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Pharmaceutical Applications of Liquid Chromatography Coupled with Mass Spectrometry (LC/MS)

Abstract High performance liquid chromatography (HPLC) coupled with mass spectrometry (MS) is an extremely powerful and indispensable methodology practiced in virtually every stage of pharmaceutical discovery and development processes, including biological target discovery, biological assay for high throughput screening, characterization of physicochemical properties of drug candidates, and drug metabolism and pharmacokinetics. With continued advances and innovations in the areas of column technologies, LC/MS interfaces, and instrumentation, the field of LC/MS is strengthening and expanding to new disciplines constantly. In this report, the recent developments in the LC/MS interface ionization techniques, such as ESI, APCI, APPI, and MALDI, and novel hardware and software of mass spectrometry devices, are compared and reviewed in the light of drug discovery and development effort. The diverse qualitative and quantitative applications of LC/MS in the pharmaceutical industry are reported in four key fields; synthetic organic chemistry, combinatorial library parallel synthesis, bioanalysis in support of ADME, and proteomics. Other analytical techniques used in conjunction with LC/MS to augment analytical information content are also discussed. As the use of LC/MS is exceedingly widespread and ever increasing, this paper primarily focuses on recent progresses reported in the literature with selected publications.