细胞色素P450酶的时间依赖性抑制研究及其在新药研发中的作用被引量：3

Research advances of time-dependent inhibition of cytochrome P450 enzymes in drug discovery and development

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摘要细胞色素P450酶介导绝大多数药物的体内代谢,有些临床药物相互作用问题是由于药物对细胞色素P450酶的时间依赖性抑制引起的,但在传统的体外抑制筛选方法中并未包括对时间依赖性抑制的评价方案。本文综述了药物时间依赖性抑制的研究意义及评价方法 (包括单点抑制法、IC50shift筛选法、酶动力学实验法等),并介绍如何利用所得体外数据进行临床预测。 Cytochrome P450 enzymes mediated the metabolism of the overwhelming majority of drugs. Some clinical drug interaction problems were due to the drugs caused by time-dependent inhibition （TDI） of cytochrome P450 enzymes. However, TDI study was not included in routine in vitro inhibition screening protocols. This artical reviewed the significance and evaluation methods of TDI research. Meanwhile, an introduction on the strategies for clinical prediction using in vitro data was presented.

作者谢珊珊王盼郭建军詹彧卜海之陈西敬

机构地区中国药科大学药物代谢研究中心苏州圣苏新药开发有限公司

出处《中国新药与临床杂志》 CAS CSCD 北大核心 2013年第6期419-426,共8页 Chinese Journal of New Drugs and Clinical Remedies

基金苏州科学技术局姑苏创新创业领军人才基金资助(XG0826)

关键词细胞色素P450 时间依赖性抑制生物转化构效关系机理性抑制药物相互作用临床预测 cytochrome P450 time- dependent inhibition biotransformation structure- activity rela-tionship mechanism-based inactivation drug interactions clinical prediction

分类号 R96 [医药卫生—药理学]

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