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首页> 外文期刊>British Journal of Cancer >Amiodarone is more efficient than verapamil in reversing resistance to anthracyclines in tumour cells
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Amiodarone is more efficient than verapamil in reversing resistance to anthracyclines in tumour cells

机译：胺碘酮比维拉帕米更有效地逆转肿瘤细胞对蒽环类药物的耐药性

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We have previously demonstrated that amiodarone is able to reverse resistance of rat colon cancer cells to anthracyclines. We now compare the efficiency of amiodarone to verapamil one, another antiarrhythmic agent used in experimental systems and in clinical trials to enhance the effects of anthracyclines on resistant cancer cells. Amiodarone is more efficient than verapamil when both drugs are used at the same molar concentrations. Desethylamiodarone, the main metabolite of amiodarone, is as efficient as its precursor. Optimal concentrations of amiodarone are obtained without side effects in the sera of patients treated by oral administration followed by a loading infusion of amiodarone. On the other hand, maximal tolerated levels of verapamil reported in clinical trials are less efficient than amiodarone maximal levels in the reversal of resistance to anthracyclines in our experimental model in vitro. We suggest that amiodarone, which is more efficient and less toxic than verapamil, could be substituted for verapamil in future clinical trials.
机译：我们以前已经证明胺碘酮能够逆转大鼠结肠癌细胞对蒽环类药物的耐药性。现在，我们比较胺碘酮与维拉帕米（一种新的抗心律不齐药物）在实验系统和临床试验中的作用，以增强蒽环类药物对耐药癌细胞的作用。当两种药物以相同的摩尔浓度使用时，胺碘酮比维拉帕米更有效。胺碘酮的主要代谢产物去乙基胺碘酮与它的前体一样有效。获得最佳浓度的胺碘酮在口服给药后负荷输注胺碘酮治疗的患者血清中无副作用。另一方面，在我们的体外实验模型中，临床试验中报告的维拉帕米的最大耐受水平在逆转对蒽环类药物的耐药性方面不如胺碘酮最大水平有效。我们建议在未来的临床试验中，比维拉帕米更有效，毒性更小的胺碘酮可以代替维拉帕米。

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