Composition on the basis of an amino-acid and vitamins for use in cancer therapy.

0001The present invention relates to a new composition which can be used in therapy, and more particularly an association based on amino acid, on the one hand, and vitamins, on the other hand, which can be used in cancer therapy.

0002Various therapeutic treatments for cancer have been proposed in surgery, radiotherapy and chemotherapy.

0003Thus, surgical excisions, the indications of which depend on the location and invasion of the tumor, can be satisfactory on the carcinological level, or simply palliative. However, they constitute a certain aggression for the organism and can lead to permanent mutilation.

0004Radiotherapy, isolated or associated with another treatment, has an undeniable action on certain types of tumors, but its action always exceeds the regional framework of the tumor, leading to sequelae which depend on the location. The impact on the general condition of the patient depends on the cumulative doses made necessary depending on the mass treated.

0005In chemotherapy, for example, heavy metal salts are used, alkylating agents such as cyclophosphamide or mechloretamine, anti-metabolites such as uracil or cytosine derivatives, certain derivatives from the series of antibiotics such as bleomycin or daunomycin, or alkaloids such as vinblastine and vincristine. These compounds can be used, as the case may be, alone or in combination of two or more. They generally have toxic side effects that limit or prohibit their use at high doses, all the more if the patient has associated defects or sequelae from mutilating surgery or radiotherapy.

0006All of these therapies, to varying degrees, aim to eliminate the maximum or all of cancerous tumors, but none of them exerts an action on the evolutionary genius of the cancer process.

0007We know the importance of vitamins, water-soluble and fat-soluble, in nutritional physiology and biochemistry. However, their use for the treatment of cancer, alone or in combination with other compounds, has not been described so far.

0008On the other hand, certain amino acids are used therapeutically for the treatment of various diseases. Thus, for example, it is known that 5-alanine has properties which inhibit peripheral vasodilation allowing its administration for the treatment of hot flashes of menopause. Its toxicity is low since the lethal dose DL_soorally in mice and rats, is greater than 10 g / kg, and its tolerance is generally satisfactory. If the antiallergic and antihistamine activity of β-alanine has been described, on the other hand, no application of this compound is known, alone or in combination, for the treatment of cancer.

0009It is also recognized that β-alanine acts as a chemical mediator in the central nervous system, and could act at the cellular level in relation to the calcium signal.

0010Some compositions are known to contain various components, including certain amino acids and vitamins; for example "Unlisted Drug" vol. 28 no7 cites a composition which can be used as a nutritional supplement, containing pyridoxine, citric acid, taurine, etc. However, the specific use of β-alanine combined with vitamins has not been envisaged.

0011It has now been found that a composition containing β-alanine in combination with various vitamins has properties allowing its application in therapy for the treatment of cancer, while no comparable activity is observed when each of them is used in isolation. these compounds.

0012The present invention therefore relates to a new composition based on β-alanine and vitamins, which can be used for the treatment of cancer.

0013The new composition in accordance with the present invention comprises at least one vitamin and β-alanine represented by the following general formula (I):<ul id="ul0001" list-style="none"><li>H₂N - (CH₂)₂- COOH (I)</li></ul>or one of its acid or base salts.

0014More particularly, the composition in accordance with the invention comprises β-alanine corresponding to formula (I) above and one or more vitamins chosen from vitamin A, vitamin Bi, vitamin B₂, vitamin Bs, pyridoxine, ascorbic acid, tocopherol, vitamin D₂, and vitamin PP.

0015Β-alanine can be used alone or, if necessary, in combination with one or more other amino acids; for example 5-alanine and glycine, or β-alanine and taurine, can be combined.

0016In addition to the vitamins and the amino acid indicated above, the composition may also advantageously include additives such as glucose, β-carotene, or other vitamins such as biotin and vitamin B₁₂.

0017According to a preferred embodiment of the invention, the composition comprises β-alanine, and several vitamins chosen from those indicated above, as well as glucose, and optionally taurine, and / or glycine. It may be preferable to add to all of these constituents P-carotene, a precursor of vitamin A.

0018The weight ratio of the amino acid to the total of the vitamins is between approximately 50/1 and 500/1, and preferably between approximately 100/1 and 300/1, and the amount of amino acid administered per day is between 50g and 200g approximately for an attack treatment, and between 10 and 50g approximately for a maintenance treatment in adult men. Of course, the dose administered is determined by the doctor depending on the condition of the patient. When glucose is used, it can represent between 10 and 30% by weight of the dose of amino acid for an attack treatment. The amount of glucose used is substantially the same in an attack treatment and in a maintenance treatment.

0019The invention also relates to a method for preparing a composition useful in cancer therapy.

0020The components constituting the composition of the present invention can be administered as a mixture or separately, preferably orally. It is possible, for example, to mix the amino acid, the vitamins and, where appropriate, the glucose and the other additives, in the form of a powder which can be packaged in various usual forms, for example in sachets, capsules or capsules. It is also possible to package separately the amino acid, on the one hand, and the vitamins and the other optional additives, on the other hand, for example in the form of capsules or capsules which can be administered orally, separately, the administration of each of these two parts can be spaced in time from a few minutes to a few hours, without however exceeding 4 to 5 hours approximately.

0021The composition in accordance with the present invention can constitute a therapy which accompanies the usual therapeutic, chemical, chemotherapeutic or radiotherapeutic treatments, in the case of cancer treatment. The advantage of the therapy in accordance with the present invention lies in particular in the fact that the known treatments, which, as indicated above, are traumatic, even toxic, can now be used at lower doses which avoid harmful side effects.

0022The experimental results have shown that the composition according to the invention does not destroy the cancer cell, but inhibits its cell division. It has the property, like antimitotics and radiotherapy, of acting on carcinomedin, a potentiator of tumor cell multiplication. It is particularly interesting to note that these results are obtained when the components are administered simultaneously, as a mixture, but also when the vitamins, on the one hand, and the amino acid, on the other hand, are administered separately at an interval of times ranging from a few minutes to around 4 to 5 hours.

0023On the other hand, no destructive effect on cancer cells is observed if only an amino acid or vitamins are administered, or if their weight ratio or the doses administered are outside the above limits.

0024Toxicological studies have shown that the toxicity of the composition according to the invention is zero at the doses administered for the treatment of cancer.

0025Examples of compositions in accordance with the present invention are given below without implied limitation.

EXAMPLE 1

0026A mixture of the components indicated below is prepared:<tables id="tabl0001" num="0001"><img file="EP0280593A2_D0001.tif" /></tables>

0027These components are carefully mixed so as to obtain a homogeneous composition corresponding to the dose administered in 24 hours for an attack treatment. The administration is made orally in four equal parts, every 6 hours, either by voluntary intake, or added to the enteral nutrition solution.

EXAMPLE 2

0028The procedure is as in Example 1, using the components below to prepare a composition intended for a maintenance treatment:<tables id="tabl0002" num="0002"><img file="EP0280593A2_D0002.tif" /></tables>

0029An amount of composition is thus obtained corresponding to the dose administered in 24 hours during a maintenance treatment. The above composition is administered in four equal parts, every 6 hours.

EXAMPLE 3

0030By proceeding as in Example 1, a mixture of the following components is prepared:<tables id="tabl0003" num="0003"><img file="EP0280593A2_D0003.tif" /></tables>

0031The mixture is homogenized and then distributed between 5 identical sachets for oral administration. In addition, 5 sachets dosed with 4g of taurine are prepared in the usual manner.

0032The composition is administered at the rate of five intakes of a sachet of the above mixture of vitamins and β-alanine, spaced four hours apart, followed at one hour intervals by five intakes of a sachet of taurine. There is thus an attack treatment which is renewed for a period which depends on the clinical condition of the patient.