ABSTRACT

Drug metabolism and pharmacokinetics (DMPK)-related studies are among the most important phases of drug discovery and development and are increasingly involved in lead optimization. Recent advances in high-throughput screening, combinatorial chemistry, and genomics have significantly increased the numbers of samples requiring DMPK profiling. Hence, high-throughput pharmaceutical bioanalysis is necessary to support the increasing numbers of DMPK studies to expedite the drug discovery and development processes. High-throughput bioanalysis has been achieved by using a combination of high performance liquid chromatography and tandem mass spectrometry (LC/MS/MS).1-11 This technique revolutionized bioanalysis by dramatically increasing throughput for the quantitative determination of drugs and metabolites in biological matrices due to its inherent specificity and sensitivity.