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盐酸伊立替康(CPT - 11)

[Irinotecan hydrochloride (CPT-11)].

作者信息

Furue H

机构信息

Fourth Dept. of Internal Medicine, Teikyo University School of Medicine, Kawasaki, Japan.

出版信息

Gan To Kagaku Ryoho. 1994 Apr;21(5):709-17.

PMID:8154899
Abstract

Irinotecan hydrochloride (CPT-11) is a water-soluble semisynthetic derivative of camptothecin. CPT-11 is a prodrug that undergoes deesterification in vivo to produce SN-38, a metabolite that is 1,000-fold more potent than the parent compound in vitro. CPT-11 is a potent topoisomerase I inhibitor with a broad spectrum of experimental antitumor activity. Recent clinical trials also reveal that CPT-11 is very effective in the treatment of cancers including lung cancer, cervix cancer, ovary cancer, etc. Now, comparative trials of combination chemotherapy in responsive tumors are indicated from these excellent clinical results.

摘要

盐酸伊立替康(CPT - 11)是喜树碱的水溶性半合成衍生物。CPT - 11是一种前体药物,在体内进行去酯化反应生成SN - 38,该代谢产物在体外的活性比母体化合物强1000倍。CPT - 11是一种强效的拓扑异构酶I抑制剂,具有广泛的实验性抗肿瘤活性。近期的临床试验还表明,CPT - 11在治疗包括肺癌、宫颈癌、卵巢癌等多种癌症方面非常有效。现在,基于这些出色的临床结果,有必要针对反应性肿瘤进行联合化疗的对比试验。

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