埃坡霉素类化合物临床研究进展

Clinical research progress of epothilone analogues

埃坡霉素类化合物是一种新型的抗肿瘤药物,通过与肿瘤细胞中的微管蛋白结合,促进微管蛋白聚合并抑制微管的解聚,使细胞周期停止,最终诱导细胞凋亡。动物实验显示其具有广泛的抗肿瘤活性,并可作用于已经产生多药耐药性的肿瘤患者。目前有多个此类化合物正处于临床试验阶段,是一类非常有前景的抗肿瘤药物。本文对具有代表性的几个埃坡霉素类化合物的临床药代动力学及其毒性反应研究进行综述。

Epothilone analogues are a new type of antitumor drugs, which can promote the polymerization of tubulin heterodimers into microtubule polymers, stabilize microtubules against depolymerization, induce mitotic cell cycle arrest and eventually apoptosis. They have showed broad antitumor activity in different animal models, and have significant effect in multidrug-resistant tumor patients. This kind of compounds has a promising application prospect in antitumor therapy, some of which have advanced into clinical studies. In this article, the clinical pharmacokinetics and adverse reactions of several epothilone analogues are reviewed.