Simpson W G, Tseng M T, Anderson K C, Harty J I
J Urol. 1984 Sep;132(3):574-6. doi: 10.1016/s0022-5347(17)49749-7.
The calcium influx blocker verapamil has been used to overcome drug resistance in several tumor systems. The possible in vitro enhancement of drug efficacy was assessed in bladder cancer cell line T24. Combination of thiotepa and doxorubicin hydrochloride with verapamil significantly reduced the survival and growth of T24 cells after as little as 1 hour of drug exposure. An increase in doxorubicin hydrochloride-induced inhibition of [3H]thymidine uptake resulted when verapamil was administered. However, this trend was not demonstrated when combined with thiotepa. It appears that verapamil enhances thiotepa-induced cytotoxicity while it potentiates the antimitotic nature of doxorubicin hydrochloride. The data presented is consistent with the postulate that verapamil alters active efflux of drug from malignant cells and suggests that verapamil has a role in the clinical management of bladder cancer.
钙内流阻滞剂维拉帕米已被用于克服多种肿瘤系统中的耐药性。在膀胱癌细胞系T24中评估了其在体外增强药物疗效的可能性。塞替派和盐酸多柔比星与维拉帕米联合使用，在药物暴露仅1小时后就显著降低了T24细胞的存活和生长。给予维拉帕米后，盐酸多柔比星诱导的[3H]胸苷摄取抑制作用增强。然而，与塞替派联合使用时未显示出这种趋势。似乎维拉帕米增强了塞替派诱导的细胞毒性，同时增强了盐酸多柔比星的抗有丝分裂特性。所呈现的数据与维拉帕米改变恶性细胞中药物主动外排的假设一致，并表明维拉帕米在膀胱癌的临床治疗中具有作用。
