新一代TKI类药物瑞派替尼在胃肠间质瘤中的作用及研究进展  

The role of a new generation of TKI ripretinib in gastrointestinal stromal tumor treatment and its research progress

作　　者：张轶雯 潘宗富 叶强[1] 刘宇佳 孙娇[2] 李莉 黄萍 ZHANG Yi-wen;PAN Zong-fu;YE Qiang;LIU Yu-jia;SUN Jiao;LI Li;HUANG Ping(Department of Pharmacy,Zhejiang Provincial People's Hospital,People's Hospital of Hangzhou Medical College,Hangzhou 310014,China;Department of Pharmacy,Zhejiang Cancer Hospital,Hangzhou 310022,China;Department of Pharmacy,the First People's Hospital of Chun-an,Hangzhou 311700,China)

机构地区：[1]浙江省人民医院,杭州医学院附属人民医院药学部,杭州310014 [2]浙江省肿瘤医院药剂科,杭州310022 [3]浙江省淳安县第一人民医院药剂科,杭州311700

出　　处：《中国新药杂志》2020年第23期2690-2694,共5页Chinese Journal of New Drugs

基　　金：浙江省自然科学基金(LY20H310001,LYQ20H310001);浙江省医药卫生科技计划项目(2018KY297,2019KY047,2019KY559)。

摘　　要：胃肠间质瘤是一种较为罕见的消化系统肿瘤,具有较大的肿瘤异质性。传统酪氨酸激酶抑制剂(TKI)类药物由于作用靶点相对单一,在胃肠间质瘤治疗中存在一定局限。瑞派替尼作为一种新型的TKI,可有效抑制原癌基因KIT和血小板源生长因子受体α(PDGFRα)广谱突变导致的激酶活化从而发挥抗肿瘤作用。本文从临床前及临床研究两方面,深入阐述瑞派替尼的双重作用机制及疗效,为其临床应用提供参考。Gastrointestinal stromal tumor(GIST) is a rare malignant neoplasm of digestive system with a great heterogeneity.The traditional TKI drugs have limitations in the treatment of gastrointestinal stromal tumors due to their single targets.As a novel tyrosine kinase inhibitor,ripretinib can effectively inhibit the kinase activation caused by broad-spectrum mutation of KIT and PDGFRα,then play an anti-tumor role.In this paper,dual mechanisms of ripretinib are expounded from pre-clinical and clinical research aspects,providing reference for the clinical application.

关 键 词：瑞派替尼 胃肠间质瘤 KIT PDGFRΑ 研究进展 

分 类 号：R979.1[医药卫生—药品]