Literature DB >> 19356071

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

Loren M Berry1, Zhiyang Zhao.   

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.

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Year:  2008        PMID： 19356071     DOI： 10.2174/187231208783478407

Source DB:  PubMed          Journal:  Drug Metab Lett        ISSN： 1872-3128


  14 in total

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3.  P450-Based Drug-Drug Interactions of Amiodarone and its Metabolites: Diversity of Inhibitory Mechanisms.

Authors:  Matthew G McDonald; Nicholas T Au; Allan E Rettie
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4.  Reversible Mechanisms of Enzyme Inhibition and Resulting Clinical Significance.

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5.  Evaluation of Strategies for the Assessment of Drug-Drug Interactions Involving Cytochrome P450 Enzymes.

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Journal:  Eur J Drug Metab Pharmacokinet       Date:  2018-12       Impact factor: 2.441

6.  The Application of Mass Spectrometry in Drug Metabolism and Pharmacokinetics.

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Journal:  Adv Exp Med Biol       Date:  2021       Impact factor: 2.622

7.  In Vitro Evaluation of Reversible and Time-Dependent Inhibitory Effects of Kalanchoe crenata on CYP2C19 and CYP3A4 Activities.

Authors:  Charles Awortwe; Vamshi K Manda; Cristina Avonto; Shabana I Khan; Ikhlas A Khan; Larry A Walker; Patrick J Bouic; Bernd Rosenkranz
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8.  In vitro-in vivo extrapolation of zolpidem as a perpetrator of metabolic interactions involving CYP3A.

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Review 9.  Time-dependent enzyme inactivation: Numerical analyses of in vitro data and prediction of drug-drug interactions.

Authors:  Jaydeep Yadav; Erickson Paragas; Ken Korzekwa; Swati Nagar
Journal:  Pharmacol Ther       Date:  2019-12-11       Impact factor: 12.310

10.  A systematic approach to evaluate herb-drug interaction mechanisms: investigation of milk thistle extracts and eight isolated constituents as CYP3A inhibitors.

Authors:  Scott J Brantley; Tyler N Graf; Nicholas H Oberlies; Mary F Paine
Journal:  Drug Metab Dispos       Date:  2013-06-25       Impact factor: 3.922
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