FIELD: medicine, oncology, pharmacy. SUBSTANCE: invention relates to pharmaceutical composition showing an antitumor activity and containing themozolomid: 8-carbamoyl-3-methylimidazo-[5,1-d]-1,2,3,5-tetrazine-4-(3H)-one as an active component and inhibitor of O6-alkylguanine-DNA-alkyltransferase at ratio from 1:1 to 1:20.000. Also, pharmaceutical composition has at least one pharmaceutically acceptable carrier. Inhibitor is taken among the group including O6-alkylguanines, O6-arylguanines and O6-benzylated guanines, guanosines and 2'-deoxyguanosines. Method of preparing the pharmaceutical composition involves mixing themozolomid with inhibitor of O6-alkylguanine-DNA-alkyl-transferase and pharmaceutically acceptable carrier. EFFECT: enhanced antitumor activity of composition. 4 cl, 5 dwg, 2 tbl, 6 ex
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