达沙替尼药动学及治疗药物监测研究进展  

Research development on pharmacokinetics and therapeutic drug monitoring of dasatinib

作　　者：罗兴献 黄琳[1] 赵海艳[1] 薛学财[1,2] 胡蕾 杨长青 冯婉玉 LUO Xing-xian;HUANG Lin;ZHAO Hai-yan;XUE Xue-cai;HU Lei;YANG Chang-qing;FENG Wan-yu(Department of Pharmacy,People Hospital of Peking University,Belting 100044,China;School of Basic Medicine and Clinical Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]北京大学人民医院药剂科,北京100044 [2]中国药科大学基础医学与临床药学学院,南京211198

出　　处：《中国新药杂志》2018年第15期1737-1743,共7页Chinese Journal of New Drugs

摘　　要：酪氨酸激酶抑制剂(TKIs)对肿瘤细胞的增殖和凋亡起重要的作用,常用于慢性粒细胞白血病、胃肠间质肿瘤、非小细胞肺癌等多种疾病,具有高选择性、不良反应少等特点。达沙替尼作为第2代口服广谱酪氨酸激酶抑制剂,通过抑制BCR-ABL、SRC家族、C-Kit和PDGF-B等多种酪氨酸激酶,广泛用于甲磺酸伊马替尼耐药或不耐受的慢性白血病患者。随着临床应用增加,其药物的疗效和不良反应逐渐显现出来。本文基于近几年来的文献,对达沙替尼的药物作用机制、药动学特点、药物安全性及治疗药物监测等方面进行综述,以期为达沙替尼个体化合理用药指导提供思路。Tyrosine kinase inhibitors（TKIS） play an important role in tumor cell proliferation and apoptosis,and are commonly used in treatment of cancers including chronic myeloid leukemia,gastrointestinal stromal tumors and non-cell lung cancer diseases with high selectivity and fewer adverse effects. As a second-generation oral broadspectrum tyrosine kinase inhibitor,Dasatinib are widely used in chronic leukemia patients resistance or intolerance of methanesulfonic acid imatinib by inhibiting BCR-ABL,SRC family,C-Kit,PDGF-B and other tyrosine kinases.With the increase in clinical application,the efficacy and adverse reactions of dasatinib have gradually emerged.Based on the literatures of recent years,this paper reviews the drug mechanism,pharmacokinetic characteristics,drug safety and therapeutic drug monitoring of dasatinib so as to provide references for the personalized and rational drug use of dasatinib.

关 键 词：达沙替尼 慢性粒细胞白血病 酪氨酸激酶抑制剂 药动学 治疗药物监测 

分 类 号：R972[医药卫生—药品]