药物诱导CYP450的体外检测方法研究进展

中国临床药理学与治疗学 ›› 2010, Vol. 15 ›› Issue (8): 954-960.

• 综述与讲座 • 上一篇

药物诱导CYP450的体外检测方法研究进展

苏静华, 孙建国, 王广基

中国药科大学药物代谢动力学重点实验室,南京 210009,江苏

收稿日期:2010-03-15 修回日期:2010-04-19 出版日期:2010-08-26 发布日期:2020-09-17
通讯作者: 王广基,男,教授,研究方向:药物代谢动力学。E-mail: guangjiwang@hotmail.com孙建国,男,副教授,研究方向:药物代谢动力学。E-mail: jgsuncpucn@yahoo.com.cn
作者简介:苏静华,女,硕士研究生,研究方向:药物代谢动力学。Tel: 13524613006 E-mail: susan0702@163.com
基金资助:
中央高校基本科研业务费专项资助(项目批准号JKP2009007);国家自然科学基金(30901832)

Current practices and recommendations of in vitro induction of Cytochrome P450

SU Jing-hua, SUN Jian-guo, WANG Guang-ji

Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009,Jiangsu, China

Received:2010-03-15 Revised:2010-04-19 Online:2010-08-26 Published:2020-09-17

摘要/Abstract

摘要： 在联合用药时,药物之间时常发生的代谢动力学相互作用是药物疗效发生改变的重要因素之一。细胞色素P450酶被诱导是影响药物代谢动力学的一个主要原因。近年来,CYP450酶诱导的体外检测方法被广泛运用,根据核受体能激活酶基因的转录,建立了一些核受体[芳香烃受体(AhR)、孕烷X受体(PXR)和组成型雄甾烷受体(CAR)]测定方法;体外肝细胞能有效地反映酶诱导效应,是最常用的检测工具。通过体外酶诱导的检测数据预测体内药物相互作用,为进一步的在体和临床研究提供指导意见。本文主要综述了近年来常用的几种测定方法的原理、应用、数据分析以及发展现状。

关键词: 细胞色素P450 , 诱导, 测定

Abstract: Cytochrome P450 (CYP) induction is one of the factors that can affect the pharmacokinetics of a drug molecule upon multiple dosing, and can result in pharmacokinetic drug-drug interactions with coadministered drugs causing potential therapeutic effect change. In recent years, various in vitro assays have been developed and used routinely to assess the potential for drug-drug interactions due to CYP induction, such as nucleolus receptors assay(PXR, AhR, CAR assays) and hepatocyte assays which is more effective. With the data from in vitro assays, we can assess the potential for drug-drug interactions and plan appropriate in vivo and clinical research. This review summaries the currently used models and data interpretation.

Key words: Cytochrome P450, Induction, Assay

中图分类号:

R969.1

苏静华, 孙建国, 王广基. 药物诱导CYP450的体外检测方法研究进展[J]. 中国临床药理学与治疗学, 2010, 15(8): 954-960.

SU Jing-hua, SUN Jian-guo, WANG Guang-ji. Current practices and recommendations of in vitro induction of Cytochrome P450[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2010, 15(8): 954-960.

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药物诱导CYP450的体外检测方法研究进展

Current practices and recommendations of in vitro induction of Cytochrome P450

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