摘要
埃坡霉素(epothilones)是一类非紫杉烷类促微管蛋白聚合剂,其作用机制与紫杉醇相似,但结构完全不同,临床前研究结果显示其细胞毒活性较紫杉醇强,对紫杉类耐药的细胞株和小鼠肿瘤移植模型显示出较强的抗肿瘤活性。近来合成或半合成了很多埃坡霉素类似物,目前已进入临床抗肿瘤治疗研究的埃坡霉素类似物主要有ixabepilone、patupilone、BMS-310705、ZK -EPO、KOS-862及KOS-1584。现有的临床研究结果提示部分接受过紫杉类药物治疗的晚期乳腺癌、卵巢癌、膀胱癌或非小细胞肺癌患者埃坡霉素治疗有效。本文就埃坡霉素的化学结构,作用机制、药理活性及毒副作用等临床研究的进展进行了回顾和综述。
Epothilones are 16 -member ring macrolides with antimicrotubule activity that share a similar mechanism of action to the taxanes but with the potential advantage of activity in taxane-resistant settings in preclinical models. They are structurally unrelated to the taxanes. Recently, a wealth of new analogue has been developed in the biosynthesis and clinical administration of epothilones. The epothilones ixabepilone, patupilone, BMS- 310705, KOS- 862, KOS- 1584, and ZK- EPO are in early clinical trials for cancer treatment. In these studies, the responses to epothilones have been observed in some taxane pretreated patients with breast, ovarian, bladder, and non-small-cell lung cancers. This review presents recent progress in mechanisms of action, antitumor activity, and side-effects of epothilones.
出处
《癌症进展》
2009年第1期44-51,11,共9页
Oncology Progress
