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Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors

文献类型：期刊论文

作者Ding Juefang; Zhong Dafang
刊名Acta Pharmaceutica Sinica
出版日期2013
卷号48期号:7页码:1080-1090
关键词tyrosine kinase inhibitor pharmacokinetics drug-drug interaction
ISSN号0513-4870
其他题名小分子酪氨酸激酶抑制剂的临床药代动力学研究进展
文献子类Review
英文摘要Human protein tyrosine kinases play an essential role in carcinogenesis and have been recognized as promising drug targets. By the end of 2012, eight small molecule tyrosine kinase inhibitors (TKIs) have been approved by State Food and Drug Administration of China for cancer treatment. In this paper, the pharmacokinetic characteristics (absorption, distribution, metabolism and excretion) and drug-drug interactions of the approved TKIs are reviewed. Overall, these TKIs reach their peak plasma concentrations relatively fast; are extensively distributed and highly protein bound (<90%); are primarily metabolized by CYP3A4; most are heavily influenced by CYP3A4 inhibitors or inducers except for sorafenib; are mainly excreted with feces and only a minor fraction is eliminated with the urine; and are substrate of the efflux transporters ABCB1 (P-gp) and ABCG2 (BCRP). Additionally, many of the TKIs can inhibit some CYP450 enzymes, UGT enzymes, and transporters. Gefitinib, erlotinib, dasatinib, and sunitinib are metabolized to form reactive metabolites capable of covalently binding to biomolecules.
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:4882824
源URL[http://119.78.100.183/handle/2S10ELR8/267773]  
专题上海药物代谢研究中心
通讯作者Zhong Dafang
作者单位Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China.
推荐引用方式
GB/T 7714		 Ding Juefang,Zhong Dafang. Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors[J]. Acta Pharmaceutica Sinica,2013,48(7):1080-1090.
APA Ding Juefang,&Zhong Dafang.(2013).Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors.Acta Pharmaceutica Sinica,48(7),1080-1090.
MLA Ding Juefang,et al."Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors".Acta Pharmaceutica Sinica 48.7(2013):1080-1090.

入库方式： OAI收割

来源：上海药物研究所

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