分子靶向抗肿瘤药物的作用机制及临床研究进展.pdf

1232 药学学报 Acta Pharmaceutica Sinica 20 15, 50 ( 10): 1232 1239 子靶向抗肿瘤药物的作用机制及临床研究进展 * 胡宏祥, 王学清, 张 华, 张 强 (北京大学药学院, 北京 100191) 摘要: 肿瘤分子靶向药物因其特异性强、耐受性好等特点, 在肿瘤治疗中占有越来越重要的地位。分子靶向 治疗药物的种类很多, 包括单克隆抗体和小分子激酶抑制剂等, 从 1997 年首个单抗药物利妥昔单抗上市到目前 为止, 已被批准上市的药物达 50 多种, 抗肿瘤靶点也趋于多样化。以肿瘤细胞特异性分子靶点为导向的药物研 发已经成为现代抗肿瘤药物发展的主流趋 。本文对FDA 批准上市的分子靶向药物进行总结, 按照作用靶点的 不同进行分类, 并对各类药物的分子机制及临床使用情况作一概述。 关键词: 分子靶向治疗; 单克隆抗体; 蛋白酪氨酸激酶; 抗肿瘤 中图 类号: R943 文献标识码: A 文章编号: 0513-4870 (20 15) 10- 1232-08 Mechanism and clinical progress of molecular targeted cancer therapy * HU Hong-xiang, WANG Xue-qing, ZHANG Hua , ZHANG Qiang (School of Pharmaceutical Sciences, Peking University, Beij ing 100191, China ) Abstract : Molecular target-based cancer therapy is playing a more and more important role in cancer therapy because of its high specificity, good tolerance and so on. There are different kinds of molecular targeted drugs such as monoclonal antibodies and small molecular kinase inhibitors, and more than 50 drugs have been approved since 1997. When the first monoclonal antibody, rituximab, was on the market. The development of molecular target-based cancer therapeutics has become the main approach. Based on this, we summarized the drugs approved by FDA and introduced their mechanism of actions and clinical applications. In order to incorporate most molecular targeted drugs and describe clearly various characteristics, we divided them into four cat