Department of Oncology, Catholic University of the Sacred Heart, Campobasso, Italy.
Curr Pharm Des. 2012;18(19):2793-803. doi: 10.2174/138161212800626238.
Among the drugs targeting microtubule functions by interfering with tubulin subunits, epothilones represent a class of anticancer agents which recently entered clinical development. Although epothilones share mechanisms of action similar to taxanes, they have non-overlapping mechanisms of resistance; in particular, while overexpression of class III β-tubulin plays a major role in taxane resistance, epothilones display their highest efficacy in class III β-tubulin overexpressing malignancies. Three compounds belonging to this family (patupilone, ixabepilone and sagopilone), have been actively investigated in clinical trials, and some of them are at an advanced stage of development. This review provides a comprehensive analysis of the available literature on epothilones, focusing on their clinical development and potential as an additional weapon in the arsenal against tumors.
在通过干扰微管蛋白亚基来靶向微管功能的药物中，埃坡霉素类代表了一类最近进入临床开发的抗癌药物。尽管埃坡霉素类与紫杉烷类具有相似的作用机制，但它们具有非重叠的耐药机制；特别是，虽然 III 类β-微管蛋白的过表达在紫杉烷类耐药中起主要作用，但埃坡霉素类在 III 类β-微管蛋白过表达的恶性肿瘤中显示出最高的疗效。该家族的三种化合物（帕他泊隆、伊沙匹隆和沙格泊隆）已在临床试验中得到积极研究，其中一些已处于开发的后期阶段。本文对埃坡霉素类的现有文献进行了全面分析，重点介绍了它们的临床开发及其作为对抗肿瘤的另一种武器的潜力。
