Understanding CYP2D6 interactions
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Updated: Jun 21, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Marcel J de Groot1, Florian Wakenhut, Gavin Whitlock
1World Wide Medicinal Chemistry (WWMC), United Kingdom. marcel.degroot@pfizer.com
Abstract:
Owing to the polymorphic nature of CYP2D6, clinically significant issues can arise when drugs rely on that enzyme either for clearance, or metabolism to an active metabolite. Available screening methods to determine if the compound is likely to cause drug-drug interactions, or is likely to be a victim of inhibition of CYP2D6 by other compounds will be described. Computational models and examples will be given on strategies to design out the CYP2D6 liabilities for both heme-binding compounds and non-heme-binding compounds.
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