Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors | |
Ding Juefang; Zhong Dafang![]() | |
刊名 | Acta Pharmaceutica Sinica
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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 |
内容类型 | 期刊论文 |
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. |
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