新型非紫杉类微管动力抑制剂——Eribulin的研究进展  

A study on mechanistically-unique microtubule inhibitor——Eribulin

作　　者：吴玲[1] 彭娟[1] 

机构地区：[1]中南大学药学院,湖南长沙410013

出　　处：《肿瘤药学》2011年第4期327-329,共3页Anti-Tumor Pharmacy

摘　　要：复发性和转移性乳腺癌是目前难以治愈的疾病之一。Halaven(eribulin甲磺酸盐)是来源于深海中一种黑色海绵类生物的天然产物Haichondrin(HB)的合成衍生物。它是一种非紫杉类微管抑制剂,通过抑制微管的运动,从而表现出抗有丝分裂的作用,引起癌细胞的凋亡。目前已完成Ⅲ期临床试验,于2010年11月通过美国食品药品局批准上市,成为治疗接受过至少两种化疗方案的复发性和转移性乳腺癌患者的新选择。Currently recurrent and metastatic Breast cancer is one of the difficult to cured disease. Eribulin（E7389）, a macrocyclic ketone analog of the marine natural product Halichondrin B, and is a mechanistically-unique mierotubule non-taxol-inhihitor. Eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assenrbly of microtubules, l^s@ing in inhibition of mitotic spindle assembly, induction of cell cycle an＇est al G2/M phase, and, potentially, nmlor regression. A phase m clinical trial has been finished at present. United States Food and Drug Administration approved eribulin mesylate appear in the market in Nov. 2010, which has come a new choice for those who with me,static breast cancer received at least two chemotherapy strategies.

关 键 词：Halaven(eribulin甲磺酸盐) 复发性和转移性乳腺癌 临床试验 

分 类 号：R73[医药卫生—肿瘤] R97[医药卫生—临床医学]