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在评估人肝微粒体中CYP3A4、CYP2D6和CYP2C9的时间依赖性抑制作用时对IC50和IC50位移实验的考察。

An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes.

作者信息

Berry Loren M, Zhao Zhiyang

机构信息

Pharmacokinetics and Drug Metabolism, Amgen, Inc., 1 Kendal Sq., Cambridge, MA 02139, USA.

出版信息

Drug Metab Lett. 2008 Jan;2(1):51-9. doi: 10.2174/187231208783478407.

DOI:10.2174/187231208783478407
PMID:19356071
Abstract

The relationship between time-dependent inactivation (TDI) and IC50 is examined using a consolidated method for evaluating CYP450 inhibition during drug discovery. An IC50 fold-shift of >1.5 indicated significant TDI potency. Further, the "shifted IC50" could be used to estimate, the K(I) and TDI potency ratio k(inact)/K(I) to within 2-fold in most cases.

摘要

在药物研发过程中，采用一种综合方法来评估细胞色素P450（CYP450）抑制作用，以此研究时间依赖性失活（TDI）与半数抑制浓度（IC50）之间的关系。IC50变化倍数>1.5表明具有显著的TDI效力。此外，在大多数情况下，“变化后的IC50”可用于估计抑制常数（K(I)）以及TDI效力比k(inact)/K(I)，误差在2倍以内。

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