Albert Einstein College of Medicine, Department of Medical Oncology, Montefiore Medical Center, 1695 Eastchester Road, Bronx, NY 10461, United States.
Crit Rev Oncol Hematol. 2012 Feb;81(2):163-84. doi: 10.1016/j.critrevonc.2011.03.002. Epub 2011 Apr 14.
Eribulin mesylate is a non-taxane, structurally simplified, completely synthetic, halichondrin B derivative with an end poisoning, microtubule inhibitory action. Preclinical studies have demonstrated activity in various cancer cell lines and synergistic action with gemcitabine, epirubicin, trastuzumab, cisplatin, docetaxel and vinorelbine. Eribulin has recently been approved by United States Food and Drug Administration as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has also advanced to phase II trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Combination trials with carboplatin, gemcitabine, pemetrexed, cisplatin, and erlotinib are currently ongoing. Eribulin potentially has a low incidence of peripheral neuropathy. The predominant side effects are neutropenia and fatigue, which are manageable. This article reviews the available information on eribulin with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, preclinical studies and clinical trials.
甲磺酸艾日布林是一种非紫杉烷类、结构简化、完全合成的海鞘素 B 衍生物，具有末端中毒、微管抑制作用。临床前研究表明，它在各种癌细胞系中均具有活性，并与吉西他滨、表柔比星、曲妥珠单抗、顺铂、多西他赛和长春瑞滨具有协同作用。甲磺酸艾日布林最近已被美国食品和药物管理局批准用于转移性乳腺癌患者的三线治疗，这些患者先前已接受过蒽环类药物和紫杉烷类药物治疗。它也已进入非小细胞肺癌、胰腺癌、前列腺癌、膀胱癌、头颈部癌、肉瘤和卵巢癌及其他妇科肿瘤的 II 期临床试验。目前正在进行与卡铂、吉西他滨、培美曲塞、顺铂和厄洛替尼联合治疗的试验。甲磺酸艾日布林的周围神经病变发生率可能较低。主要副作用是中性粒细胞减少和疲劳，这些副作用是可以控制的。本文综述了有关甲磺酸艾日布林的临床药理学、作用机制、药代动力学、药效学、代谢、临床前研究和临床试验的现有信息。
