕΙΚ3θσΘΘ3Εν0ΕνΕ30 SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYY7WSVKDRFTISRL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQT TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLL</td><td>YNQKjsés^ GGSG^GfcS FSGVWpA JSKNTAYfeK</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td> ·.· · ·</td><td></td>
185
<td></td><td></td><td></td><td></td><td></td><td></td><td>SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td><td></td>
<td></td><td> 431</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td><td></td><td></td>
<td></td><td> 432</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td><td></td>
<td></td><td> 433</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
<td rowspan="2"> 5</td><td> 434</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VL CDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td><td></td><td></td>
<td> 435</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td></td><td></td>
<td></td><td> 436</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VL CDR3</td><td>aa</td><td>SQSSIYPWT</td><td></td><td></td>
<td></td><td> 437</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSIS TAYMELS SLRS EDTAVYFCAS LYDYDWYFDVWGQGTMVTVS S</td><td></td>
<td> 10</td><td> 438</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIK</td><td></td>
<td rowspan="2"> 15 20</td><td> 439</td><td>BCMA-44</td><td>BC 7A4 96F4-D7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS divmtqtplslsvtpgqpas:i:sckssqslvhsngntylhwylqkpgqspqlij:i:ykvsnrfsgvpdrf SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIK</td><td> 186</td>
<td> 440</td><td>BCMA-44 HL x CD3 HL</td><td>BC 7A4 96F4-D7 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNC VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGE DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSC SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIKSGGGGSEVQLVESGGG: SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDS QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTW TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGl SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>5KFTGR >GGGGS iVPDRF jVQPGG cntayl! ’QEPSB: aalt£¿ 533 =95</td><td rowspan="2">IMPI</td>
<td></td><td> 441</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td><td>IEDAO TRIAL</td>
<td></td><td> 442</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td><td>Mi</td>
<td></td><td> 443</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
444
BCMA-45
VL CDR1
KSSQSLVHSNGNTYLH aa
BC 7A4 96F4-E7
<td> 445</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td><td rowspan="10">«i 187</td>
<td> 446</td><td>BCMA-45</td><td>BC 7A4 96- F4-E7</td><td>VL CDR3</td><td>aa</td><td colspan="2">SQSTYPEFT</td>
<td> 447</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 448</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td>
<td> 449</td><td>BCMA-45</td><td>BC 7A4 96F4-E7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td>
<td> 450</td><td>BCMA-45 HL x CD3 HL</td><td>BC 7A4 96F4-E7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSISTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 451</td><td>BCMA-46</td><td>BC 7A4 96G2-A12</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 452</td><td>BCMA-46</td><td>BC 7A4 96G2-A12</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNEKFTG</td>
<td rowspan="2"> 453</td><td rowspan="2">BCMA-46</td><td rowspan="2">BC 7A4 96G2-A12</td><td rowspan="2">VH CDR3</td><td rowspan="2">aa</td><td colspan="2">LYDYDWYFDV ,</td>
<td></td><td></td>
<td> 454</td><td>BCMA-46</td><td>BC 7A4 96G2-A12</td><td>VLCDR1</td><td>aa</td><td>KSSQSLVHSNGNTYLH</td><td>_____ni</td><td></td>
<td> 455</td><td>BCMA-46</td><td>BC 7A4 96G2-A12</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td>VI UTO* f LAFI INi</td><td></td>
<td> 456</td><td>BCMA-46</td><td>BC 7A4 96G2-A12</td><td>VL CDR3</td><td>aa</td><td>SQSSTAPWT</td><td>gs?.</td><td>í</td>
<td> 457</td><td>BCMA-46</td><td>BC 7A4 96-</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNS]</td><td>YNEKFTQ^</td><td> 1</td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
458
BCMA-46
459
BCMA-46
G2-A12
BC 7A4 96G2-A12
VL aa
VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS
BC 7A4 96G2-A12 scFv aa
460
461
462
463
464
465
466
467
468
469
BCMA-46 HL X CD3 HL
BC 7A4 96G2-A12 HL xCD3 HL bispecific molecule aa
DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNEKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIK
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNEKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSTAPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGG'TKFLAPGTPARFSGSLLiGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BCMA-47
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
BC 7A4 96G2-D7
VH CDR1 aa DYYIN
VH CDR2
VH CDR3
VL CDR1
VL CDR2
VL CDR3
VH
VL scFv aa aa aa aa aa aa aa
<img file="MX349396B_D0094.tif" />
WIYFAS GNSEYNE KFTG
LYDYDWYFDV
KSSQSLVHSNGNTYLH
KVSNRFS
SQSSIYPWT
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEY SIEKFTGR
VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS
ΟίνΜΤΟΤΡΒΞηενεΒσΟΡΑείΞαΚΞΞΟεΕνΗδΝαΝΤΥΏΗΝΥΓΟΚΡσοεΡΟΓ,ΕΙΥΚνΞΝΕΡ SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIK
SGVPgi
QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEY VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGG DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRF
4EKFÍ&^ 3SGGGG 3GVP
00
IMPI
<img file="MX349396B_D0095.tif" />
<td></td><td></td><td></td><td></td><td></td><td colspan="2">SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIK</td>
<td> 470</td><td>BCMA-47 HL X CD3 HL</td><td>BC 7A4 96G2-D7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNEKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSSIYPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 471</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 472</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNEKFTG</td>
<td> 473</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV</td>
<td> 474</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VL CDR1</td><td>aa</td><td colspan="2">KS S QSLVHSNGNTYLH</td>
<td> 475</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 476</td><td>BCMA-48</td><td>BC 7A4 96- G2-E7</td><td>VL CDR3</td><td>aa</td><td colspan="2">SQSTYPEFT</td>
<td> 477</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNEKFTGR VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 478</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td>
<td> 479</td><td>BCMA-48</td><td>BC 7A4 96G2-E7</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYI VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGG( DIVMTQTPLSLSVSLGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRF. SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIK</td><td>\TEKFTGR 3SGGGGS IGVPDRF</td>
<td> 480</td><td>BCMA-48 HL x CD3 HL</td><td>BC 7A4 96G2-E7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEY VTMTRDTSSSTAYMELSSLRSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGG DIVMTQTPLSL·SVSL·GQPASISCKSSQSLVHSNGNTYL·HWYLQKPGQSPQLL·IYKVSNRF SGSGSGTDFTLKISRVEAEDVGVYYCSQSTYPEFTFGQGTKLEIKSGGGGSEVQLVESGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDD</td><td>IEKFT<^ ISGGClg » jgvpm| i ILVQfSí . ;knt¿-?£ '</td>
189
<img file="MX349396B_D0096.tif" />
<td></td><td></td><td></td><td></td><td></td><td colspan="2">QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVS PGGTVTLT CG S STGAVT SGNY PNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 481</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td> 482</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VH CDR2</td><td>aa</td><td colspan="2">WIYFASGNSEYNQKFTG</td>
<td> 483</td><td>BCMA-49</td><td>BC 7A4 OTAS-A^</td><td>VH CDR3</td><td>aa</td><td colspan="2">LYDYDWYFDV</td>
<td> 484</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VL CDR1</td><td>aa</td><td colspan="2">KSSQSLVHSNGNTYLH</td>
<td> 485</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 486</td><td>BCMA-49</td><td>BC 7A4 OTAS-A^</td><td>VLCDR3</td><td>aa</td><td colspan="2">SQSSTAPWT</td>
<td> 487</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELS SLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVS S</td>
<td> 488</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>VL</td><td>aa</td><td colspan="2">DIVMTQTPLSIjSVTPGQPASISCKSSQSLVHSNGNTYIjHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSSTAPWTFGQGTKLEIK</td>
<td> 489</td><td>BCMA-49</td><td>BC 7A4 97A3-A12</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS ϋΐνΜΤ0ΤΡΕ3Ε2νΤΡσ0ΡΑεΐ3αΚ3303ΕνΗ3ΝσΝΤΥΕΗΚΥΕ0ΚΡσ03Ρ0ΕΕΙΥΚν3ΝΡΡ3θνΡΟΡΡ SGSGSGTDFTLKISRVEAEDVGIYYCSQSSTAPWTFGQGTKLEIK</td>
<td> 490</td><td>BCMA-49 HL x CD3 HL</td><td>BC 7A4 97A3-A12 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYS FPDYYINWVRQAPGQGLEWMGWIYFASGNS EYN( VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGG. ΟΐνΜΤ0ΤΡΕ3ΕενΤΡΟ0ΡΑ3Ι3ΟΚ3303ΕνΗ3ΝΟΝΤΥΕΗΝΥΕ0ΚΡΟ03Ρ0ΕΕΙΥΚν3ΝΡΡ3( SGSGSGTDFTLKISRVEAEDVGIYYCSQSSTAPWTFGQGTKLEIKSGGGGSEVQLVESGGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDS QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTW TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGG SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>2KFTGR 3GGGGS 3VPDRF ..VQPGG CNTAYL5 7QEPSL: CAALTg:</td>
<td> 491</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VH CDR1</td><td>aa</td><td>DYYIN</td><td>UCANl HEDAÍ ÍSTRIAÍ</td>
<td> 492</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNQKFTG</td><td></td>
IMPI
<img file="MX349396B_D0097.tif" />
493
VH CDR3
BCMA-50
LYDYDWYFDV aa
BC 7A4 97A3-D7
<td> 494</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VLCDR1</td><td>aa</td><td colspan="2">KSSQSLVHSNGNTYLH</td><td rowspan="10"><sup>191</sup> 1</td>
<td> 495</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VL CDR2</td><td>aa</td><td colspan="2">KVSNRFS</td>
<td> 496</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VL CDR3</td><td>aa</td><td colspan="2">SQSSIYPWT</td>
<td> 497</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 498</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>VL</td><td>aa</td><td colspan="2">divmtqtplslsvtpgqpasisckssqslvhsngntylhwylqkpgqspqlliykvsnrfsgvpdrf SGSGSGTDFTLKISRVEAEDVGIYYCSQSSIYPWTFGQGTKLEIK</td>
<td> 499</td><td>BCMA-50</td><td>BC 7A4 97A3-D7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSSIYPWTFGQGTKLEIK</td>
<td> 500</td><td>BCMA-50 HL x CD3 HL</td><td>BC 7A4 97- A3-D7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSSIYPWTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 501</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VH CDR1</td><td>aa</td><td colspan="2">DYYIN</td>
<td rowspan="2"> 502</td><td rowspan="2">BCMA-51</td><td rowspan="2">BC 7A4 97A3-E7</td><td rowspan="2">VH CDR2</td><td rowspan="2">aa</td><td colspan="2"></td>
<td>WIYFASGNSEYNQKFTG</td><td>x |</td>
<td> 503</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td>J</td><td></td>
<td> 504</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VL CDR1</td><td>aa</td><td>KS S QSLVHSNGNTYLH</td><td> 2?*</td><td rowspan="3"></td>
<td> 505</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td>Canc lEPAl* TRíAl</td>
<td> 506</td><td>BCMA-51</td><td>BC 7A4 97-</td><td>VL CDR3</td><td>aa</td><td>SQSTYPEFT</td><td></td>
<td colspan="6"></td><td> 1</td><td></td>
<td></td><td></td><td>A3-E7</td><td></td><td></td><td></td>
<td> 507</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VH</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSS</td>
<td> 508</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>VL</td><td>aa</td><td>DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSTYPEFTFGQGTKLEIK</td>
<td> 509</td><td>BCMA-51</td><td>BC 7A4 97A3-E7</td><td>scFv</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSTYPEFTFGQGTKLEIK</td>
<td> 510</td><td>BCMA-51 HL xCD3HL</td><td>BC 7A4 97A3-E7 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGAEVKKPGASVKVSCKASGYSFPDYYINWVRQAPGQGLEWMGWIYFASGNSEYNQKFTGR VTMTRDTSINTAYMELSSLTSEDTAVYFCASLYDYDWYFDVWGQGTMVTVSSGGGGSGGGGSGGGGS DIVMTQTPLSLSVTPGQPASISCKSSQSLVHSNGNTYLHWYLQKPGQSPQLLIYKVSNRFSGVPDRF SGSGSGTDFTLKISRVEAEDVGIYYCSQSTYPEFTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGG SLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYL QMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSL TVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTL SGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 511</td><td>BCMA-52</td><td>BC E11 19F11-F8</td><td>VH CDR1</td><td>aa</td><td>NAWMD</td>
<td> 512</td><td>BCMA-52</td><td>BCE11 19F11-F8</td><td>VH CDR2</td><td>aa</td><td>QITAKSNNYATYYAE PVKG</td>
<td> 513</td><td>BCMA-52</td><td>BC E11 19F11-F8</td><td>VH CDR3</td><td>aa</td><td>DGYH</td>
<td> 514</td><td>BCMA-52</td><td>BC E11 19F11-F8</td><td>VL CDR1</td><td>aa</td><td>RASEDIRNGLA</td>
<td> 515</td><td>BCMA-52</td><td>BC E11 19- F11-F8</td><td>VL CDR2</td><td>aa</td><td>NANSLHT ¡ a h</td>
<td> 516</td><td>BCMA-52</td><td>BC E11 19- F11-F8</td><td>VL CDR3</td><td>aa</td><td>j EDTSKYPYT i -g</td>
<td> 517</td><td>BCMA-52</td><td>BC E11 19F11-F8</td><td>VH</td><td>aa</td><td>Εν0ΕνΕ3ασαΕνΚΡ0Ε8ΕΡΒ30ΑΑ3αΡΤΕ3ΝΑΝΜϋΝνΡ0ΑΡσΚΡΕΕΝνΑ0ΙΤΑΚ3ΝΝΥΑΐγΥΑΕ|§Ι&η GRFTISRDDSKNTLYLQMNSLKTEDTAVYYCTDDGYHWGQGTLVTVSS < !</td>
<td> 518</td><td>BCMA-52</td><td>BC E11 19- F11-F8</td><td>VL</td><td>aa</td><td>AIQMTQSPSSLSASVGETVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVP$RFSGS^ GTEFTLKISSLQPEDEATYYCEDTSKYPYTFGQGTKLEIK i</td>
<td> 519</td><td>BCMA-52</td><td>BC E11 19F11-F8</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWVAQITAKSNNYATYYAEPVK GRFTISRDDSKNTLYLQMNSLKTEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGETVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTEF TLKISSLQPEDEATYYCEDTSKYPYTFGQGTKLEIK</td>
<td> 520</td><td>BCMA-52 HL x CD3 HL</td><td>BC E11 19F11-F8HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWVAQITAKSNNYATYYAEPVK GRFTISRDDSKNTLYLQMNSLKTEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGETVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTEF TLKISSLQPEDEATYYCEDTSKYPYTFGQGTKLEIKSGGGGSEVQIjVESGGGIjVQPGGSLKLSCAAS GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 521</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VH CDR1</td><td>aa</td><td>NAWMD</td>
<td> 522</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VH CDR2</td><td>aa</td><td>QITAKSNNYATYYAA?VKG</td>
<td> 523</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VH CDR3</td><td>aa</td><td>DGYH</td>
<td> 524</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VL CDR1</td><td>aa</td><td>RASEDIRNGLA</td>
<td> 525</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VL CDR2</td><td>aa</td><td>NANSLHS</td>
<td> 526</td><td>BCMA-53</td><td>BC E11 19- G3-F8</td><td>VL CDR3</td><td>aa</td><td>EDTSKYPYT</td>
<td> 527</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYYAAPVK GRFTIS RDDS KNTLYLQMNS L KKEDTAVYYCTDDGYHWGQGTLVTVS S</td>
<td> 528</td><td>BCMA-53</td><td>BC E11 19- G3-F8</td><td>VL</td><td>aa</td><td>AIQMTQSPSSLSASVGDRVTIKCRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHSGVPSRFSGSGS GTDFTLTISSMQPEDEGTYYCEDTSKYPYTFGQGTKLEIK i</td>
<td> 529</td><td>BCMA-53</td><td>BC E11 19G3-F8</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYmAAPVIC: GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQlfí TQSPSSLSASVGDRVTIKCRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHSGVPSRFSGSGSGTEffia TLTISSMQPEDEGTYYCEDTSKYPYTFGQGTKLEIK |</td>
<td> 530</td><td>BCMA-53 HL x CD3 HL</td><td>BC E11 19G3-F8 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATY ÍAJkPVh' GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGG SSAIQ^</td>
LO
<img file="MX349396B_D0098.tif" />
<img file="MX349396B_D0099.tif" />
<td></td><td></td><td>xCD3HL</td><td>ca</td><td></td><td colspan="2">TQSPSSLSASVGDRVTIKCRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHSGVPSRFSGSGSGTDF TLTISSMQPEDEGTYYCEDTSKYPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLKLSCAAS GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 531</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NAWMD</td>
<td> 532</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VH CDR2</td><td>aa</td><td colspan="2">QITAKSNNYATYYAAPVKG</td>
<td> 533</td><td>BCMA-54</td><td>BC E11 19- B2-F8</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYH</td>
<td> 534</td><td>BCMA-54</td><td>BC E11 19- B2-F8</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASEDIRNGLA</td>
<td> 535</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VL CDR2</td><td>aa</td><td colspan="2">NANSLHT</td>
<td> 536</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VL CDR3</td><td>aa</td><td colspan="2">EDTSKYPYT</td>
<td> 537</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYYAAPVK GRFTISRDDS KNTLYLQMNS LKKEDTAVYYCTDDGYHWGQGTLVTVS S</td>
<td> 538</td><td>BCMA-54</td><td>BC E11 19B2-F8</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGS GTDFTLTISSLQPEDEAIYYCEDTSKYPYTFGQGTKLEIK</td>
<td> 539</td><td>BCMA-54</td><td>BC E11 19- B2-F8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYYAAPVK GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTDF TLTISSLQPEDEAIYYCEDTSKYPYTFGQGTKLEIK</td>
<td> 540</td><td>BCMA-54 HL x CD3 HL</td><td>BC E11 19B2-F8 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td>ΕνθΒνΕ3θσ6ΕνΚΡσΕ3ΕΕΗ3σΑΑ3σΡΤΡ3ΝΑΗΜΟΝνΕ0ΑΡΟΚΕΒΕΝΙΑ0ΙΤΑΚ3ΝΝΥΑΊ GRFTISRDDS KNTLYLQMNS LKKEDTAVYYCTDDGYHWGQGTLVTVS SGGGGSGGGGS GC TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKL·L·IYNANSL·HTGVPSRFSC TLTISSLQPEDEAIYYCEDTSKYPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSI GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQL· TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLT1 LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSC EYYCVLWYSNRWVFGGGTKLTVL</td><td>ΎΥΑΆΡνΚ GGSAIQjfl. SGSGTLtT KLSC^Ot<sup>r</sup>SPGG33®£s rVQP^^fek -rcr</td>
<td> 541</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>VH CDR1</td><td>aa</td><td>NAWMD</td><td></td>
LO
<td> 542</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>VH CDR2</td><td>aa</td><td colspan="2">QITAKSΝΝΥΑΤ ΥΎΑΑΡVKG</td><td rowspan="10"> 195 4</td>
<td> 543</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYH</td>
<td> 544</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASEDIRNGLA</td>
<td> 545</td><td>BCMA-55</td><td>BC E11-20H9-E9</td><td>VL CDR2</td><td>aa</td><td colspan="2">NANSLHT</td>
<td> 546</td><td>BCMA-55</td><td>BC E11-20H9-E9</td><td>VL CDR3</td><td>aa</td><td colspan="2">EETLKYPYT</td>
<td> 547</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGSLVKPGGSLRLSCAASGFTFSNAWMDWVRQAPGKRLEWVAQITAKSNNYATYYAAPVK GRFTIS RDDS KNTLYLQMNS LKEEDTAVYYCTDDGYHWGQGTLVTVSS</td>
<td> 548</td><td>BCMA-55</td><td>BC E11-20H9-E9</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGS GTDFTLTISNLQPEDEATYYCEETLKYPYTFGQGTKLEIK</td>
<td> 549</td><td>BCMA-55</td><td>BC E11-20- H9-E9</td><td>scFv</td><td>aa</td><td colspan="2">Εν0ΕνΕ3σθ3ΕνΚΡσθ3ΕΕΕΞαΆΑ3σΡΤΡ3ΝΑΝΜΌΝνΕ0ΑΡΘΚΕΕΕΝνΑ0ΙΤΑΚ3ΝΝΥΑΤΥΥΑΑΡνΚ ΘΕΡΤΙ3Εϋϋ3ΚΝΤΕΥΕ0ΜΝ3ΕΚΕΕΟΤΑνΥΥΟΤΠθσΥΗΝσζ2σΤΕντν33θσΘσ3σσσΘΞσθσθ3ΑΙ0Μ TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTDF TLTISNLQPEDEATYYCEETLKYPYTFGQGTKLEIK</td>
<td> 550</td><td>BCMA-55 HL x CD3 HL</td><td>BC El 1-20- H9-E9 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGSLVKPGGSLRLSCAASGFTFSNAWMDWVRQAPGKRLEWVAQITAKSNNYATYYAAPVK GRFTISRDDSKNTLYLQMNSLKEEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGG3AIQM TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTDF ΤΕΤΙ3ΝΕ0ΡΕϋΕΑΤΥΥσΕΕΤΕΚΥΡΥΤΡΘ0σΤΚΕΕΙΚ3Θσσσ3ΕνςΕνΕ3σΘσΕν0ΡΘσ3ΕΚΕ30ΑΑ3 GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 551</td><td>BCMA-56</td><td>BC E11-19- F11-E9</td><td>VH CDR1</td><td>aa</td><td colspan="2">NAWMD · i _</td>
<td> 552</td><td>BCMA-56</td><td>BC E11-19F11-E9</td><td>VH CDR2</td><td>aa</td><td>QITAKSNN YAT YY AEPVKG</td><td> 8 2</td><td></td>
<td> 553</td><td>BCMA-56</td><td>BC E11-19F11-E9</td><td>VH CDR3</td><td>aa</td><td>DGYH</td><td></td><td rowspan="3"></td>
<td> 554</td><td>BCMA-56</td><td>BC E11-19F11-E9</td><td>VL CDR1</td><td>aa</td><td>RASEDIRNGLA</td><td>IVIIUS, ivasfd</td>
<td> 555</td><td>BCMA-56</td><td>BC E11-19-</td><td>VL CDR2</td><td>aa</td><td>NANSLHT</td><td></td>
<td></td><td></td><td>F11-E9</td><td></td><td colspan="4"></td>
<td> 556</td><td>BCMA-56</td><td>BC E11-19- F11-E9</td><td>VL CDR3</td><td>aa</td><td colspan="2">EETLKYPYT</td><td></td>
<td> 557</td><td>BCMA-56</td><td>BC E11-19F11-E9</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWVAQITAKSNNYATYYAEPVK GRFTISRDDS KNTLYLQMNS LKTEDTAVYYCTDDGYHWGQGTLVTVS S</td><td></td>
<td> 558</td><td>BCMA-56</td><td>BC E11-19- F11-E9</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGETVTIACEASEDIENGLAWYQQKPGKAPKLLIYNANSLHTGVPSEFSGSGS GTEFTLKISSLQPEDEATYYCEETLKYPYTFGQGTKLEIK ,</td><td></td>
<td> 559</td><td>BCMA-56</td><td>BC E11-19- F11-E9</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVKPGESLELSCAASGFTFSNAWMDWVEQAPGKELEWVAQITAKSNNYATYYAEPVK GEFTISRDDSKNTLYLQMNSLKTEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGETVTIACEASEDIENGLAWYQQKPGKAPKLLIYNANSLHTGVPSEFSGSGSGTEF TLKISSLQPEDEATYYCEETLKYPYTFGQGTKLEIK</td><td></td>
<td> 560</td><td>BCMA-56 HL x CD3 HL</td><td>BC E11-19F11-E9 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVKPGESLELSCAASGFTFSNAWMDWVEQAPGKELEWVAQITAKSNNYATYYAEPVK GEFTISRDDSKNTLYLQMNSLKTEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGETVTIACEASEDIENGLAWYQQKPGKAPKLLIYNANSLHTGVPSEFSGSGSGTEF ΤΕΚΙΒεΕΟΡΕϋΕΑΤΥΥΟΕΕΤΕΚΥΡΥΤΕΘΟΘΤΚΕΕΙΚεσΘσΘεΕνΟΕνΕεσΟΟΕνΟΡΘσδΕΚΏεΟΑΑΞ GFTFNKYAMNWVEQAPGKGLEWVAETESKYNNYATYYADSVKDRFTISEDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 561</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VH CDR1</td><td>aa</td><td colspan="2">NAWMD</td><td></td>
<td> 562</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VH CDR2</td><td>aa</td><td colspan="2">QITAKSNNYATYYAAPVKG</td><td></td>
<td> 563</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VH CDR3</td><td>aa</td><td colspan="2">DGYH</td><td></td>
<td> 564</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VL CDR1</td><td>aa</td><td>RASEDIRNGLA</td><td></td><td></td>
<td> 565</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VL CDR2</td><td>aa</td><td>NANSLHT</td><td>ir Nsint PE</td><td></td>
<td> 566</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VL CDR3</td><td>aa</td><td>EETLKYPYT</td><td></td><td></td>
<td> 567</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>VH</td><td>aa</td><td>ΞνΟΕνΕΞσσσΕνΚΡΘΕδΕΕΕδσΑΑΞΟΕΤΡδΝΑΉΜΌΝνΕΟΑΡσΚΕΕΕΚΙΑΟΙΤΑΚΞΝΝΥΑ GEFTISEDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSS</td><td>rYYAMgtfK</td><td> 5</td>
<td> 568</td><td>BCMA-57</td><td>BC E11-19- B2-E9</td><td>VL</td><td>aa</td><td>AIQMTQSPSSLSASVGDEVTIACRASEDIENGLAWYQQKPGKAPKLLIYNANSLHTGVP</td><td colspan="2"></td>
196
<td></td><td></td><td></td><td></td><td></td><td>GTDFTLTISSLQPEDEAIYYCEETLKYPYTFGQGTKLEIK</td>
<td> 569</td><td>BCMA-57</td><td>BC E11-19B2-E9</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRL.EWIAQITAKSNNYATYYAAPVK GRFTISRDDSKNTLYLQMNS LKKEDTAVYYCTDDGYHWGQGTLVTVS SGGGGS GGGGS GGGGSAIQM TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTDF TLTISSLQPEDEAIYYCEETLKYPYTFGQGTKLEIK</td>
<td> 570</td><td>BCMA-57 HL xCD3HL</td><td>BC E11-19B2-E9 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYYAAPVK GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGDRVTIACRASEDIRNGLAWYQQKPGKAPKLLIYNANSLHTGVPSRFSGSGSGTDF TLTISSLQPEDEAIYYCEETLKYPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLKLSCAAS GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 571</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VH CDR1</td><td>aa</td><td>NAWMD</td>
<td> 572</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VH CDR2</td><td>aa</td><td>QITAKSNNYATYYAAPVKG</td>
<td> 573</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VH CDR3</td><td>aa</td><td>DGYH</td>
<td> 574</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VL CDR1</td><td>aa</td><td>RASEDIRNGLA</td>
<td> 575</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VL CDR2</td><td>aa</td><td>NANSLHS</td>
<td> 576</td><td>BCMA-58</td><td>BC E11-19- G3-E9</td><td>VL CDR3</td><td>aa</td><td>EETLKYPYT</td>
<td> 577</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>VH</td><td>aa</td><td>Εν0ΒνΕ3σσσΕνΚΡΘΕ3ΕΕΓ5αΑΑ3σΡΤΕ3ΝΑΗΜΕΚνΡ0ΑΡβΚΕΒΕΝΙΑ0ΙΤΑΚ3ΝΝΥΑΤΥΥΑΑΡνΚ GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSS</td>
<td> 578</td><td>BCMA-58</td><td>BC E11-19- G3-E9</td><td>VL</td><td>aa</td><td>aiqmtqspsslsasvgdrvtikcrasedirnglawyqqkpgkapklliynanslhsgvpsífsgsgs GTDFTLTISSMQPEDEGTYYCEETLKYPYTFGQGTKLEIK f</td>
<td> 579</td><td>BCMA-58</td><td>BC E11-19G3-E9</td><td>scFv</td><td>aa</td><td>EVQLiVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRIjEWIAQITAKSNNYATKYAAP'^e J GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLV’rVSSGGGGSGGGGSGGCGSAjSify TQSPSSLSASVGDRVTIKCRASEDIRNGLAWYQQKPGKAPKIiLIYNANSLHSGVPSRFSCKGSG?^'^ TLTISSMQPEDEGTYYCEETLKYPYTFGQGTKLEIK I --------------------------------------------------------------1------------------------------------------------------------------1--------fe</td>
197
<img file="MX349396B_D0100.tif" />
<td> 580</td><td>BCMA-58 HL x CD3 HL</td><td>BC E11-19G3-E9 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVKPGESLRLSCAASGFTFSNAWMDWVRQAPGKRLEWIAQITAKSNNYATYYAAPVK GRFTISRDDSKNTLYLQMNSLKKEDTAVYYCTDDGYHWGQGTLVTVSSGGGGSGGGGSGGGGSAIQM TQSPSSLSASVGDRVTIKCRASEDIRNGLAWYQQKPGKAPKLLIYNANSIjHSGVPSRFSGSGSGTDF ΤΕΤΙ33Μ0ΡΕΟΕσΤΥΥσΕΕΤΕΚΥΡΥΤΡΟ0ΟΤΚΕΕΙΚΞσσσα8Εν0ΕνΕ3σθσ£ν0Ρθσ3ΕΚΕ3σΑΑ3 GFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTED TAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVSPGGTVT LTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEA EYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 581</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td>
<td> 582</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VH CDR2</td><td>aa</td><td>SIITSGGDNYYRDSVKG</td>
<td> 583</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td>
<td> 584</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VLCDR1</td><td>aa</td><td>KASQSVGINVD</td>
<td> 585</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td>
<td> 586</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td>
<td> 587</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VH</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 588</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>VL</td><td>aa</td><td>EIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQSEEFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 589</td><td>BCMA-59</td><td>BC 5G9-91D2</td><td>scFv</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYEMAWVRQAPGKGLEWVASIITSGGENYYRESVKGR FTISRDNAKNTLYLQMNSLRAEBTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEEFAVYYCLQYGSIPFTFGPGTKVDIK 1</td>
<td></td><td></td><td rowspan="2">BC 5G9-91- D2 HL x CD3 HL</td><td rowspan="2">bispecific molecule</td><td></td><td>_ _____________ ______ _ ______ ________J____11-· QVQLVESGGGWQPGRSLRLSCAASGFTFSNYEMAWVRQAPGKGLEWVASIITSGGDWYRBSVjGR FTISRDNAKNTLYLCMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGqSGGGG^SG^'</td>
<td> 590</td><td>BCMA-59 HL x CD3 HL</td><td>aa</td><td>GSEIVMTQSPASMSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRH<sup>,</sup>]jGIPA|S?bS<sup>!s </sup>GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGaLVQE^^feíH LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYTVDSVKDRFTISRDDaKNTT^g^N' NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVS SGGGGS GGGGSGGGGS QTWTQE PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGfKAAI^pg^</td>
<td></td><td></td><td></td><td></td><td></td><td>QPEDEAEYYCVLWYSNRWVFGGGTKLTVL·</td><td></td><td></td>
<td> 591</td><td>BCMA-60</td><td>BC 5G9-91- C7</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td></td><td></td>
<td> 592</td><td>BCMA-60</td><td>BC 5G9-91- C7</td><td>VH CDR2</td><td>aa</td><td>SIITSGGDNYYRDSVKG</td><td></td><td></td>
<td> 593</td><td>BCMA-60</td><td>BC 5G9-91C7</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td></td><td></td>
<td> 594</td><td>BCMA-60</td><td>BC 5G9-91C7</td><td>VL CDR1</td><td>aa</td><td>KASQSVGINVD</td><td></td><td></td>
<td> 595</td><td>BCMA-60</td><td>BC 5G9-91C7</td><td>VL CDR2</td><td>aa</td><td>GASNRHT</td><td></td><td></td>
<td> 596</td><td>BCMA-60</td><td>BC 5G9-91- C7</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td></td><td></td>
<td> 597</td><td>BCMA-60</td><td>BC 5G9-91- C7</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td><td></td>
<td> 598</td><td>BCMA-60</td><td>BC 5G9-91- C7</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td></td>
<td> 599</td><td>BCMA-60</td><td>BC 5G9-91C7</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td><td> 199</td>
<td> 600</td><td>BCMA-60 HL x CD3 HL</td><td>BC 5G9-91- C7 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNY· FTISRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGS GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTG GSGREFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGL LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSK] NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWT PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGK, QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>ZRDSVKGR 3GGGSGGG IPARFSGS VQPGGSLK NTAYLQMN 2EPSLTVS lALTLSGV</td><td rowspan="2"></td>
<td> 601</td><td>BCMA-61</td><td>BC 5G9-91- E4</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td>IV TTTVTt Oí u</td>
<td> 602</td><td>BCMA-61</td><td>BC 5G9-91E4</td><td>VH CDR2</td><td>aa</td><td>SIITSGGDNYYRDSVKG</td><td>i r > FBORI INDur</td><td></td>
<td> 603</td><td>BCMA-61</td><td>BC 5G9-91- E4</td><td>VH CDR3</td><td>aa</td><td>HDYYDGSYGFAY</td><td>1 ¡Al* ¡DAD TtlAL</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
604
BCMA-61
VLCDR1
KASQSVGINVD aa
BC 5G9-91E4
<td> 605</td><td>BCMA-61</td><td>BC 5G9-91- E4</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASNRHT</td><td rowspan="10"> 200</td>
<td> 606</td><td>BCMA-61</td><td>BC 5G9-91E4</td><td>VLCDR3</td><td>aa</td><td colspan="2">LQYGSIPFT</td>
<td> 607</td><td>BCMA-61</td><td>BC 5G9-91E4</td><td>VH</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td> 608</td><td>BCMA-61</td><td>BC 5G9-91E4</td><td>VL</td><td>aa</td><td colspan="2">EIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 609</td><td>BCMA-61</td><td>BC 5G9-91E4</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIK</td>
<td> 610</td><td>BCMA-61 HL x CD3 HL</td><td>BC 5G9-91E4HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTISRDNSKNTLYLQMNSLRSEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVWTQSPATLSVSPGERVTLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQSEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 611</td><td>BCMA-62</td><td>BC 5G9-92E10</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 612</td><td>BCMA-62</td><td>BC 5G9-92E10</td><td>VH CDR2</td><td>aa</td><td colspan="2">SIITSGGDNYYRDSVKG</td>
<td rowspan="2"> 613</td><td rowspan="2">BCMA-62</td><td rowspan="2">BC 5G9-92E10</td><td rowspan="2">VH CDR3</td><td rowspan="2">aa</td><td colspan="2"></td>
<td></td><td></td>
<td> 614</td><td>BCMA-62</td><td>BC 5G9-92- E10</td><td>VLCDR1</td><td>aa</td><td>KASQSVGINVD</td><td>ir</td><td></td>
<td> 615</td><td>BCMA-62</td><td>BC 5G9-92E10</td><td>VLCDR2</td><td>aa</td><td>GASNRHT</td><td>LTA Hito.· RttAÍ tu</td><td rowspan="4"> «4</td>
<td> 616</td><td>BCMA-62</td><td>BC 5G9-92E10</td><td>VL CDR3</td><td>aa</td><td>LQYGSIPFT</td><td>Hiwcn VTHT31 T</td>
<td> 617</td><td>BCMA-62</td><td>BC 5G9-92-</td><td>VH</td><td>aa</td><td>QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNY!</td><td>RDSVKGR^</td>
<td colspan="6"></td><td></td>
618
BCMA-62
619
BCMA-62
Ε10
BC 5G9-92E10
VL aa
FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSS
EIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGSGS GTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIK
BC 5G9-92E10 scFv
<img file="MX349396B_D0101.tif" />
QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIK
620
621
622
623
624
625
626
627
628
629
BCMA-62 HL x CD3 HL
BC 5G9-92E10 HL x CD3 HL bispecific molecule
<img file="MX349396B_D0102.tif" />
QVQLVESGGGWQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVASIITSGGDNYYRDSVKGR FTVSRDNSKNTLYLQMNSLRAEDTAVYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSEIVMTQSPATLSVSPGERATLSCKASQSVGINVDWYQQKPGQAPRLLIYGASNRHTGIPARFSGS GSGTEFTLTISSLQAEDFAVYYCLQYGSIPFTFGPGTKVDIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BCMA-63
BC 3A4-37C8______
BC 3A4-37C8______
BC 3A4-37C8______
BC 3A4-37C8______
BC 3A4-37C8______
BC 3A4-37C8
BC 3A4-37C8
BC 3A4-37C8
BC 3A4-37C8
VH CDR1
VH CDR2
VH CDR3
VL CDR1
VL CDR2
VL CDR3
VH
VL scFv aa aa aa aa aa aa aa aa
<img file="MX349396B_D0103.tif" />
NYDMA
SISTRGDITSYRDSVKG
QDYYTDYMGFAY
RASEDIYNGLA
GASSLQD
QQSYKYPLT
EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSY^DSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS
AIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPS GTDYTLTISSLQPEDEATYYCQQSYKYPLTFGGGTKVEIK
FSGS
<img file="MX349396B_D0104.tif" />
-EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSY iDSvffg FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSG 3GGSSS§
GSAIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGV ?SRFS
GGSSS§É=a4
<img file="MX349396B_D0105.tif" />
<td></td><td></td><td></td><td></td><td></td><td colspan="2">GSGTDYTLTISSLQPEDEATYYCQQSYKYPLTFGGGTKVEIK</td>
<td> 630</td><td>BCMA-63 HL x CD3 HL</td><td>BC 3A4-37- C8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDYTLTISSLQPEDEATYYCQQSYKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL·</td>
<td> 631</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 632</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 633</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 634</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 635</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 636</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQSYKYPLT</td>
<td> 637</td><td>BCMA-64</td><td>BC 3A4-37- C9</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGL·VQPGRSL·RL·SCAASGFTFSNYDMAWVRQAPGKGL·EWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 638</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTDFTLTISSMQPEDEATYYCQQSYKYPLTFGGGTKVEIK</td>
<td> 639</td><td>BCMA-64</td><td>BC 3A4-37C9</td><td>scFv</td><td>aa</td><td>EVQLL·ESGGGLVQPGRSL·RL·SCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITS5 FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSC GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGI GSGTDFTLTISSMQPEDEATYYCQQSYKYPLTFGGGTKVEIK</td><td>ÍRDSVKGR 3GGGSGGG PSRFSGS I*</td>
<td> 640</td><td>BCMA-64 HL x CD3 HL</td><td>BC 3A4-37C9HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQL·LESGGGLVQPGRSL·RL·SCAASGFTFSNYDMAWVRQAPGKGL·EWVSSISTRGDITS<sup>, </sup>FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSC GSAIQMTQSPSSL·SASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDG’ GSGTDFTLTISSMQPEDEATYYCQQSYKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGL' LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSK</td><td>RDsvág^ 0603035^® ’PSR^&S^ 'QPG«f$í$ ftaylQWn</td>
202
<img file="MX349396B_D0106.tif" />
NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS
<td></td><td></td><td></td><td></td><td></td><td colspan="2">pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 641</td><td>BCMA-65</td><td>BC 3A4-37- E11</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td></td><td></td>
<td> 642</td><td>BCMA-65</td><td>BC 3A4-37- E11</td><td>VH CDR2</td><td>aa</td><td>SISTRGDITSYRDSVKG</td><td></td><td></td>
<td> 643</td><td>BCMA-65</td><td>BC 3A4-37E11</td><td>VH CDR3</td><td>aa</td><td>QDYYTDYMGFAY</td><td></td><td></td>
<td> 644</td><td>BCMA-65</td><td>BC 3A4-37E11</td><td>VL CDR1</td><td>aa</td><td>RASEDIYNGLA</td><td></td><td></td>
<td> 645</td><td>BCMA-65</td><td>BC 3A4-37E11</td><td>VL CDR2</td><td>aa</td><td>GASSLQD</td><td></td><td></td>
<td> 646</td><td>BCMA-65</td><td>BC 3A4-37E11</td><td>VL CDR3</td><td>aa</td><td>QQSYKYPLT</td><td></td><td></td>
<td> 647</td><td>BCMA-65</td><td>BC 3A4-37E11</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td><td></td>
<td> 648</td><td>BCMA-65</td><td>BC 3A4-37- E11</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTHYTLTISSLQPEDEATYYCQQSYKYPLTFGGGTKVEIK</td><td></td>
<td> 649</td><td>BCMA-65</td><td>BC 3A4-37- E11</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTHYTLTIS SLQPEDEATYYCQQSYKYPLTFGGGTKVEIK</td><td> 203</td>
<td> 650</td><td>BCMA-65 HL xCD3 HL</td><td>BC 3A4-37- E11 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSY FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGV GSGTHYTLTISSLQPEDEATYYCQQSYKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLV LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQ PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGK^ QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>RDSVKGR GGGSGGG ’SRFSGS JPGGSL£> PAYLQ^t> üPSLTJfg’ <sup>1LT</sup>W</td><td rowspan="2"></td>
<td> 651</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td>IV b αν 2 ON 1 V</td>
<td> 652</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VH CDR2</td><td>aa</td><td>SISTRGDITSYRDSVKG</td><td></td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td colspan="2">ΓΜ\</td>
<td> 653</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 654</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 655</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 656</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VL CDR3</td><td>aa</td><td colspan="2">AGPHKYPLT</td>
<td> 657</td><td>BCMA-66</td><td>BC 3A4-37C8-G1</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 658</td><td>BCMA-66</td><td>BC 3A4-37- C8-G1</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTDYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 659</td><td>BCMA-66</td><td>BC 3A4-37- C8-G1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 660</td><td>BCMA-66 HL x CD3 HL</td><td>BC 3A4-37- C8-G1 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS ΡσστνΤΕΤ0σ33ΤσΆνΤ3σΝΥΡΝΝν00ΚΡΟ0ΑΡΡσΕΐασΤΚΡΒΑΡσΤΡΑΡΡ3Ο3ΕησθΚΑΑΕΤΏ30ν QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 661</td><td>BCMA-67</td><td>BC 3A4-37E11-G1</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 662</td><td>BCMA-67</td><td>BC 3A4-37- E11-G1</td><td>VH CDR2</td><td>aa</td><td colspan="2">SIS TRGDITSYRDSVKG</td>
<td> 663</td><td>BCMA-67</td><td>BC 3A4-37E11-G1</td><td>VH CDR3</td><td>aa</td><td>QDYYTDYMGFAY</td><td></td>
<td> 664</td><td>BCMA-67</td><td>BC 3A4-37E11-G1</td><td>VLCDR1</td><td>aa</td><td>RASEDIYNGLA</td><td></td>
<td> 665</td><td>BCMA-67</td><td>BC 3A4-37- E11-G1</td><td>VL CDR2</td><td>aa</td><td>GASSLQD</td><td>X J roMu LABIO INDI</td>
<td> 666</td><td>BCMA-67</td><td>BC 3A4-37-</td><td>VLCDR3</td><td>aa</td><td>AGPHKYPLT</td><td>- J JCANt »ISDAi STRIA</td>
204
<td></td><td></td><td>E11-G1</td><td></td><td colspan="3"></td>
<td> 667</td><td>BCMA-67</td><td>BC 3A4-37E11-G1</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 668</td><td>BCMA-67</td><td>BC 3A4-37E11-G1</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTHYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 669</td><td>BCMA-67</td><td>BC 3A4-37- E11-G1</td><td>scFv</td><td>aa</td><td colspan="2">ΕνοΕΕΕεοσαΕνορσσεΕΕΕδαΑΑΒσρτρεΝΥΌΜΑΗνΕςΑΡΟκοΒΕΝνΞείΕΤΕαϋΐτΞΥΕϋενκσΕ FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTHYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 670</td><td>BCMA-67 HL XCD3HL</td><td>BC 3A4-37E11-G1 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTHYTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 671</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 672</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 673</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 674</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 675</td><td>BCMA-68</td><td>BC 3A4-37- C8-G8</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 676</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VL CDR3</td><td>aa</td><td>QQSRNYQQT</td><td></td>
<td> 677</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VH</td><td>aa</td><td>EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSY FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVS S</td><td>tDSVKqá#</td>
<td> 678</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>VL</td><td>aa</td><td>AIQMTQSPSSLSASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPS GTDYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td><td>RFSGStS^<sup>1 </sup>te</td>
205
<img file="MX349396B_D0107.tif" />
<td> 679</td><td>BCMA-68</td><td>BC 3A4-37C8-G8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG σ5ΑΙ0ΜΤ03Ρ38Β3Α3νσΌΤνΤΙΤσΡΑ3ΕΟΙΥΝσΕΑΝΥ00ΚΡσΚΑΡΚΒΒΙΥσΑ33Ε0ΌσνΡ3ΕΡ3σ3 GSGTDYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td>
<td> 680</td><td>BCMA-68 HL XCD3HL</td><td>BC 3A4-37C8-G8 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSL·SASVGDTVTITCRASEDIYNGLAWYQQKPGKAPKL·LIYGASSL·QDGVPSRFSGS GSGTDYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 681</td><td>BCMA-69</td><td>BC 3A4-37- E11-G8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 682</td><td>BCMA-69</td><td>BC 3A4-37E11-G8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 683</td><td>BCMA-69</td><td>BC 3A4-37E11-G8</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 684</td><td>BCMA-69</td><td>BC 3A4-37- E11-G8</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 685</td><td>BCMA-69</td><td>BC 3A4-37E11-G8</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 686</td><td>BCMA-69</td><td>BC 3A4-37E11-G8</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQSRNYQQT</td>
<td> 687</td><td>BCMA-69</td><td>BC 3A4-37- E11-G8</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 688</td><td>BCMA-69</td><td>BC 3A4-37- E11-G8</td><td>VL</td><td>aa</td><td>AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKL·LIYGASSLQDG GTHYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td><td>VPSRFSGSGS</td>
<td> 689</td><td>BCMA-69</td><td>BC 3A4-37E11-G8</td><td>scFv</td><td>aa</td><td>EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDI FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLC GSGTHYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td><td>rSYRDStte^ ssgggSs^h* DGVP§^.|’^a| k__u _</td>
<td> 690</td><td>BCMA-69 HL x CD3 HL</td><td>BC 3A4-37E11-G8HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDj FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGC</td><td>TSYR^^KO^ GSGGGG^qaG</td>
206
<td></td><td></td><td>xCD3 HL</td><td>ca</td><td></td><td colspan="2">GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRPSGS GSGTHYTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 691</td><td>BCMA-70</td><td>BC 3A4-37- A11-G8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 692</td><td>BCMA-70</td><td>BC 3A4-37- A11-G8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 693</td><td>BCMA-70</td><td>BC 3A4-37- A11-G8</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 694</td><td>BCMA-70</td><td>BC 3A4-37- A11-G8</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 695</td><td>BCMA-70</td><td>BC 3A4-37A11-G8</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 696</td><td>BCMA-70</td><td>BC 3A4-37- A11-G8</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQSRNYQQT</td>
<td> 697</td><td>BCMA-70</td><td>BC 3A4-37A11-G8</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 698</td><td>BCMA-70</td><td>BC 3A4-37A11-G8</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTEFTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td>
<td> 699</td><td>BCMA-70</td><td>BC 3A4-37A11-G8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTEFTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td>
<td> 700</td><td>BCMA-70 HL x CD3 HL</td><td>BC 3A4-37A11-G8 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITÉ FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGS GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDC GSGTEFTLTISSLQPEDEATYYCQQSRNYQQTFGGGTKVEIKSGGGGSEVQLVESGGGI LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSI NL.KTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWn PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGl QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>7RDSVKGR 3GGGSGGG VPSRF^s VQPGfSafe NTAYI^lS QEPSaHR/iS_ AALli^ví</td>
207
Λ)
<td> 701</td><td>BCMA-71</td><td>BC 3A4-37- A11-G1</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 702</td><td>BCMA-71</td><td>BC 3A4-37- A11-G1</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 703</td><td>BCMA-71</td><td>BC 3A4-37A11-G1</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 704</td><td>BCMA-71</td><td>BC 3A4-37- A11-G1</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASEDIYNGLA</td>
<td> 705</td><td>BCMA-71</td><td>BC 3A4-37A11-G1</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 706</td><td>BCMA-71</td><td>BC 3A4-37- A11-G1</td><td>VL CDR3</td><td>aa</td><td colspan="2">AGPHKYPLT</td>
<td> 707</td><td>BCMA-71</td><td>BC 3A4-37A11-G1</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 708</td><td>BCMA-71</td><td>BC 3A4-37A11-G1</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTE FTLTISSLQPEDEATYYCAGPHKYPLT FGGGTKVEIK</td>
<td> 709</td><td>BCMA-71</td><td>BC 3A4-37A11-G1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTEFTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 710</td><td>BCMA-71 HL x CD3 HL</td><td>BC 3A4-37A11-G1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGGSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTEFTLTISSLQPEDEATYYCAGPHKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL i</td>
<td> 711</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>VH CDR1</td><td>aa</td><td>NYDMA</td><td>I</td>
<td> 712</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>VH CDR2</td><td>aa</td><td>SISTRGDITS YRD SVKG</td><td>Jai «i» r</td>
<td> 713</td><td>BCMA-72</td><td>BC 3A4-37- C9-G1</td><td>VH CDR3</td><td>aa</td><td>QDYYTDYMGFAY</td><td>r fjucai mea 1USTKI</td>
<td> 714</td><td>BCMA-72</td><td>BC 3A4-37-</td><td>VL CDR1</td><td>aa</td><td>RASEDIYNGLA</td><td></td>
208
<td rowspan="14"> 5 10 15 20</td><td></td><td></td><td>C9-G1</td><td></td><td></td><td colspan="2"></td><td rowspan="13">209 I M J</td>
<td> 715</td><td>BCMA-72</td><td>BC 3A4-37- C9-G1</td><td>VL CDR2</td><td>aa</td><td colspan="2">GASSLQD</td>
<td> 716</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>VL CDR3</td><td>aa</td><td colspan="2">AGPHKYPLT</td>
<td> 717</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>VH</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 718</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>VL</td><td>aa</td><td colspan="2">AIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTDFTLTISSMQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 719</td><td>BCMA-72</td><td>BC 3A4-37C9-G1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDFTLTISSMQPEDEATYYCAGPHKYPLTFGGGTKVEIK</td>
<td> 720</td><td>BCMA-72 HL x CD3 HL</td><td>BC 3A4-37C9-G1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">Εν0ΕΕΕ3ΟΟΟΕν0Ρ6Ε3ΕΕΕ3αΑΑ3σΡΤΡ3ΝΥΏΜΑΜνΕ0ΑΡΟΚΟΕΕΚν3ΞΙ3ΤΕαθΙΤ3ΥΕΟ3νΚ6Ε FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDFTLTISSMQPEDEATYYCAGPHKYPLTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 721</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NYDMA</td>
<td> 722</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SISTRGDITSYRDSVKG</td>
<td> 723</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VH CDR3</td><td>aa</td><td colspan="2">QDYYTDYMGFAY</td>
<td> 724</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VLCDR1</td><td>aa</td><td>RASEDIYNGLA</td><td></td>
<td> 725</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VL CDR2</td><td>aa</td><td>GASSLQD</td><td>al</td>
<td> 726</td><td>BCMA-73</td><td>BC 3A4-37- C9-G8</td><td>VL CDR3</td><td>aa</td><td>QQSRNYQQT</td><td></td>
<td> 727</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VH</td><td>aa</td><td>EVQLLESGGGLVQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSS</td><td>?svk3Í5 >> *</td><td> >—<</td>
<img file="MX349396B_D0108.tif" />
<td> 728</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>VL</td><td>aa</td><td colspan="2">ATQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGSGS GTDFTLTISSMQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td>
<td> 729</td><td>BCMA-73</td><td>BC 3A4-37C9-G8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDTYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDFTLTISSMQPEDEATYYCQQSRNYQQTFGGGTKVEIK</td>
<td> 730</td><td>BCMA-73 HL x CD3 HL</td><td>BC 3A4-37C9-G8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLLESGGGLVQPGRSLRLSCAASGFTFSNYDMAWVRQAPGKGLEWVSSISTRGDITSYRDSVKGR FTISRDNSKNTLYLQMNSLRAEDTAVYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGGG GSAIQMTQSPSSLSASVGDRVTITCRASEDIYNGLAWYQQKPGKAPKLLIYGASSLQDGVPSRFSGS GSGTDFTLTISSMQPEDEATYYCQQSRNYQQTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 731</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 732</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 733</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 734</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNYLN</td>
<td> 735</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 736</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VL CDR3</td><td>aa</td><td colspan="2">MGQTISSYT</td>
<td> 737</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYA FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td>DSVKGR =</td>
<td> 738</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSR GTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td><sup>f</sup>SGSG§:</td>
<td> 739</td><td>BCMA-74</td><td>BC C3-33D7-B1</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYA FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVP GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td>)SVKá|p SGSGíleÉ ;rfsÍs-</td>
IMPI
Al
<td> 740</td><td>BCMA-74 HL x CD3 HL</td><td>BC C3-33- D7-B1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTTSRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS οεοτϋΥΤΕΤιεεΕςρΕΟΕΑΤΥΥσΜσοτίΞεγτΕσοοτκΕΕίκεσοοαεΕνοΕνΕεασσΕνορσσΞΕκ LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 741</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 742</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 743</td><td>BCMA-75</td><td>BC C3-33- F8-B1</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 744</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNYLN</td>
<td> 745</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 746</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VL CDR3</td><td>aa</td><td colspan="2">MGQTTSSYT</td>
<td> 747</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 748</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td>
<td> 749</td><td>BCMA-75</td><td>BC C3-33F8-B1</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTY ΡΤΙδΚΏΝΑΚΝΤΕΥΕΟΜΝΒΕΕΑΕΏΤΑνΥΥΟνΕΗαΥΥϋαΥΗΕΡηΥΝΟΟαΤΕντνεΞααΟαε GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSG GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td>YADSVKGR GGGGSGGG .VPSRFSGS</td>
<td> 750</td><td>BCMA-75 HL x CD3 HL</td><td>BC C3-33F8-B1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLWVSSITTGGGDTY FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGS GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSC GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGI LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSI NLKTEDTAVYYCVRHGNFGNS YIS YWAYWGQGTLVTVS SGGGGS GGGGS GGGGS QTW PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGI</td><td>ZADSV^g GGGGj^G VPSR^^ VQPGÉÉBt^ NTAYLQMN QEPstí^ff AAL'flg^gl</td>
QPE DEAEYYCVLWYSNRWVFGGGTKLTVL
<td> 751</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td> 752</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td></td><td></td>
<td> 753</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td><td></td>
<td> 754</td><td>BCMA-76</td><td>BC C3-33- F9-B1</td><td>VL CDR1</td><td>aa</td><td>RASQGISNYLN</td><td></td><td></td>
<td> 755</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 756</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td><td></td><td></td>
<td> 757</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGL·VQPGGSL·RL·SC7kASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td></td>
<td> 758</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td> 759</td><td>BCMA-76</td><td>BC C3-33F9-B1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR ρτιεΕΏΝΑΚΝΤΒΥΒΟΜοβΕΗεΕοτΑνγγονρΗογγοσΥΗΕΡΌγκσοΘΤΕντνεεσσοσεοσσοδοσο GSDIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td> 212</td>
<td> 760</td><td>BCMA-76 HL xCD3HL</td><td>BC C3-33F9-B1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVEQAPGKGLVWVSSITTGGGDTYYA ftisrdnakntlylqmdslrsedtavyycvrhgyydgyhlfdywgqgtlvtvssggggsgg GSDIQMTQSPSSLSASVGDRVTISCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVP GSGTDYTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQ LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNT NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQE PGGTVTLTCGS STGAVTSGNYPNWVQQKPGQAPRGLIGGT KFLAPGTPARFSGS LLGGKAA QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>DSVKGR GGSGGG SRFSGS PGGSLK AYLQMN RSLTVS iTLSGV . z</td><td></td>
<td> 761</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td>- -i</td><td rowspan="3"> £</td>
<td> 762</td><td>BCMA-77</td><td>BC C3-33- F10B1</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td>uJCai I0FIID 'USTRI</td>
<td> 763</td><td>BCMA-77</td><td>BC C3-33- F10B1</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td> 764</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VL CDR1</td><td>aa</td><td>RASQGISNYLN</td><td></td><td></td>
<td> 765</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 766</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VL CDR3</td><td>aa</td><td>MGQTISSYT</td><td></td><td></td>
<td> 767</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td></td>
<td> 768</td><td>BCMA-77</td><td>BC C3-33F10B1</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td> 769</td><td>BCMA-77</td><td>BC C3-33- F10B1</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIK</td><td></td>
<td> 770</td><td>BCMA-77 HL xCD3HL</td><td>BC C3-33- F10B1 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS GGGGSGGGG S GGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNYLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCMGQTISSYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVS SGGGGS GGGGSGGGGS QT WTQEPS LTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td> 213</td>
<td> 771</td><td>BCMA-78</td><td>BC E5-33A11-A1O</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td> 772</td><td>BCMA-78</td><td>BC E5-33A11-A1O</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td></td><td></td>
<td> 773</td><td>BCMA-78</td><td>BC E5-33A11-A10</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td><td rowspan="2"></td>
<td> 774</td><td>BCMA-78</td><td>BC E5-33A11-A10</td><td>VL CDR1</td><td>aa</td><td>RASQGISNHLN</td><td>O</td>
<td> 775</td><td>BCMA-78</td><td>BC E5-33A11-A10</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td>A MIOI INDU</td><td></td>
<td> 776</td><td>BCMA-78</td><td>BC E5-33A11-A10</td><td>VL CDR3</td><td>aa</td><td>QQYFDRPYT</td><td>iídad íTRIAL</td><td></td>
<td> 777</td><td>BCMA-78</td><td>BC E5-33-</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYAJ</td><td>SVKGRY —- -a r</td><td></td>
<td></td><td></td><td>A11-A10</td><td></td><td></td><td colspan="2">FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 778</td><td>BCMA-78</td><td>BC E5-33A11-A10</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWFQQKPGRAPKPLIYYTSNLQSGVPSRFSGSGS GTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td>
<td> 779</td><td>BCMA-78</td><td>BC E5-33A11-A1O</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWFQQKPGRAPKPLTYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td>
<td> 780</td><td>BCMA-78 HL x CD3 HL</td><td>BC E5-33- A11-A1O HLxCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR ρτιεΗϋΝΑΚΝΤΒΥΒΟΜΝδΒΡΑΕΟΤΑνγγανΗΗΘΥΥϋσΥΗΒΡΌΥΝσοστΒντνεεσσοαεοοσοεσοσ GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWFQQKPGRAPKPLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVS SGGGGSGGGGSGGGG S QTWTQE PS LTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 781</td><td>BCMA-79</td><td>BC E5-33- B11-A1O</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 782</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 783</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 784</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNHLN</td>
<td> 785</td><td>BCMA-79</td><td>BC E5-33B11-A10</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 786</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQYFDRPYT</td>
<td> 787</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS | 1 5 L.</td>
<td> 788</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLIYYTSNLQSGVP GTDYTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td><td>jRFSG^.</td>
<td> 789</td><td>BCMA-79</td><td>BC E5-33B11-A1O</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTY FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGS GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLTYYTSNLQSG</td><td>□ SÍ ADSWg>r jgggsSSg rPSRFSOÍ</td>
<td></td><td></td><td></td><td></td><td></td><td colspan="2">GSGTDYTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td>
<td> 790</td><td>BCMA-79 HL x CD3 HL</td><td>BC E5-33- B11-A1O HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 791</td><td>BCMA-80</td><td>BC E5-33G11-A1O</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 792</td><td>BCMA-80</td><td>BC E5-33G11-A1O</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 793</td><td>BCMA-80</td><td>BC E5-33G11-A1O</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 794</td><td>BCMA-80</td><td>BC E5-33G11-A10</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASQGISNHLN</td>
<td> 795</td><td>BCMA-80</td><td>BC E5-33G11-A1O</td><td>VLCDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 796</td><td>BCMA-80</td><td>BC E5-33G11-A1O</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQYFDRPYT</td>
<td> 797</td><td>BCMA-80</td><td>BC E5-33G11-A10</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 798</td><td>BCMA-80</td><td>BC E5-33G11-A10</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQGISNHLNWFQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td>
<td> 799</td><td>BCMA-80</td><td>BC E5-33G11-A10</td><td>scFv</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDT FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGG GSDIQMTQSPSSLSASVGDRVTITCRASQGISNHLNWFQQKPGKAPKPLIYYTSNLQS GSGTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td><td>YYADSVKGR SGGGGSGGG GVPSRFSGS Ϊ</td>
<td> 800</td><td>BCMA-80 HL x CD3 HL</td><td>BC E5-33- G11-A10 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDl ΡΤΙ3ΗΟΝΑΚΝΤΒΥΒ0ΜΟ3ΕΗΑΞϋΤΑνΥΥσνΗΗσΥΥϋσΥΗΕΕΟΥΝ0α0ΤΕντν33α0α£ GSDIQMTQSPSSLSASVGDRVTITCRASQGISNHLNWFQQKPGKAPKPLIYYTSNLQS GSGTDFTLTIS S LQPEDFATYYCQQYFDRPYTFGGGTKVEIKS GGGGS EVQLVESGGG LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDE</td><td>YYADSSXe^ SGGGS^b^ GvpsaJSls#· LVQPS^LK* KNTAYLÓMtT</td>
<img file="MX349396B_D0109.tif" />
<td></td><td></td><td></td><td></td><td></td><td colspan="2">NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL·</td><td></td>
<td> 801</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td></td><td></td>
<td> 802</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td></td><td></td>
<td> 803</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td><td></td>
<td> 804</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VL CDR1</td><td>aa</td><td>RASQGISNHLN</td><td></td><td></td>
<td> 805</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 806</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VL CDR3</td><td>aa</td><td>QQYFDRPYT</td><td></td><td></td>
<td> 807</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td></td>
<td> 808</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGSGS GTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td><td></td>
<td> 809</td><td>BCMA-81</td><td>BC E5-33G12-A10</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIK</td><td> 216</td>
<td> 810</td><td>BCMA-81 HL x CD3 HL</td><td>BC E5-33G12-A10 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYY FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSG GSDIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGV GSGTDFTLTISSLQPEDFATYYCQQYFDRPYTFGGGTKVEIKSGGGGSEVQLVESGGGLV LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTC PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKA QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td>ADSVKGR GGGSGGG PSRFSGS 2PGGSLK rAYLQI^T. EPSLTV®. ALTLSEy,</td><td></td>
<td> 811</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td>L J <iCAN< eiEDAl ISTRIAi</td><td rowspan="2"></td>
<td> 812</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td></td>
<td> 813</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 814</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VLCDR1</td><td>aa</td><td colspan="2">EASQGISNHLN</td>
<td> 815</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 816</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VLCDR3</td><td>aa</td><td colspan="2">QQYSNLPYT</td>
<td> 817</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSC7KASGFTFSNFDMAWVEQAPGKGLVWVSSITTGGGDTYYADSVKGE FTISEDNAKNTLYLQMNSLEAEDTAVYYCVEHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 818</td><td>BCMA-82</td><td>BC E5-33A11-B8</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDEVTISCEASQGISNHLNWFQQKPGEAPKPLIYYTSNLQSGVPSEFSGSGS GTDFTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIK</td>
<td> 819</td><td>BCMA-82</td><td>BC E5-33- A11-B8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVEQAPGKGLVWVSSITTGGGDTYYADSVKGE FTISEDNAKNTLYLQMNSLEAEDTAVYYCVEHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDEVTISCEASQGISNHLNWFQQKPGEAPKPLIYYTSNLQSGVPSEFSGS GSGTDFTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIK</td>
<td> 820</td><td>BCMA-82 HL xCD3 HL</td><td>BC E5-33A11-B8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGE ftisednakntlylqmnsleaedtavyycvehgyydgyhlfdywgqgtlvtvssggggsggggsggg GSDIQMTQSPSSLSASVGDEVTISCEASQGISNHLNWFQQKPGEAPKPLIYYTSNLQSGVPSRFSGS σεστΌΡΤΕΤιεβηςρΕϋΡΑΤΥΥσοΰΥεΝΕΡΥΤΡΟοστκνΕίκεσοοσεΕνοΕνΕΒσοσι,νοροσΞΕΚ LSCAASGFTFNKYAMNWVRQAPGKGLEWVAEIESKYNNYATYYADSVKDEFTISEDDSKNTAYLQMN NLKTEDTAVYYCVEHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPEGLIGGTKFLAPGTPAEFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNEWVFGGGTKLTVL</td>
<td> 821</td><td>BCMA-83</td><td>BC E5-33- B11-B8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 822</td><td>BCMA-83</td><td>BC E5-33- B11-B8</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td></td>
<td> 823</td><td>BCMA-83</td><td>BC E5-33- B11-B8</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td></td>
<td> 824</td><td>BCMA-83</td><td>BC E5-33- B11-B8</td><td>VL CDR1</td><td>aa</td><td>EASQGISNHLN</td><td>i<sup>3</sup>* ce .</td>
<td> 825</td><td>BCMA-83</td><td>BC E5-33- B11-B8</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td>ICANC PISCAD STRIAL ___1</td>
<td> 826</td><td>BCMA-83</td><td>BC E5-33-</td><td>VL CDR3</td><td>aa</td><td>QQYSNLPYT</td><td></td>
<td colspan="6"></td><td></td>
217
<td></td><td></td><td>B11-B8</td><td></td><td></td><td colspan="2"></td>
<td> 827</td><td>BCMA-83</td><td>BC E5-33B11-B8</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVS S</td>
<td> 828</td><td>BCMA-83</td><td>BC E5-33B11-B8</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIK</td>
<td> 829</td><td>BCMA-83</td><td>BC E5-33B11-B8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIK</td>
<td> 830</td><td>BCMA-83 HL x CD3 HL</td><td>BC E5-33B11-B8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQGISNHLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 831</td><td>BCMA-84</td><td>BC E5-33G12-B8</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 832</td><td>BCMA-84</td><td>BC E5-33G12-B8</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 833</td><td>BCMA-84</td><td>BC E5-33G12-B8</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 834</td><td>BCMA-84</td><td>BC E5-33- G12-B8</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNHLN</td>
<td> 835</td><td>BCMA-84</td><td>BC E5-33- G12-B8</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td>
<td> 836</td><td>BCMA-84</td><td>BC E5-33- G12-B8</td><td>VL CDR3</td><td>aa</td><td>QQYSNLPYT</td><td></td>
<td> 837</td><td>BCMA-84</td><td>BC E5-33G12-B8</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTl· FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td><td>g ω nuoMv</td>
<td> 838</td><td>BCMA-84</td><td>BC E5-33G12-B8</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGvisRFff^^· GTDFTLTISSLQPEDFATYYCQQYSNLPYTFGGGTKVEIK I /iVX</td>
218
<td> 839</td><td>BCMA-84</td><td>BC E5-33- G12-B8</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDFTLTIS SLQPEDFATYYCQQYSNLPYTFGGGTKVEIK</td>
<td> 840</td><td>BCMA-84 HL X CD3 HL</td><td>BC E5-33G12-B8HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGRSLRLSCAASGFTFSNFDMAWVRQAPAKGLEWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGERVTITCRASQGISNHLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS α3ΟΤΏΡΤΕΤΙ3ΞΒ0ΡΕΟΡΑΤΥΥθς0Υ3ΝΕΡΥΤΡΟθσΤΚνΕΙΚ3Οθα63Εν0ΕνΕ3σασΐ<sub>1</sub>νςΡαα3ΕΚ LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 841</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFGMN</td>
<td> 842</td><td>BCMA-85</td><td>BC C6-97- G5</td><td>VH CDR2</td><td>aa</td><td colspan="2">WINTYTGE SIYADDFKG</td>
<td> 843</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VH CDR3</td><td>aa</td><td colspan="2">GGVYGGYDAMDY</td>
<td> 844</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQDISNYLN</td>
<td> 845</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHS</td>
<td> 846</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQGNTLPWT</td>
<td> 847</td><td>BCMA-85</td><td>BC C6-97- G5</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 848</td><td>BCMA-85</td><td>BC C6-97G5</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSF GTDYTLTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIK</td><td>.FSGSGS</td>
<td> 849</td><td>BCMA-85</td><td>BC C6-97G5</td><td>scFv</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYí FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGG GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVE GSGTDYTLTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIK</td><td>Λ DDFKGR4 3GSGGK S<sup>R</sup>FS^</td>
<td> 850</td><td>BCMA-85 HL xCD3HL</td><td>BC C6-97- G5 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGW1NTYTGESIY7 FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDTVMDYWGQGTLVTVSSGGGGSGC</td><td>DDFK^P GGSGg<?<</td>
NJ
ΙΟ
<td></td><td></td><td>XCD3HL</td><td>ca</td><td></td><td>GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEPEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN nlktedtavyycvrhgnfgnsyisywaywgqgtlvtvssggggsggggsggggsqtwtqepsltvs PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 851</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VH CDR1</td><td>aa</td><td>NFGMN</td>
<td> 852</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VH CDR2</td><td>aa</td><td>WINTYTGESIYADDFKG</td>
<td> 853</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td>
<td> 854</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VLCDR1</td><td>aa</td><td>RASQDISNYLN</td>
<td> 855</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td>
<td> 856</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td>
<td> 857</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 858</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>VL</td><td>aa</td><td>DIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGSGS GTDYSLTISNLQPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 859</td><td>BCMA-86</td><td>BC C6-98-C8</td><td>scFv</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 860</td><td>BCMA-86 HL XCD3HL</td><td>BC C6-98-C8 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSfGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQQGNTLPWTFGQGTKVETKSGGGGSEVQLVESGGGllzQPGGSnK· LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSI®JTAYI^lte nlktedtavyycvrhgnfgnsyisywaywgqgtlvtvssggggsggggsggggsqtw'Jqepsj^iS pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggmaalt^cpíQPEDEAEYYCVLWYSNRWVFGGGTKLTVL i JgP *</td>
<td> 861</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VH CDR1</td><td>aa</td><td>NFGMN |</td>
220
<td> 862</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VH CDR2</td><td>aa</td><td colspan="2">WINTYTGESIYADDFKG</td>
<td> 863</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VH CDR3</td><td>aa</td><td colspan="2">GGVYGGYDAMDY</td>
<td> 864</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQDISNYLN</td>
<td> 865</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHS</td>
<td> 866</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQGNTLPWT</td>
<td> 867</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVF SLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVS S</td>
<td> 868</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGSGS GTDYTLTISSLEQEDIATYFCQQGNTLPWTFGQGTKVEIK</td>
<td> 869</td><td>BCMA-87</td><td>BC C6-97-A6</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEQEDIATYFCQQGNTLPWTFGQGTKVEIK</td>
<td> 870</td><td>BCMA-87 HL x CD3 HL</td><td>BC C6-97-A6 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEQEDIATYFCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 871</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VH CDR1</td><td>aa</td><td>NFGMN</td><td></td>
<td> 872</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VH CDR2</td><td>aa</td><td>WINTYTGESIYADDFKG</td><td> * -2 3</td>
<td> 873</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td><td></td>
<td> 874</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VL CDR1</td><td>aa</td><td>RASQDISNYLN</td><td>¡Ir</td>
<td> 875</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td><td>’cr, J</td>
221
BC C6-98C8-E3
876
BCMA-88
VL CDR3
QSFATLPWT aa
<td> 877</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSS</td><td></td>
<td> 878</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGSGS GTDYSLTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIK</td><td></td>
<td> 879</td><td>BCMA-88</td><td>BC C6-98C8-E3</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIK</td><td></td>
<td> 880</td><td>BCMA-88 HL x CD3 HL</td><td>BC C6-98C8-E3 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDTSNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td></td>
<td> 881</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VH CDR1</td><td>aa</td><td>NFGMN</td><td></td><td>bJ NJ NJ</td>
<td> 882</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VH CDR2</td><td>aa</td><td>WINTYTGESIYADDFKG</td><td></td><td></td>
<td> 883</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td><td></td><td></td>
<td> 884</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VL CDR1</td><td>aa</td><td>RASQDISNYLN</td><td></td><td></td>
<td> 885</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td><td></td><td></td>
<td> 886</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VL CDR3</td><td>aa</td><td>QSFATLPWT</td><td>1 Λ NSTm DE</td><td></td>
<td> 887</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESn FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td><td></td><td></td>
<td> 888</td><td>BCMA-89</td><td>BC C6-98- A1-E3</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPÍ GTDYTFTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIK</td><td>RFScH^i</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td> 889</td><td>BCMA-89</td><td>BC C6-98A1-E3</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTFTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIK</td>
<td> 890</td><td>BCMA-89 HL x CD3 HL</td><td>BC C6-98A1-E3 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTFTISNLQPEDIATYYCQSFATLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 891</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFGMN</td>
<td> 892</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VH CDR2</td><td>aa</td><td colspan="2">WINTYTGESIYADDFKG</td>
<td> 893</td><td>BCMA-90</td><td>BC C6-97- G5-E3</td><td>VH CDR3</td><td>aa</td><td colspan="2">GGVYGGYDAMDY</td>
<td> 894</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VLCDR1</td><td>aa</td><td colspan="2">RASQDISNYLN</td>
<td> 895</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHS</td>
<td> 896</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VL CDR3</td><td>aa</td><td colspan="2">QSFATLPWT</td>
<td> 897</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 898</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPS GTDYTLTISSLEPEDIATYYCQSFATLPWTFGQGTKVEIK</td><td>IFSGSGS i*</td>
<td> 899</td><td>BCMA-90</td><td>BC C6-97G5-E3</td><td>scFv</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIY FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSG GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGV GSGTDYTLTISSLEPEDIATYYCQSFATLPWTFGQGTKVEIK</td><td>WDFKMt > 3GGSGS$l <sup>psre</sup>M ík.</td>
<td> 900</td><td>BCMA-90 HL x CD3 HL</td><td>BC C6-97- G5-E3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIl· FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGS(</td><td>addf'kg'R GGGS/jgCl</td>
<td></td><td></td><td>x CD3 HL</td><td>ca</td><td></td><td colspan="2">GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEPEDIATYYCQSFATLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td rowspan="11">224 _ _____ ___Τΐιητ x</td>
<td> 901</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFGMN</td>
<td> 902</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VH CDR2</td><td>aa</td><td colspan="2">WINTYTGESIYADDFKG</td>
<td> 903</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VH CDR3</td><td>aa</td><td colspan="2">GGVYGGYDAMDY</td>
<td> 904</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQDISNYLN</td>
<td> 905</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHS</td>
<td> 906</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VL CDR3</td><td>aa</td><td colspan="2">QSFATLPWT</td>
<td> 907</td><td>BCMA-91</td><td>BC C6-97- A6-E3</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVS CKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 908</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGSGS GTDYTLTISSLEQEDIATYFCQSFATLPWTFGQGTKVEIK</td>
<td> 909</td><td>BCMA-91</td><td>BC C6-97A6-E3</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEQEDIATYFCQSFATLPWTFGQGTKVEIK</td>
<td> 910</td><td>BCMA-91 HL xCD3 HL</td><td>BC C6-97A6-E3 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESI FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGS GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSG GSGTDYTLTISSLEQEDIATYFCQSFATLPWTFGQGTKVEIKSGGGGSEVQLVESGGGL LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSK NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWT PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGK QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td><td><sup>r</sup>ADDFKGR ÍGGGSGJ^· rPSRF§3$L ^qpgg|§i< ΙΤΑΥΚβέίΓ kALTEBSV</td>
<td> 911</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VH CDR1</td><td>aa</td><td>' I ' ' ' ,. , , ,.— . - . NFGMN</td>
<td> 912</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VH CDR2</td><td>aa</td><td>WINTYTGESIYADDFKG</td>
<td> 913</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td>
<td> 914</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VL CDR1</td><td>aa</td><td>RASQDISNYLN</td>
<td> 915</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td>
<td> 916</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VL CDR3</td><td>aa</td><td>QHFRTLPWT</td>
<td> 917</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 918</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSRFSGSGS GTDYTLTISSLEPEDIATYYCQHFRTLPWTFGQGTKVEIK</td>
<td> 919</td><td>BCMA-92</td><td>BC C6-97G5-G9</td><td>scFv</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR fvfsldtsvttaylqinslkdedtavyycarggvyggydamdywgqgtlvtvssggggsggggsggg GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEPEDIATYYCQHFRTLPWTFGQGTKVEIK</td>
<td> 920</td><td>BCMA-92 HL XCD3HL</td><td>BC C6-97G5-G9 HL XCD3HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASLGDRVTITCRASQDISNYLNWYQQKPDKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEPEDIATYYCQHFRTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN ΝΕΚΤΕϋΤΑλ7ΥγσνρΗσΝΡσΝ8ΥΐεΥΜΑΥΝσαστΕντν88σσασεσσοσεβσσσεοτννταΕΡει,τνε pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkáaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL | y</td>
<td> 921</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VH CDR1</td><td>aa</td><td>J > NFGMN |</td>
<td> 922</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VH CDR2</td><td>aa</td><td>- WINTYTGESIYADDFKG j ______________________________________________________________________________1</td>
<td> 923</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY ’ k-</td>
<td> 924</td><td>BCMA-93</td><td>BC C6-98-</td><td>VL CDR1</td><td>aa</td><td>RASQDISNYLN /ΛΧ1</td>
NJ NJ en
<img file="MX349396B_D0110.tif" />
<td></td><td></td><td>C8-G9</td><td></td><td></td><td colspan="2"> ' — ' ----------------</td>
<td> 925</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSRLHS</td>
<td> 926</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VL CDR3</td><td>aa</td><td colspan="2">QHFRTLPWT</td>
<td> 927</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VH</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 928</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGSGS GTDYSLTISNLQPEDIATYYCQHFRTLPWTFGQGTKVEIK</td>
<td> 929</td><td>BCMA-93</td><td>BC C6-98C8-G9</td><td>scFv</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQHFRTLPWTFGQGTKVEIK</td>
<td> 930</td><td>BCMA-93 HL x CD3 HL</td><td>BC C6-98C8-G9 HL xCD3HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINSLKAEDTAVYFCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQTPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKALKLLIYYTSRLHSGVPSRFSGS GSGTDYSLTISNLQPEDIATYYCQHFRTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 931</td><td>BCMA-94</td><td>BC C6-97- A6-G9</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFGMN</td>
<td> 932</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VH CDR2</td><td>aa</td><td colspan="2">WINTYTGESIYADDFKG</td>
<td> 933</td><td>BCMA-94</td><td>BC C6-97- A6-G9</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td><td> ______24·</td>
<td> 934</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VLCDR1</td><td>aa</td><td>RASQDISNYLN</td><td></td>
<td> 935</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td><td>11 O MU Λ ruoi INDI*'</td>
<td> 936</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VL CDR3</td><td>aa</td><td>QHFRTLPWT</td><td>’ 1 CANO Udad</td>
<td> 937</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESI FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td><td><sup>r</sup>ADDKí^J</td>
226
<td> 938</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>VL</td><td>aa</td><td colspan="3">ΏΙ0ΜΤ03Ρ33ΕεΑ3νθΌΕνΤΙΤ0ΕΑ30ΌΙ3ΝΥΕΝΝΥ00ΚΡΘΚΑΡΚΒΕΙΥΥΤ3ΕΒΗ3ΘνΡ3ΕΡΞΟΞΟ3 GTDYTLTIS S LEQEDIATYFCQH FRTLPWTFGQGTKVEIK</td>
<td> 939</td><td>BCMA-94</td><td>BC C6-97A6-G9</td><td>scFv</td><td>aa</td><td colspan="3">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR fvfsldtsvttaylqinslkdedtavyycarggvyggydamdywgqgtlvtvssggggsggggsggg GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEQEDIATYFCQHFRTLPWTFGQGTKVEIK</td>
<td> 940</td><td>BCMA-94 HL x CD3 HL</td><td>BC C6-97A6-G9 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="3">QVQLVQSGSELKKPGASVKVSCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSLDTSVTTAYLQINSLKDEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTLTISSLEQEDIATYFCQHFRTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL·</td>
<td> 941</td><td>BCMA-95</td><td>BC C6-98- A1-G9</td><td>VH CDR1</td><td>aa</td><td colspan="3">NFGMN</td>
<td> 942</td><td>BCMA-95</td><td>BC C6-98A1-G9</td><td>VH CDR2</td><td>aa</td><td colspan="3">WINTYTGE SIYADDFKG</td>
<td> 943</td><td>BCMA-95</td><td>BC C6-98- A1-G9</td><td>VH CDR3</td><td>aa</td><td colspan="3">GGVYGGYDAMDY</td>
<td> 944</td><td>BCMA-95</td><td>BC C6-98- A1-G9</td><td>VL CDR1</td><td>aa</td><td colspan="3">RASQDISNYLN</td>
<td> 945</td><td>BCMA-95</td><td>BC C6-98A1-G9</td><td>VL CDR2</td><td>aa</td><td colspan="3">YTSRLHS</td>
<td> 946</td><td>BCMA-95</td><td>BC C6-98- A1-G9</td><td>VL CDR3</td><td>aa</td><td colspan="3">QHFRTLPWT</td>
<td> 947</td><td>BCMA-95</td><td>BC C6-98A1-G9</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESI FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td><td colspan="2">'ADDFKGR</td>
<td> 948</td><td>BCMA-95</td><td>BC C6-98- A1-G9</td><td>VL</td><td>aa</td><td>ΟΙ0ΜΤ03Ρ33Ε3Α3νΘΟΚνΤΙ3ΰΕΑ30ΟΙ3ΝΥΕΝΝΥ00ΚΡσΚΑΡΚΕΕΙΥΥΤ3ΚΕΗ3σνΡ GTDYTFTISNLQPEDIATYFCQHFRTLPWTFGQGTKVEIK</td><td>JRFSGg c</td><td></td>
<td rowspan="2"> 949</td><td rowspan="2">BCMA-95</td><td rowspan="2">BC C6-98A1-G9</td><td rowspan="2">scFv</td><td rowspan="2">aa</td><td rowspan="2">QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESI FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGS GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSG GSGTDYTFTISNLQPEDIATYFCQHFRTLPWTFGQGTKVEIK</td><td></td><td></td>
<td>MOQUAu MDuenftAL Q o ω _</td><td> 8“</td>
227
<td> 950</td><td>BCMA-95 HL xCD3 HL</td><td>BC C6-98A1-G9 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTFTISNLQPEDIATYFCQHFRTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGS STGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSG SLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 951</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VH CDR1</td><td>aa</td><td>NFGMN</td>
<td> 952</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VH CDR2</td><td>aa</td><td>WINTYTGESIYADDFKG</td>
<td> 953</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VH CDR3</td><td>aa</td><td>GGVYGGYDAMDY</td>
<td> 954</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VL CDR1</td><td>aa</td><td>RASQDISNYLN</td>
<td> 955</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VL CDR2</td><td>aa</td><td>YTSRLHS</td>
<td> 956</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VL CDR3</td><td>aa</td><td>QQGNTLPWT</td>
<td> 957</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VH</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSS</td>
<td> 958</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>VL</td><td>aa</td><td>DIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGSGS GTDYTFTISNLQPEDI AT YYCQQGNTLPWT FGQGTKVEIK</td>
<td> 959</td><td>BCMA-96</td><td>BC C6 98-A1</td><td>scFv</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVPSRFSGS GSGTDYTFTISNLQPEDIATYYCQQGNTLPWTFGQGTKVEIK</td>
<td> 960</td><td>BCMA-96 HL X CD3 HL</td><td>BC C6 98-A1 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td>QVQLVQSGSELKKPGASVKISCKASGYTFTNFGMNWVRQAPGQGLEWMGWINTYTGESIYADDFKGR FVFSSDTSVSTAYLQINNLKAEDTAVYYCARGGVYGGYDAMDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTISCRASQDISNYLNWYQQKPGKAPKLLIYYTSRLHSGVP 5RFSGS GSGTDYTFTISNLQPEDIATYYCQQGNTLPWTFGQGTKVEIKSGGGGSEVQLVESGGGLVQ ?GGSLK3 LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNT kYLQMgl NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQE PSLTysf pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaAtls^^ QPEDEAEYYCVLWYSNRWVFGGGTKLTVL |</td>
228 o
¡y
<td> 961</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 962</td><td>BCMA-97</td><td>BC B12-33- G2-B2</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 963</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 964</td><td>BCMA-97</td><td>BC B12-33- G2-B2</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNNLN</td>
<td> 965</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 966</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQFTSLPYT</td>
<td> 967</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>VH</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 968</td><td>BCMA-97</td><td>BC B12-33- G2-B2</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK</td>
<td> 969</td><td>BCMA-97</td><td>BC B12-33G2-B2</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK</td>
<td> 970</td><td>BCMA-97 HL x CD3 HL</td><td>BC B12-33- G2-B2 HL xCD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMNSLRAEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL ,</td>
<td> 971</td><td>BCMA-98</td><td>BC B12-33- A4-B2</td><td>VH CDR1</td><td>aa</td><td>NFDMA</td><td>3C! UI1SN</td>
<td> 972</td><td>BCMA-98</td><td>BC B12-33- A4-B2</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYADSVKG</td><td>I</td>
<td> 973</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td>P1 hCA* REDAÍ Estría i</td>
<td> 974</td><td>BCMA-98</td><td>BC B12-33-</td><td>VL CDR1</td><td>aa</td><td>RANQGISNNLN</td><td> —</td>
229
<td></td><td></td><td>A4-B2</td><td></td><td></td>
<td> 975</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>VL CDR2</td><td>aa</td>
<td> 976</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>VL CDR3</td><td>aa</td>
<td> 977</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>VH</td><td>aa</td>
<td> 978</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>VL</td><td>aa</td>
<td> 979</td><td>BCMA-98</td><td>BC B12-33A4-B2</td><td>scFv</td><td>aa</td>
<td> 980</td><td>BCMA-98 HL x CD3 HL</td><td>BC B12-33A4-B2 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td>
<td> 981</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VH CDR1</td><td>aa</td>
<td> 982</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VH CDR2</td><td>aa</td>
<td> 983</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VH CDR3</td><td>aa</td>
<td> 984</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VL CDR1</td><td>aa</td>
<td> 985</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VL CDR2</td><td>aa</td>
<td> 986</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VL CDR3</td><td>aa</td>
<td> 987</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VH</td><td>aa</td>
YTSNLQS
QQFTSLPYT
ΕνΟΕνΕβΟσσί,νΟΡΟΟβΙιΕΕβαΑΑβΘΡΤΕ^ΝΡϋΜΑΝνΕΟΑΡβΚΘΕνΝνεείΤΤσσσϋΤΥΥΆΟδνΚΟΕ FTISRDNAKSTLYLQMDSLESEDTAVYYCVEHGYYDGYHLFDYWGQGTLVTVS S
DIQMTQSPSSLSASVGDRVTITCRANQGISNNLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKSTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRANQGISNNLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKSTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSLSASVGDRVTITCRANQGISNNLNWYQQKPGKAPKPLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL
NFDMA
SITTGGGDTYYADSVKG
HGYYDGYHLFDY
RASQGISNNLN
YTSNLQS
QQFTSLPYT
IdWI
<img file="MX349396B_D0111.tif" />
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSV
FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSS I
<td> 988</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>VL</td><td>aa</td><td colspan="2">DIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGSGS GTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK</td><td rowspan="10">NJ UJ</td>
<td> 989</td><td>BCMA-99</td><td>BC B12-33A5-B2</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIK</td>
<td> 990</td><td>BCMA-99 HL XCD3HL</td><td>BC B12-33A5-B2 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="2">EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTYYADSVKGR FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFTSLPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS pggtvtltcgsstgavtsgnypnwvqqkpgqaprgliggtkflapgtparfsgsllggkaaltlsgv QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 991</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VH CDR1</td><td>aa</td><td colspan="2">NFDMA</td>
<td> 992</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYADSVKG</td>
<td> 993</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VH CDR3</td><td>aa</td><td colspan="2">HGYYDGYHLFDY</td>
<td> 994</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VL CDR1</td><td>aa</td><td colspan="2">RASQGISNNLN</td>
<td> 995</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VL CDR2</td><td>aa</td><td colspan="2">YTSNLQS</td>
<td> 996</td><td>BCMA-100</td><td>BC B12-33- A5-C10</td><td>VL CDR3</td><td>aa</td><td colspan="2">QQFAHLPYT</td>
<td> 997</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VH</td><td>aa</td><td>EVQLVESGGGLVQPGGSLRLSCAASGFTFSNFDMAWVRQAPGKGLVWVSSITTGGGDTY' FTISRDNAKNTLYLQMD SLRS EDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVS S</td><td>ADSVKGR</td>
<td> 998</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>VL</td><td>aa</td><td>DIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVP GTDYTLTISSLQPEDFATYYCQQFAHLPYTFGQGTKLEIK</td><td>JRFSGfgS^</td><td></td>
<td> 999</td><td>BCMA-100</td><td>BC B12-33A5-C10</td><td>scFv</td><td>aa</td><td>EVQLVE SGGGLVQPGGSLRLS CAASGFTFSNFDMAWVRQAPGKGLVWVS SITTGGGDTY FTISRDNAKNTLYLQMDSLRSEDTAVYYCVRHGYYDGYHLFDYWGQGTLVTVS SGGGGS GSDIQMTQSPSSMSASVGDRVTITCRASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSG GSGTDYTLTISSLQPEDFATYYCQQFAHLPYTFGQGTKLEIK</td><td>'ADS-Í^Ir' sgggsGSg^ ZPSREasS?</td><td>i</td>
<td> 1000</td><td>BCMA-100 HLxCD3 HL</td><td>BC B12-33A5-C10 HL x CD3 HL</td><td>bispecific molecule</td><td>aa</td><td colspan="3">EVQLVESGGGLVQPGGSLELSCAASGFTFSNFDMAWVEQAPGKGLVWVSSITTGGGDTYYADSVKGE FTISEDNAKNTLYLQMDSLESEDTAVYYCVEHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGGG GSDIQMTQSPSSMSASVGDEVTITCEASQGISNNLNWYQQKPGKAPKSLIYYTSNLQSGVPSRFSGS GSGTDYTLTISSLQPEDFATYYCQQFAHLPYTFGQGTKLEIKSGGGGSEVQLVESGGGLVQPGGSLK LSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMN NLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTWTQEPSLTVS PGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPEGLIGGTKFLAPGTPAEFSGSLLGGKAALTLSGV QPEDEAEYYCVLWYSNRWVFGGGTKLTVL</td>
<td> 1001</td><td colspan="2">BCMA humano</td><td>humano</td><td>na</td><td colspan="3">atgttgcagatggctgggcagtgctcccaaaatgaatattttgacagtttgttgcatgcttgcatac cttgtcaacttcgatgttcttctaatactcctcctctaacatgtcagcgttattgtaatgcaagtgt gaccaattcagtgaaaggaacgaatgcgattctctggacctgtttgggactgagcttaataatttct ttggcagttttcgtgctaatgtttttgctaaggaagataaactctgaaccattaaaggacgagttta aaaacacaggatcaggtctcctgggcatggctaacattgacctggaaaagagcaggactggtgatga aattattcttccgagaggcctcgagtacacggtggaagaatgcacctgtgaagactgcatcaagagc aaaccgaaggtcgactctgaccattgctttccactcccagctatggaggaaggcgcaaccattcttg tcaccacgaaaacgaatgactattgcaagagcctgccagctgctttgagtgctacggagatagagaa atcaatttctgctaggtaa</td>
<td> 1002</td><td colspan="2">BCMA humano</td><td>humano</td><td>aa</td><td colspan="3">MLQMAGQCSQNEYFDSLIjHACIPCQLRCSSNTPPLTCQRYCNASVTNSVKGTNAILWTCLGLSLIIS ΙΑνΡνηΜΕ^ΕΚΙΝΒΕΡΕΚΌΕΓΚΝΤΰΞΘΕΕαΜΑΝίυΕΕΚδΕΤΟΌΕΙΙΙ,ΡΕΟΏΕΥΤνΕΕσΓΟΕΟΟΙΚδ KPKVDSDHCFPLPAMEEGATILVTTKTNDYCKSLPAALSATEIEKSISAE</td>
<td> 1003</td><td colspan="2">BCMA murine</td><td>murine</td><td>na</td><td colspan="3">atggcgcaacagtgtttccacagtgaatattttgacagtctgctgcatgcttgcaaaccgtgtcact tgcgatgttccaaccctcctgcaacctgtcagccttactgtgatccaagcgtgaccagttcagtgaa agggacgtacacggtgctctggatcttcttggggctgaccttggtcctctctttggcacttttcaca atetcattcttgctgaggaagatgaaccccgaggccctgaaggacgagcctcaaagcccaggtcago ttgacggatcggctcagctggacaaggccgacaccgagctgactaggatcagggctggtgacgacag gatctttccccgaagcctggagtatacagtggaagagtgcacctgtgaggactgtgtcaagagcaaa cccaagggggattctgaccatttcttcccgcttccagccatggaggagggggcaaccattjcttgtca ccacaaaaacgggtgactacggcaagtcaagtgtgccaactgctttgcaaagtgtcatgtJgga tgc^j, gaagccaactcacactagataa j</td>
<td> 1004</td><td colspan="2">BCMA murine</td><td>murine</td><td>aa</td><td>MAQQCFHSEYFDSLLHACKPCHLECSNPPATCQPYCDPSVTSSVKGTYTVLWIFLGLTL ISFLLEKMNPEALKDEPQSPGQLDGSAQLDKADTELTEIEAGDDEIFPESLEYTVEECT PKGDSDHFFPLPAMEEGATILVTTKTGDYGKSSVPTALQSVMGMEKPTHTE</td><td colspan="2">IEDC-\^K</td>
<td> 1005</td><td colspan="2">BCMA de macaco</td><td>rhesus</td><td>na</td><td>atgttgcagatggctcggcagtgctcccaaaatgaatattttgacagtttgttgcatga cttgtcaacttcgatgttctagtactcctcctctaacatgtcagcgttattgcaatgca caattcagtgaaaggaatgaatgcgattctctggacctgtttgggactgagcttgataa</td><td colspan="2">Ltgcáá^i?' igtat^c^</td>
<td colspan="6"></td><td></td><td></td>
232
<td></td><td></td><td></td><td></td>
<td> 1006</td><td>BCMA de macaco</td><td>rhesus</td><td>aa</td>
<td> 1007</td><td>ECD BCMA hu= posiciones 1-54 de SEQ ID NO: 1002</td><td>humano</td><td>aa</td>
<td> 1008</td><td>ECD BCMAmu= posiciones 1-49 de SEQ ID NO: 1004</td><td>murine</td><td>aa</td>
<td> 1009</td><td>ECD BCMAhu/E1 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1010</td><td>ECD BCMAhu/E2 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1011</td><td>ECD BCMAhu/E3 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1012</td><td>ECD BCMA hu / E4 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1013</td><td>ECD BCMA hu / E5 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1014</td><td>ECD BCMAhu/E6 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1015</td><td>ECD BCMAhu/E7 murine</td><td>chimerical hu / mu</td><td>aa</td>
<td> 1016</td><td>clúster de epítopes 3 de BCMAhu</td><td>humano</td><td>aa</td>
<td> 1017</td><td>clúster de epítopes 3 de BCMAma</td><td>macaco</td><td>aa</td>
<td> 1018</td><td>clúster de epítopes 1 de BCMAhu</td><td>humano</td><td>aa</td>
<td> 1019</td><td>clúster de epítopes 4 de BCMAhu</td><td>humano</td><td>aa</td>
<td> 1020</td><td>clúster de epítopes 1 de BCMA ma</td><td>macaco</td><td>aa</td>
<td colspan="2">gcagttttcgtgctaacgtttttgctaaggaagatgagctctgaaccattaaaggatgagtttaaaa acacaggatcaggtctcctgggcatggctaacattgacctggaaaagggcaggactggtgatgaaat tgttcttccaagaggcctggagtacacggtggaagaatgcacctgtgaagactgcatcaagaataaa ccaaaggttgattctgaccattgctttccactcccagccatggaggaaggcgcaaccattctcgtca ccacgaaaacgaatgactattgcaatagcctgtcagctgctttgagtgttacggagatagagaaatc aatttctgctaggtaa</td>
<td colspan="2">MLQMARQCSQNEYFDSIjLHDCKPCQLRCSSTPPLTCQRYCNASMTNSVKGMNAILWTCLGLSLIISL ΑνΡνΕΤΓΕΕΕΚΜ33ΕΡΕΚΟΕΡΚΝΤσ3σΕΕαΜΑΝΙΟΕΕΚαΕΤΟϋΕΐνΕΡΗΟΕΕΥΤνΕΕσΤΟΕΌΟΙΚΝΚ PKVDSDHCFPLPAMEEGATILVTTKTNDYCNSLSAALSVTEIEKSISAR</td>
<td colspan="2">MLQMAGQCSQNEYFDSLLHACIPCQLRCSSNTPPLTCQRYCNASVTNSVKGTNA</td>
<td colspan="2">MAQQCFHSEYFDSIjLiHACKPCHLRCSNPPATCQPYCDPSVTSSVKGTYT</td>
<td colspan="2">MAQQCSQNEYFDSLLHACIPCQLRCSSNTPPLTCQRYCNASVTNSVKGTNA</td>
<td colspan="2">ΜΕαΜΑΟ0σΓΗ3ΕΥΡΟ3ΕΕΗΑσΐΡ00ΕΚΟ33ΝΤΡΡΕΤΟ0ΕΥΌΝΑ3νΤΝ3νΚ6ΤΝΑ</td>
<td colspan="2">ΜΕ0ΜΑσ0€30ΝΕΥΡΟ3ΕΕΗΑσΐΡσΗΕΡσ3ΝΡΡΑΤσ0ΡΥεΝΑ3νΤΝ3νκσΤΝΑ</td>
<td colspan="2">ΜΕΟΜΑΟΟ€30ΝΕΥΡΌ3ΕΕΗΑσΐΡΟΟΕΡε33ΝΤΡΡΕΤΟΟΡΥσΌΡ3νΤ33νκσΤΥΤ</td>
<td colspan="2">MLQMAGQCSQNEYFDSLLHACKPCQLRCSSNTPPLTCQRYCNASVTNSVKGTNA</td>
<td colspan="2">MLQMAGQCSQNEYFDSLLHACIPCHLRCSSNTPPLTCQRYCNASVTNSVKGTNA</td>
<td colspan="2">MLQMAGQCSQNEYFDSLLHACIPCQLRCSSNTPPLTCQPYCNASVTNSVKGTNA</td>
<td colspan="2">CQLRCSSNTPPLTCQRYC</td>
<td>CQLRCSSTPPLTCQRYC</td><td></td>
<td>MLQMAGQ</td><td>__4S'</td>
<td>NASVTNSVKGTNA</td><td>11 DMIX1 * PM*</td>
<td>MLQMARQ</td><td>i ? TO</td>
<td></td><td></td>
Μ
<td> 1021</td><td colspan="2">clúster de epítopes 4 de BCMA ma</td><td>macaco</td><td>aa</td>
<td> 1022</td><td>BCMA-101</td><td>BC 5G9</td><td>VH CDR1</td><td>aa</td>
<td> 1023</td><td>BCMA-101</td><td>BC 5G9</td><td>VH CDR2</td><td>aa</td>
<td> 1024</td><td>BCMA-101</td><td>BC 5G9</td><td>VH CDR3</td><td>aa</td>
<td> 1025</td><td>BCMA-101</td><td>BC 5G9</td><td>VLCDR1</td><td>aa</td>
<td> 1026</td><td>BCMA-101</td><td>BC 5G9</td><td>VL CDR2</td><td>aa</td>
<td> 1027</td><td>BCMA-101</td><td>BC 5G9</td><td>VLCDR3</td><td>aa</td>
<td> 1028</td><td>BCMA-101</td><td>BC 5G9</td><td>VH</td><td>aa</td>
<td> 1029</td><td>BCMA-101</td><td>BC 5G9</td><td>VL</td><td>aa</td>
<td> 1030</td><td>BCMA-101</td><td>BC 5G9</td><td>scFv</td><td>aa</td>
<td> 1031</td><td>BCMA-102</td><td>BC 244-A7</td><td>VH CDR1</td><td>aa</td>
<td> 1032</td><td>BCMA-102</td><td>BC 244-A7</td><td>VH CDR2</td><td>aa</td>
<td> 1033</td><td>BCMA-102</td><td>BC 244-A7</td><td>VH CDR3</td><td>aa</td>
<td> 1034</td><td>BCMA-102</td><td>BC 244-A7</td><td>VLCDR1</td><td>aa</td>
<td> 1035</td><td>BCMA-102</td><td>BC 244-A7</td><td>VL CDR2</td><td>aa</td>
<td> 1036</td><td>BCMA-102</td><td>BC 244-A7</td><td>VLCDR3</td><td>aa</td>
<td> 1037</td><td>BCMA-102</td><td>BC 244-A7</td><td>VH</td><td>aa</td>
<td> 1038</td><td>BCMA-102</td><td>BC 244-A7</td><td>VL</td><td>aa</td>
<td colspan="2">NASMTNSVKGMNA</td>
<td colspan="2">GFTFSNYDMA</td>
<td colspan="2">SIITSGGDNYYRDSVKG</td>
<td colspan="2">HDYYDGSYGFAY</td>
<td colspan="2">KASQSVGINVD</td>
<td colspan="2">GASNRHT</td>
<td colspan="2">LQYGSIPFT</td>
<td colspan="2">EVQLVESGGGLVQPGRSLKLSCAASGFTFSNYDMAWVRQAPTKGLEWVASIITSGGDNYYRDSVKGR FTVSRDNAKSTLYLQMDSLRSEDTATYYCVRHDYYDGSYGFAYWGQGTLVTVSS</td>
<td colspan="2">ETVMTQSPTSMSTSIGERVTLNCKASQSVGINVDWYQQTPGQSPKLLIYGASNRHTGVPDRFTGSGF GRDFTLTISNVEAEDLAVYYCLQYGSIPFTFGSGTKLELK</td>
<td colspan="2">EVQLVESGGGLVQPGRSLKLSCAASGFTFSNYDMAWVRQAPTKGLEWVASIITSGGDNYYRDSVKGR FTVSRDNAKSTLYLQMDSLRSEDTATYYCVRHDYYDGSYGFAYWGQGTLVTVSSGGGGSGGGGGSGG GGSETVMTQSPTSMSTSIGERVTLNCKASQSVGINVDWYQQTPGQSPKLLIYGASNRHTGVPDRFTG SGFGRDFTLTISNVEAEDLAVYYCLQYGSIPFTFGSGTKLELK</td>
<td colspan="2">GYTFTNHIIH</td>
<td colspan="2">YINPYNDDTEYNEKFKG</td>
<td colspan="2">DGYYRDMDVMDY</td>
<td>RASQDISNYLN</td><td></td>
<td>YTSRLHS</td><td> _</td>
<td>QQGNTLPWT</td><td>4 TOMJ rwn a ।</td>
<td>EVQLVEQSGPELVKPGASVKMSCKASGYTFTNHIIHWVKQKPGQGLEWIGYINPYNDD KATLTSDKSSTTAYMELSSLTSEDSAVYYCARDGYYRDMDVMDYWGQGTTVTVSS</td><td>’EYN^gÍK^i</td>
<td>ELVMTQTPSSLSASLGDRVTISCRASQDISNYLNWYQQKPDGTVKLLIYYTSRLHSGV:</td><td></td>
<td></td><td></td>
234
GTDYSLTISNLEQEDIATYFCQQGNTLPWTFGGGTKLEIK
<td> 1039</td><td>BCMA-102</td><td>BC 244-A7</td><td>scFv</td><td>aa</td><td>EVQLVEQSGPELVKPGASVKMSCKASGYTFTNHIIHWVKQKPGQGLEWIGYINPYNDDTEYNEKFKG KATLTSDKSSTTAYMELSSLTSEDSAVYYCARDGYYRDMDVMDYWGQGTTVTVSSGGGGSGGGGSGG GGSELVMTQTPSSLSASLGDRVTISCRASQDISNYLNWYQQKPDGTVKLLIYYTSRLHSGVPSRFSG SGSGTDYSLTISNLEQEDIATYFCQQGNTLPWTFGGGTKLEIK</td>
<td> 1040</td><td>BCMA-103</td><td>BC 263-A4</td><td>VH CDR1</td><td>aa</td><td>GFTFSNYDMA</td>
<td> 1041</td><td>BCMA-103</td><td>BC 263-A4</td><td>VH CDR2</td><td>aa</td><td>SISTRGDITSYRDSVKG</td>
<td> 1042</td><td>BCMA-103</td><td>BC 263-A4</td><td>VH CDR3</td><td>aa</td><td>QDYYTDYMGFAY</td>
<td> 1043</td><td>BCMA-103</td><td>BC 263-A4</td><td>VLCDR1</td><td>aa</td><td>RASEDIYNGLA</td>
<td> 1044</td><td>BCMA-103</td><td>BC 263-A4</td><td>VL CDR2</td><td>aa</td><td>GASSLQD</td>
<td> 1045</td><td>BCMA-103</td><td>BC 263-A4</td><td>VL CDR3</td><td>aa</td><td>QQSYKYPLT</td>
<td> 1046</td><td>BCMA-103</td><td>BC 263-A4</td><td>VH</td><td>aa</td><td>EVQLVEESGGGLLQPGRSLKLSCAASGFTFSNYDMAWVRQAPTKGLEWVASISTRGDITSYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCARQDYYTDYMGFAYWGQGTLVTVSS</td>
<td> 1047</td><td>BCMA-103</td><td>BC 263-A4</td><td>VL</td><td>aa</td><td>EL·VMTQSPASLSASL·GΞTVTIECRASEDIYNGLAWYQQKPGKSPQL·LIYGASSLQDGVPSRFSGSGS GTQYSLKISGMQPEDEANYFCQQSYKYPLTFGSGTKLELK</td>
<td> 1048</td><td>BCMA-103</td><td>BC 263-A4</td><td>scFv</td><td>aa</td><td>EVQLVEESGGGLLQPGRSLKLSCAASGFTFSNYDMAWVRQAPTKGLEWVASISTRGDITSYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCARQDYYTDYMGFAYWGQGTLVTVSSGGGGSGGGGSGG GELVMTQSPASLSASLGETVTIECRASEDIYNGLAWYQQKPGKSPQLLIYGASSLQDGVPSRFSGSG SGTQYSLKISGMQPEDEANYFCQQSYKYPLTFGSGTKLELKGS</td>
235
<td> 1049</td><td>BCMA-104</td><td>BC 271-C3</td><td>VH CDR1</td><td>aa</td><td colspan="2">GFTFSNFDMA</td><td rowspan="4"></td>
<td> 1050</td><td>BCMA-104</td><td>BC 271-C3</td><td>VH CDR2</td><td>aa</td><td colspan="2">SITTGGGDTYYRDSVKG</td>
<td> 1051</td><td>BCMA-104</td><td>BC 271-C3</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td><td> 11=<sup>19</sup></td>
<td> 1052</td><td>BCMA-104</td><td>BC 271-C3</td><td>VL CDR1</td><td>aa</td><td>RASQGISNYL</td><td></td>
<td> 1053</td><td>BCMA-104</td><td>BC 271-C3</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td> 2?«</td><td></td>
<td> 1054</td><td>BCMA-104</td><td>BC 271-C3</td><td>VL CDR3</td><td>aa</td><td>QQYDISSYT</td><td>»o> ? jes</td><td></td>
<td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>
<td> 1055</td><td>BCMA-104</td><td>BC271-C3</td><td>VH</td><td>aa</td><td>EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGASVTVSS</td>
<td> 1056</td><td>BCMA-104</td><td>BC 271-C3</td><td>VL</td><td>aa</td><td>ELVMTQTPSSMPASLGERVTISCRASQGISNYLNWYQQKPDGTIKPLIYYTSNLQSGVPSRFSGSGS GTDYSLTINSLEPEDFAVYYCQQYDISSYTFGAGTKLEIK</td>
<td> 1057</td><td>BCMA-104</td><td>BC271-C3</td><td>scFv</td><td>aa</td><td>EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGASVTVSSGGGGSGGGGSGG GGSELVMTQTPSSMPASLGERVTISCRASQGISNYLNWYQQKPDGTIKPLIYYTSNLQSGVPSRFSG SGSGTDYSLTINSLEPEDFAVYYCQQYDISSYTFGAGTKLEIK</td>
<td> 1058</td><td>BCMA-105</td><td>BC 265-E5</td><td>VH CDR1</td><td>aa</td><td>GFTFSNFDMA</td>
<td> 1059</td><td>BCMA-105</td><td>BC 265-E5</td><td>VH CDR2</td><td>aa</td><td>SITTGGGDTYYRDSVKG</td>
<td> 1060</td><td>BCMA-105</td><td>BC 265-E5</td><td>VH CDR3</td><td>aa</td><td>HGYYDGYHLFDY</td>
<td> 1061</td><td>BCMA-105</td><td>BC 265-E5</td><td>VLCDR1</td><td>aa</td><td>RASQGISNHLN</td>
<td> 1062</td><td>BCMA-105</td><td>BC 265-E5</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td>
<td> 1063</td><td>BCMA-105</td><td>BC 265-E5</td><td>VLCDR3</td><td>aa</td><td>QQYDSFPLT</td>
<td> 1064</td><td>BCMA-105</td><td>BC 265-E5</td><td>VH</td><td>aa</td><td>EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGTLVTVSS</td>
<td> 1065</td><td>BCMA-105</td><td>BC 265-E5</td><td>VL</td><td>aa</td><td>ELVMTQTPSSMPASLGERVTISCRASQGISNHLNWYQQKPDGTIKPLIYYTSNLQSGVPSRFSGSGS GTDYSLTISSLEPEDFAMYYCQQYDSFPLTFGSGTKLEIK</td>
<td> 1066</td><td>BCMA-105</td><td>BC 265-E5</td><td>scFv</td><td>aa</td><td>EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGTLVTVSSGGGGSGGGGSGG GGSELVMTQTPSSMPASLGERVTISCRASQGISNHLNWYQQKPDGTIKPLIYYTSNLQSGVPSRFSG SGSGTDYSLTISSLEPEDFAMYYCQQYDSFPLTFGSGTKLEIK i</td>
<td> 1067</td><td>BCMA-106</td><td>BC271-B12</td><td>VH CDR1</td><td>aa</td><td>_______ 1 GFTFSNFDMA i</td>
<td> 1068</td><td>BCMA-106</td><td>BC271-B12</td><td>VH CDR2</td><td>aa</td><td>S ITTGGGDTYYRDS VKG 1</td>
<td> 1069</td><td>BCMA-106</td><td>BC271-B12</td><td>VH CDR3</td><td>aa</td><td>_ _ 1 333 HGYYDGYHLFDY /</td>
<td> 1070</td><td>BCMA-106</td><td>BC271-B12</td><td>VL CDR1</td><td>aa</td><td>RASQGISNNLN I</td>
NJ <JU
CT1
<img file="MX349396B_D0112.tif" />
<td> 1071</td><td>BCMA-106</td><td>BC271-B12</td><td>VL CDR2</td><td>aa</td><td>YTSNLQS</td><td></td><td></td>
<td> 1072</td><td>BCMA-106</td><td>BC271-B12</td><td>VL CDR3</td><td>aa</td><td>QQFDTSPYT</td><td></td><td></td>
<td> 1073</td><td>BCMA-106</td><td>BC271-B12</td><td>VH</td><td>aa</td><td colspan="2">EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGVMVTVSS</td><td></td>
<td> 1074</td><td>BCMA-106</td><td>BC271-B12</td><td>VL</td><td>aa</td><td colspan="2">ELVMTQTPSSMPASLGERVTISCRASQGISNNLNWYQQKPDGTIKPLIYYTSNLQSGVPSRFSGSGS GTDYSLTISSLEPEDFAMYYCQQFDTSPYTFGAGTKLEIK</td><td></td>
<td> 1075</td><td>BCMA-106</td><td>BC271-B12</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVEESGGGLVQPGRSLKLSCAASGFTFSNFDMAWVRQAPTRGLEWVASITTGGGDTYYRDSVKG RFTISRDNAKSTLYLQMDSLRSEDTATYYCVRHGYYDGYHLFDYWGQGVMVTVSSGGGGSGGGGSGG θα3ΕΕνΜΤ0ΤΡ35ΜΡΑ3ΕΘΕΕνΤΙ3ΟΕΑ30αΐ3ΝΝΕΝΝΥΟ0ΚΡϋΟΤΙΚΡΕΙΥΥΤ5ΝΕ03σνΡ3ΕΡ3σ SGSGTDYSLTISSLEPEDFAMYYCQQFDTSPYTFGAGTKLEIK</td><td></td>
<td> 1076</td><td>BCMA-107</td><td>BC 247-A4</td><td>VH CDR1</td><td>aa</td><td>GYSFPDYYIN</td><td></td><td></td>
<td> 1077</td><td>BCMA-107</td><td>BC 247-A4</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNE</td><td></td><td></td>
<td> 1078</td><td>BCMA-107</td><td>BC 247-A4</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td><td></td><td></td>
<td> 1079</td><td>BCMA-107</td><td>BC 247-A4</td><td>VL CDR1</td><td>aa</td><td>RS S QSLVHSNGNTYLH</td><td></td><td></td>
<td> 1080</td><td>BCMA-107</td><td>BC 247-A4</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td><td></td><td> 237</td>
<td> 1081</td><td>BCMA-107</td><td>BC 247-A4</td><td>VL CDR3</td><td>aa</td><td>SQSTHVPYT</td><td></td><td></td>
<td> 1082</td><td>BCMA-107</td><td>BC 247-A4</td><td>VH</td><td>aa</td><td colspan="2">EVQLVEQSGPELVKPGASVKISCKVSGYSFPDYYINWVKQRPGQGLEWIGWIYFASGNSEYNERFTG KATLTVDTSSNTAYMQLSSLTSEDTAVYFCASLYDYDWYFDVWGQGTTVTVSS</td><td></td>
<td> 1083</td><td>BCMA-107</td><td>BC 247-A4</td><td>VL</td><td>aa</td><td colspan="2">EL·VMTQTPLSL·PVSL·GDQASISCRSSQSL·VHSNGNTYLHWYLQKPGQSPKL·LIYKVSNRFSGVPDRF SGSGSGADFTLKISRVEAEDLGVYFCSQSTHVPYTFGGGTKLEIK</td><td></td>
<td> 1084</td><td>BCMA-107</td><td>BC 247-A4</td><td>scFv</td><td>aa</td><td colspan="2">EVQLVEQSGPELVKPGASVKISCKVSGYSFPDYYINWVKQRPGQGLEWIGWIYFASGNSEYNERFTG KATLTVDTSSNTAYMQLSSLTSEDTAVYFCASLYDYDWYFDVWGQGTTVTVSSGGGGSGGGCSGGGGg 3ΕΕνΜΤ0ΤΡΕ3ΕΡν3ΕσθΰΑ3Ι3ΟΕ3303ΕνΗ3ΝαΝΤΥΕΗΝΥΕ0ΚΡα03ΡΚΕΕΙΥΚν3ΝΕΕ|3ανΡΏ^ FSGSGSGADFTLKISRVEAEDLGVYFCSQSTHVPYTFGGGTKLEIK 1</td><td></td>
<td> 1085</td><td>BCMA-108</td><td>BC 246-B6</td><td>VH CDR1</td><td>aa</td><td>GYSFPDYYIN</td><td>MUIC inusT</td><td></td>
<td> 1086</td><td>BCMA-108</td><td>BC 246-B6</td><td>VH CDR2</td><td>aa</td><td>WIYFASGNSEYNE</td><td></td><td></td>
<img file="MX349396B_D0113.tif" />
<td> 1087</td><td>BCMA-108</td><td>BC 246-B6</td><td>VH CDR3</td><td>aa</td><td>LYDYDWYFDV</td>
<td> 1088</td><td>BCMA-108</td><td>BC 246-B6</td><td>VL CDR1</td><td>aa</td><td>RSSQSLVHSNGNTYLH</td>
<td> 1089</td><td>BCMA-108</td><td>BC 246-B6</td><td>VL CDR2</td><td>aa</td><td>KVSNRFS</td>
<td> 1090</td><td>BCMA-108</td><td>BC 246-B6</td><td>VL CDR3</td><td>aa</td><td>FQGSHVPWT</td>
<td> 1091</td><td>BCMA-108</td><td>BC 246-B6</td><td>VH</td><td>aa</td><td>EVQLVEQSGPQLVKPGASVKISCKVSGYSFPDYYINWVKQRPGQGLEWIGWIYFASGNSEYNERFTG KATLTVDTSSNTAYMQLSSLTSEDTAVYFCASLYDYDWYFDVWGQGTTVTVSS</td>
<td> 1092</td><td>BCMA-108</td><td>BC 246-B6</td><td>VL</td><td>aa</td><td>ΕΕνΜτοτρΕΞΣΡνεΕσϋΟΑειεσρβεοεΕνΗΞΝσΝΤΥΕΗΝΥΕΟΚΡσοερκΏΕΐΥκνΞΝΗΕεσνρσΡΕ SG SGSGTDFTLKINRVEAEDLGVYYCFQGSHVPWTFGGGTKLEIK</td>
<td> 1093</td><td>BCMA-108</td><td>BC 246-B6</td><td>scFv</td><td>aa</td><td>EVQLVEQSGPQLVKPGASVKISCKVSGYSFPDYYINWVKQRPGQGLEWIGWIYFASGNSEYNERFTG KATLTVDTSSNTAYMQLSSLTSEDTAVYFCASLYDYDWYFDVWGQGTTVTVSSGGGGSGGGGSGGGG SELVMTQTPLSLPVSLGDQASISCRSSQSLVHSNGNTYLHWYLQKPGQSPKLLIYKVSNRFSGVPGR FSGSGSGTDFTLKINRVEAEDLGVYYCFQGSHVPWTFGGGTKLEIK</td>
238
<img file="MX349396B_D0114.tif" />
239
<img file="MX349396B_D0115.tif" />
IMPI
Mexican Institute of Industrial Property
Contents217
773 sheets
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109 members in 41 offices
Priority claims15
| Document | Office | Kind | Date |
|---|---|---|---|
| 61560144 | United States of America | – | |
| 61560149 | United States of America | – | |
| 61560162 | United States of America | – | |
| 61560178 | United States of America | – | |
| 61560183 | United States of America | – | |
| 201161560144 | United States of America | P | |
| 201161560149 | United States of America | P | |
| 201161560162 | United States of America | P | |
| 201161560178 | United States of America | P | |
| 201161560183 | United States of America | P | |
| 61651474 | United States of America | – | |
| 61651486 | United States of America | – | |
| 201261651474 | United States of America | P | |
| 201261651486 | United States of America | P | |
| 2012072699 | European Patent Office (EPO) | W |
Members109
| Document | Office | Kind | |
|---|---|---|---|
| CA2849196A1 | Canada | A1 | |
| CA2850591A1 | Canada | A1 | |
| WO2013072406A1 | World Intellectual Property Organization (WIPO) | A1 | |
| WO2013072415A1 | World Intellectual Property Organization (WIPO) | A1 | |
| AU2012327200A1 | Australia | A1 | |
| AU2012327203A1 | Australia | A1 | |
| US2013156769A1 | United States of America | A1 | |
| US2013156770A1 | United States of America | A1 | |
| UY34453A | Uruguay | A | |
| UY34454A | Uruguay | A | |
| TW201326214A | Taiwan Province of China | A | |
| AP2014007529A0 | African Regional Intellectual Property Organization (ARIPO) | A0 | |
| SG11201400671YA | Singapore | A | |
| PH12014501076A1 | Philippines | A1 | |
| IL232603A0 | Israel | A0 | |
| IL232603D0 | Israel | D0 | |
| IL232636A0 | Israel | A0 | |
| IL232636D0 | Israel | D0 | |
| AR088883A1 | Argentina | A1 | |
| PH12014501091A1 | Philippines | A1 | |
| EA201490931A1 | Eurasian Patent Organization (EAPO) | A1 | |
| MA35449B1 | Morocco | B1 | |
| MA35450B1 | Morocco | B1 | |
| KR20140105757A | Republic of Korea | A | |
| KR20140105758A | Republic of Korea | A | |
| MX2014005852A | Mexico | A | |
| EP2780374A1 | European Patent Office (EPO) | A1 | |
| EP2780375A1 | European Patent Office (EPO) | A1 | |
| SG11201401729PA | Singapore | A | |
| EA201490932A1 | Eurasian Patent Organization (EAPO) | A1 | |
| CL2014001254A1 | Chile | A1 | |
| CL2014001263A1 | Chile | A1 | |
| CN104114578A | China | A | |
| CN104169300A | China | A | |
| US2014348837A1 | United States of America | A1 | |
| PE20141564A1 | Peru | A1 | |
| JP2014534242A | Japan | A | |
| MX2014005851A | Mexico | A | |
| US2015023967A1 | United States of America | A1 | |
| JP2015504306A | Japan | A | |
| ECSP14004893A | Ecuador | A | |
| TN2014000097A1 | Tunisia | A1 | |
| TN2014000121A1 | Tunisia | A1 | |
| ECSP14004829A | Ecuador | A | |
| US9150664B2 | United States of America | B2 | |
| AU2012327200B2 | Australia | B2 | |
| AU2012327200A8 | Australia | A8 | |
| US9340621B2 | United States of America | B2 | |
| NZ622087A | New Zealand | A | |
| SG10201606484SA | Singapore | A | |
| US9598500B2 | United States of America | B2 | |
| BR112014010630A2 | Brazil | A2 | |
| BR112014010940A2 | Brazil | A2 | |
| MX349396BThis record | Mexico | B | |
| SG10201704483RA | Singapore | A | |
| ZA201401615B | South Africa | B | |
| EA028162B1 | Eurasian Patent Organization (EAPO) | B1 | |
| JP2017195889A | Japan | A | |
| JP6231007B2 | Japan | B2 | |
| JP2018050627A | Japan | A | |
| UA116766C2 | Ukraine | C2 | |
| IL232603A | Israel | A | |
| IL232603B | Israel | B | |
| IL260189A | Israel | A | |
| IL260189D0 | Israel | D0 | |
| JP6378087B2 | Japan | B2 | |
| CN104114578B | China | B | |
| GEP20186928B | Georgia | B | |
| CN109485729A | China | A | |
| EP2780374B1 | European Patent Office (EPO) | B1 | |
| EP2780375B1 | European Patent Office (EPO) | B1 | |
| LT2780375T | Lithuania | T | |
| PT2780375T | Portugal | T | |
| DK2780375T3 | Denmark | T3 | |
| RS59373B1 | Serbia | B1 | |
| SI2780375T1 | Slovenia | T1 | |
| TWI679212B | Taiwan Province of China | B | |
| HRP20191697T1 | Croatia | T1 | |
| KR102062231B1 | Republic of Korea | B1 | |
| KR20200003934A | Republic of Korea | A | |
| SMT201900627T1 | San Marino | T1 | |
| PL2780375T3 | Poland | T3 | |
| EP3611193A1 | European Patent Office (EPO) | A1 | |
| EP3623385A1 | European Patent Office (EPO) | A1 | |
| ES2749451T3 | Spain | T3 | |
| HUE046682T2 | Hungary | T2 | |
| ES2751996T3 | Spain | T3 | |
| ME03521B | Montenegro | B | |
| EP3623385A8 | European Patent Office (EPO) | A8 | |
| JP6738314B2 | Japan | B2 | |
| US10766969B2 | United States of America | B2 | |
| JP2020202838A | Japan | A | |
| CY1122543T1 | Cyprus | T1 | |
| KR102229469B1 | Republic of Korea | B1 | |
| KR20210032012A | Republic of Korea | A | |
| CA2849196C | Canada | C | |
| KR102346029B1 | Republic of Korea | B1 | |
| MY189544A | Malaysia | A | |
| US2022064336A1 | United States of America | A1 | |
| US2022251243A1 | United States of America | A1 |
1 legal event, as the office reported them to INPADOC
Events
| Event | Code | |
|---|---|---|
| Grant or registrationFG | FG |
Numbers
- Publication
- 349396
- Application
- 5852
Titles2
- Spanish
- MOLECULAS DE UNION PARA BCMA Y CD3.
- English
- BINDING MOLECULES FOR BCMA AND CD3.
Classification
- CPC, 33
- C07K16/2809
- C07K16/468
- C07K2317/31
- C07K2317/33
- C07K2317/56
- C07K2317/565
- C07K2317/73
- C07K14/70578
- C07K2319/00
- C07K2319/21
- C07K2319/30
- C07K2319/31
- C07K2319/43
- A61K2039/505
- C07K2317/34
- C07K2317/622
- C07K2317/92
- C07K2317/94
- C07K16/2878
- A61P17/00
- A61P19/00
- A61P3/00
- A61P35/00
- A61P35/02
- A61P35/04
- A61P37/00
- A61P37/02
- A61P37/06
- A61P43/00
- A61P7/00
- A61K39/0005
- A61K2039/575
- C07K16/2875
- IPC, 5
- C07K16 28
- A61K39 395
- C07K14 575
- C07K14 705
- C07K16 46