Abstract: Mass spectrometry has been extensively utilized in drug discovery research and development, from the traditional medicinal chemistry support to drug metabolism and pharmacokinetic studies. As the industry faces with the challenges of tougher diseases and more challenging pathways/targets to tackle, it requires the development of innovative solutions to address needs from target discovery to biomarker identification. It also presents a great opportunity for scientists in the field for innovation, many of which often come from cross disciplinary efforts - chemistry, biology and technology. In this presentation, four areas of drug discovery research where innovative solutions have been developed will be presented: (1) target identification and validation through cellular metabolomic analysis and chemical proteomics; (2) hits discovery and validation using MS-based screening; (3) PK analysis of therapeutic monoclonal antibody;
(4) MS imaging for drug tissue distribution. Investment in life saving and life style improving medicines will get more intensified as standard of living improves. Drug discovery research will continue to require and present opportunity for such application driven innovations.