Combretastatin A4的抗肿瘤作用研究进展  

Vascular targeting agent-Combretastatin A4

作　　者：任萱[1] 林莉萍[1] 丁健[1] 

机构地区：[1]中国科学院上海药物所新药研究国家重点实验室肿瘤药理组,上海201203

出　　处：《中国新药杂志》2007年第17期1336-1341,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金面上项目(30572201)

摘　　要：肿瘤细胞的生存和发展需要完整的血管系统提供氧气、养料并输送废物,同时提供转移的主要路线,因此肿瘤血管成为肿瘤治疗中一个很有吸引力的靶点。以往大量的研究集中在抗新生血管生成方面,近年来对于肿瘤血管靶向药物(Vascular targeting agents)的研究逐渐增多,此类药物针对肿瘤既存血管产生迅速且有选择性的破坏作用,使肿瘤细胞由于氧气和养料缺乏而死亡。Combretastatin A4作为其中的一个候选化合物,吸引众多的研究人员对其体内外药理作用进行研究,该候选化合物的水溶性前药已经被OxiGen公司开发,目前在美国和欧洲进行II期临床试验,且已获准进入美国FDA快速通道审批。现就其体内外药效学、作用机制以及临床研究进展作一综述。A growing solid tumor relies on a developing vasculature to meet its needs in terms of oxygen, nutrients and depuration, as well as providing a main route for metastatic spread. Tumor vasculature represents an appealing target for the development of new cancer treatments. Most of the research efforts have been focused on antiangiogenic therapy. However, recently there was increased interest in developing agents, which irreversibly damage the already formed neovasculature in tumors so called vascular targeting agents （VTAs）. Many research focus on Combretastatin A4, one of the leading compound of the small molecular VTA for its remarkable anti-vascular effect in vitro and in vivo. Combretastatin A4 phosphate （CA4P） , the water soluble prodrug of CA4 has been developmented by OxiGen.

关 键 词：肿瘤血管 抗新生血管生成 肿瘤血管靶向药物 Combertastafin A4 COMBRETASTATIN A4磷酸盐 

分 类 号：R979.1[医药卫生—药品] R965.1[医药卫生—药学]