Technologies and strategies to characterize and quantitate metabolites in drug discovery and development

ABSTRACT Pharmacokinetics and toxicokinetics studies rely on the quantitation of drugs and its metabolites. Drug metabolism studies are based on the characterization of the structure of drugs and their metabolites. Liquid chromatography coupled with mass spectrometry is an undisputed technology for the routine analysis of drugs and metabolites in the drug discovery set‐up. Advancements in liquid chromatography and mass spectrometry have accelerated and improved drug discovery and development. Identification and quantitation of drugs and metabolites have gained importance because of their relevance to clinical research. In the present review, we present a bird's eye view of qualitative and quantitative analysis of drugs and their metabolites. Various technologies available to characterize and quantitate metabolites are analyzed. Characterization of metabolites of the sulfonyl urea drug glyburide and the kinetics of glyburide metabolism are discussed in detail. Copyright © 2014 John Wiley & Sons, Ltd.