Jimeno Antonio
Clin Cancer Res. 2009 Jun 15;15(12):3903-5. doi: 10.1158/1078-0432.CCR-09-1023. Epub 2009 Jun 9.
Eribulin mesylate (E7389) is a synthetic analog of the marine macrolide halichondrin B, which acts as a novel microtubule modulator with a distinct mechanism of action. Two eribulin mesylate phase 1 studies exploring weekly and 3-weekly schedules are reported in this issue. These trials show linear pharmacokinetics, a toxicity profile consisting in neutropenia and fatigue, and early hints of antitumor activity. In this commentary we give a brief historical perspective of the halichondrins and put into context eribulin mesylate as a novel tubulin modulator.
甲磺酸艾瑞布林(E7389)是海洋大环内酯类化合物海兔毒素B的合成类似物,它作为一种新型微管调节剂,具有独特的作用机制。本期报道了两项探索每周给药和每3周给药方案的甲磺酸艾瑞布林1期研究。这些试验显示出线性药代动力学、以中性粒细胞减少和疲劳为主的毒性特征,以及抗肿瘤活性的早期迹象。在本述评中,我们简要介绍了海兔毒素的历史背景,并将甲磺酸艾瑞布林作为一种新型微管蛋白调节剂进行了阐述。