第三代EGFR抑制剂研究进展  

Research Progress in the Third-generation of EGFR Inhibitors

作　　者：孔月月 饶国武[1] KONG Yue-yue;RAO Guo-wu(College of Pharmaceutical Science,Zhejiang University of Technology,Hangzhou,Zhejiang 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《浙江化工》2019年第1期14-22,共9页Zhejiang Chemical Industry

摘　　要：EGFR是细胞膜表面的表皮生长因子受体,具有酪氨酸激酶(tyrosine kinase, TK)活性。随着第一代EGFR抑制剂在临床治疗中靶点出现了T790M突变,从而发展了第二代EFGR抑制剂。然而在治疗过程中出现了野生型的EGFR T790M靶点,并且对第二代TKI产生了耐药性,随之发展了第三代EFGR抑制剂。本文对近几年出现的以第三代EGFR抑制剂进行简要总结。EGFR is an epidermal growth factor receptor on the cell membrane surface. It has tyrosine kinase (TK) activity. As the first-generation of EGFR inhibitors showed T790M mutations in clinical targets, the second-generation of EFGR inhibitors was generated. However, a wild-type EGFR T790M target has emerged and resistance to the second-generation of TKI has developed during treatment. This led to the third-generation of EFGR inhibitors. In this paper, the third-generation of EGFR inhibitors in recent years was briefly summarized.

关 键 词：EGFR EGFRT790M 耐药性 第三代EFGR抑制剂 

分 类 号：R979.1[医药卫生—药品]