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
Authors
- Nick Lynch (ORCID: https://orcid.org/0000-0002-8997-5298)
Publication Details
- Published
- 2025-05-25
- DOI
- https://doi.org/10.17504/protocols.io.81wgbkb1ygpk/v1
- Primary Topic
- Pharmacogenetics and Drug Metabolism
- Type
- article
- Field-Weighted Citation Impact
- 0.00