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Drug Metab Lett. 2008 Jan;2(1):51-9.

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

Author information

1
Pharmacokinetics and Drug Metabolism, Amgen, Inc., 1 Kendal Sq., Cambridge, MA 02139, USA. loren.berry@amgen.com

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.

PMID:
19356071
DOI:
10.2174/187231208783478407
[Indexed for MEDLINE]

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