Abstract
The 1,4‐benzothiazepine derivative JTV‐519 is a new type of calcium ion channel modulator. We examined the modulatory effect of JTV‐519 on the antitumor activity of several platinum compounds (cisplatin, carboplatin, and nedaplatin) in a human cancer cell line resistant to cisplatin (PC‐14/CDDP) in vitro. PC‐14/CDDP cells showed 8‐fold resistance to cisplatin compared with the parental PC‐14 cells as determined by dye formation [3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltet‐razolium bromide, MTT] assay. In PC‐14/CDDP, but not PC‐14 cells, augmentation of cytotoxicity was observed when a nontoxic concentration (10 μ) of JTV‐519 was combined with the platinum compounds. Increased intracellular cisplatin accumulation was observed in PC‐14/CDDP cells in the presence of JTV‐519 as measured by atomic absorption assay. Therefore, increased cisplatin accumulation was considered to be a possible mechanism underlying the reversing effect of JTV‐519 on cisplatin resistance. These results suggest that JTV‐519 is a potent agent reversing cisplatin resistance.
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