Using the monolay tumor cell culture system and the method or MTT colorimetric analysis, the cytotoxicity of the anticancer drug VM-26 and Nicardipine(NCDP) in human malignant glioma cell line U251 was studied. The results showed that the cytotoxicity of VM-26 in U251 was enhanced by NCDP at a low dose which did not show direct cytotoxicity. The authors considered that VM-26 combined with NCDP can heighten the intracellular anticancer drug concentration, reverse the drug resistance and heterogeneity in human malignant glioma cells. The mechanism of the enhanced effect was also discussed. These findings will provide an alternative chemotherapeutic clue to treat the postoperative malignant gliomas.