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Updated: Jul 14, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
In vitro approaches to investigate mechanism-based inactivation of CYP enzymes
Thomas M Polasek1, John O Miners
1Flinders University and Flinders Medical Centre, Department of Clinical Pharmacology, Bedford Park, 5042, Adelaide, Australia. tom.polasek@flinders.edu.au
Abstract:
Mechanism-based inactivation (MBI) of human drug-metabolising CYP enzymes is an important consideration in the preclinical ADME evaluation of new drug candidates. In this report, the in vitro approaches used to investigate MBI of CYP enzymes are described, with an emphasis on the characterisation required to assess potential drug-drug interactions. Recent disparities in MBI data between in vitro test systems are also reviewed, highlighting the limitations of Escherichia coli-expressed human recombinant CYP in the prediction of drug-drug interactions that arise via MBI.
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