Year: 2025
Type: preprint
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
Author: Nick Lynch
Language: English
Subfield: Pharmacology
Domain: Life Sciences
Open Access status: gold
OpenAlex ID: W4412869321