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奥沙利铂的细胞与分子药理学

Cellular and molecular pharmacology of oxaliplatin.

作者信息

Raymond Eric, Faivre Sandrine, Chaney Stephen, Woynarowski Jan, Cvitkovic Esteban

机构信息

Department of Medicine, Institut Gustave-Roussy, 39 rue Camille Desmoulins, 94805 Villejuif, France.

出版信息

Mol Cancer Ther. 2002 Jan;1(3):227-35.

Abstract

Oxaliplatin, a diaminocyclohexane-containing platinum, has a spectrum of activity and mechanisms of action and resistance that appear to be different from those of other platinum-containing compounds, notably cisplatin. The first part of this review describes the differences between oxaliplatin and cisplatin in terms of their spectrum of activity and adduct formation and then goes on to discuss molecular and cellular experimental data that potentially explain them. Particular emphasis is placed on the differential role of DNA repair mechanisms. In addition, the anticancer effects of oxaliplatin are optimized when it is administered in combination with other anticancer agents, such as 5-fluorouracil, gemcitabine, cisplatin, or carboplatin; topoisomerase I inhibitors; and taxanes. In vitro and preclinical combination data that could optimize oxaliplatin-based chemotherapy are also reviewed.

摘要

奥沙利铂是一种含二氨基环己烷的铂类药物,其活性谱、作用机制及耐药机制似乎与其他含铂化合物(尤其是顺铂)不同。本综述的第一部分描述了奥沙利铂和顺铂在活性谱及加合物形成方面的差异,接着讨论了可能解释这些差异的分子和细胞实验数据。特别强调了DNA修复机制的不同作用。此外,奥沙利铂与其他抗癌药物(如5-氟尿嘧啶、吉西他滨、顺铂或卡铂、拓扑异构酶I抑制剂以及紫杉烷类)联合使用时,其抗癌效果会得到优化。本文还综述了可优化基于奥沙利铂的化疗的体外和临床前联合用药数据。

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