In-vitro CYP inhibition pooled v1

This assay is crucial for understanding a compound's inhibitory profile across major drug-metabolizing enzymes, providing essential data for predicting clinical drug-drug interactions and supporting regulatory submissions in pharmaceutical development. An in vitro CYP inhibition assay evaluates the potential of a test compound to inhibit multiple cytochrome P450 enzymes simultaneously using a cocktail approach. This pooled assay employs a mixture of substrates specific to different CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 & CYP3A4) combined with a pooled enzyme source, such as human liver microsomes. The cocktail method offers several advantages over individual isoform testing, including: Reduced material consumption - Single test compound aliquot tests multiple CYP enzymes Higher throughput screening - Multiple CYP interactions assessed simultaneously Early drug development efficiency - Rapid identification of potential drug-drug interaction liabilities

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Publication Details

Published
2025-05-25
DOI
https://doi.org/10.17504/protocols.io.81wgbkb1ygpk/v1
Primary Topic
Pharmacogenetics and Drug Metabolism
Type
article
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article

In-vitro CYP inhibition pooled v1

Nick Lynch
Pharmacogenetics and Drug Metabolism
article

In-vitro CYP inhibition pooled v1

Nick Lynch
article en

Abstract

This assay is crucial for understanding a compound's inhibitory profile across major drug-metabolizing enzymes, providing essential data for predicting clinical drug-drug interactions and supporting regulatory submissions in pharmaceutical development. An in vitro CYP inhibition assay evaluates the potential of a test compound to inhibit multiple cytochrome P450 enzymes simultaneously using a cocktail approach. This pooled assay employs a mixture of substrates specific to different CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 & CYP3A4) combined with a pooled enzyme source, such as human liver microsomes. The cocktail method offers several advantages over individual isoform testing, including: Reduced material consumption - Single test compound aliquot tests multiple CYP enzymes Higher throughput screening - Multiple CYP interactions assessed simultaneously Early drug development efficiency - Rapid identification of potential drug-drug interaction liabilities

Openalex Percentile: Top 74%
Pharmacogenetics and Drug Metabolism
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