紫杉烷类抗肿瘤药物临床研究进展  

Advances in clinical research of taxane anticancer drugs

作　　者：陈坤成[1,2] 冯思良[2] 刘克良[2] 

机构地区：[1]中南大学药学院,长沙410013 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2013年第3期271-276,共6页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2012ZX09301003-004)

摘　　要：紫杉醇是一种重要的抗肿瘤药物,它能特异地作用于微管蛋白,促进微管蛋白的聚合并阻止其解聚,从而阻断有丝分裂过程,导致细胞凋亡。紫杉醇抗肿瘤谱广,疗效确切,在临床上已广泛应用。然而,由于不溶于水、选择性差等原因,紫杉醇存在着诸如毒副作用大(骨髓抑制、周围感觉神经病变)、使用不便以及易产生耐药性、无法透过血脑屏障等缺陷。针对这些问题,药物学家们从化合物结构以及制剂等角度着手研究,获得了一些疗效显著的紫杉醇类似物、紫杉醇前药及紫杉醇新剂型。本文对这些新型紫杉醇衍生物和新剂型单独给药或联合用药的最新临床研究进展进行了综述。Paclitaxel is an important antitumor drug which kills the tumor cells by promoting the microtubulin to polymerize and preventing the progress of mitosis.It has been widely used in clinical treatment of many kinds of cancers.However,pacliaxel still has some disadvantages such as dose-limiting toxicities,inconvenience to use,multidrug resistance and disability to cross the blood brain barrier.Many researchers have contributed to solving these problems by chemical modifications or development of new preparations.In this review,we report recent clinical progresses of several novel paclitaxel analogues,paclitaxel prodrugs and new formulations in various solid tumor malignancies.

关 键 词：紫杉醇 紫杉醇类似物 紫杉醇前药 紫杉醇新剂型 

分 类 号：R979.1[医药卫生—药品]