Simultaneous Quantitative and Qualitative Measurements in Drug-Metabolism Investigations

Simultaneous quantitative and qualitative collection of information from a drug-metabolism and pharmacokinetics analysis can increase productivity in drug discovery and development. These two data sets are traditionally collected from two parallel sample lines, run at differing concentrations, and often on separate liquid chromatography–tandem mass spectrometry (LC–MS/MS) instruments because of LC–MS technology. Most current LC–MS/MS systems offering the high mass accuracy required for metabolite identification lack the sensitivity and linear range to perform quantitative bioanalysis at therapeutic dosing levels.

This article presents the successful analysis of metabolic products from microsomal incubations of a common pharmaceutical compound. Using quadrupole time-of-flight mass spectrometry, the author obtained clearance data, metabolic identification, structural elucidation, and metabolic profiles from a single sample set.

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