酪氨酸激酶抑制剂药动学研究进展  

Progress in pharmacokinetic studies of tyrosine kinase inhibitors

作　　者：张师[1] 王明霞[1] 冯章英[1] 

机构地区：[1]河北医科大学第四医院,石家庄050011

出　　处：《中国新药杂志》2016年第14期1600-1607,共8页Chinese Journal of New Drugs

基　　金：河北省卫生厅医学科学研究重点课题项目(20100122);河北省中医药管理局科研计划项目(2013161);河北省人力资源和社会保障厅留学回国人员科技活动择优资助项目(20100313)

摘　　要：酪氨酸激酶因在肿瘤中高表达且与肿瘤细胞的生长、增殖、转移密切相关,而被作为肿瘤治疗的一个重要靶点来进行研究。酪氨酸激酶抑制剂是以受体酪氨酸激酶为靶点的药物,具有选择性高、疗效好、不良反应少等特点。但是这些药物在吸收、分布、代谢、排泄等方面具有差异。因此,本文总结了近几年的国内外相关文献,比较了吉非替尼、厄洛替尼、埃克替尼、拉帕替尼、阿法替尼、达克替尼、AZD9219、阿帕替尼以及克唑替尼的药动学并进行综述,为临床合理用药提供理论依据。Tyrosine kinase is highly expressed in tumors,and closely relates to tumor cell growth,proliferation,and metastasis. Therefore,it is an important target for tumor therapy. Tyrosine kinase inhibitors are the drugs targeting receptor tyrosine kinase with high selectivity and efficacy,and lower adverse reactions. However,the absorption,distribution,metabolism,and excretion of these drugs are different. Therefore,in this paper we summarized the relevant literature at home and abroad in recent years,compared pharmacokinetics of gefitinib,erlotinib,icotinib,lapatinib,afatinib,dacomitinib,AZD9219,apatinib and crizotinib. Our goal is to provide a theoretical basis for clinical rational use of these drugs.

关 键 词：酪氨酸激酶抑制剂 非小细胞肺癌 乳腺癌 胃癌 药动学 细胞色素P450 

分 类 号：R286.91[医药卫生—中药学]