Jain Sarika, Cigler Tessa
Department of Medicine, Weill Cornell Medical College, New York, NY, USA.
Biologics. 2012;6:21-9. doi: 10.2147/BTT.S19811. Epub 2012 Jan 1.
The treatment of metastatic breast cancer (MBC) has become increasingly challenging as the primary goals of therapy include prolonging life without added toxicity. While multiple agents are approved for the therapy of MBC, there is no standard approach for therapy beyond the second-line. Eribulin mesylate, an analog of the marine sponge halichondrin B, is a non-taxane microtubule dynamics inhibitor with a mechanism of action distinct from other tubulin-targeted drugs. Based on a significant extension in overall survival seen in a Phase III clinical trial, eribulin was approved for third-line therapy in MBC patients following anthracycline and taxane failure. Eribulin has a manageable toxicity profile and a low incidence of peripheral neuropathy. In this review, we discuss the natural source of eribulin, pharmacology, mode of action, preclinical and clinical data, and patient-focused perspectives.
转移性乳腺癌(MBC)的治疗变得越来越具有挑战性,因为治疗的主要目标包括延长生命且不增加毒性。虽然多种药物被批准用于MBC的治疗,但二线以上治疗尚无标准方法。甲磺酸艾瑞布林是海洋海绵软海绵素B的类似物,是一种非紫杉烷类微管动力学抑制剂,其作用机制与其他微管蛋白靶向药物不同。基于一项III期临床试验中观察到的总生存期显著延长,艾瑞布林被批准用于蒽环类和紫杉烷类治疗失败后的MBC患者的三线治疗。艾瑞布林具有可控的毒性特征和较低的周围神经病变发生率。在本综述中,我们讨论了艾瑞布林的天然来源、药理学、作用方式、临床前和临床数据以及以患者为中心的观点。