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The Role of Mass Spectrometry in Drug Discovery

presented by

Cornelis E.C.A. Hop
Merck Research Laboratories

December 08, 1999

The Scripps Research Institute, W.M. Keck Foundation Amphitheater


Background:

Dr. Hop received his B.Sc. and M.Sc. degrees from the University of Utrecht (The Netherlands). His doctoral research was concerned with the gas phase chemistry of ions and their neutral counterparts using magnetic sector mass spectrometers. The research was a collaborative effort between Prof. J.L. Holmes (University of Ottawa, Canada) and Dr. J.K. Terlouw (University of Utrecht). After post-doctoral studies with Prof. T.B. McMahon (University of Waterloo, Canada) developing MS/MS techniques on a FT-MS instrument, he went to Madison, Wisconsin to head up the campus-wide mass spectrometry laboratory. During his stay in Madison he wrote several successful NSF proposals for state-of-the-art equipment, including instruments capable of electrospray and MALDI. In 1996 he joined Merck (Rahway, New Jersey) as a Senior Research Fellow and supervises the bioanalytical facility of the Department of Drug Metabolism. The research in his group concerns quantitative pharmacokinetic studies as well as metabolite identification using LC-MS/MS. While at Merck, Dr. Hop has been responsible for increasing the throughput significantly by introducing new methodology, new instruments and an LIMS system. Dr. Hop is the author/co-author of 64 publications in refereed journals.

Abstract:

With the increased speed at which new drug entities are now synthesized and evaluated for pharmacological activity, a need has arisen to provide fundamental metabolism data at the early stages of drug discovery. Strategies are being developed to permit drug metabolism data to be an important part of early drug discovery. Many important properties of drugs related to drug metabolism can be the deciding factor in whether or not a compound is selected for clinical development. Some of these include the pharmacokinetic properties, identity of the (major) metabolites, presence of reactive metabolites, potential for drug-drug interaction, etc. Liquid chromatography combined with mass spectrometry has been recognized as the ultimate analytical method for routine (quantitative and qualitative) analysis of in vitro and in vivo samples due to its specificity and sensitivity. Several examples will be shown, which show the critical role of LC-MS in drug discovery and drug metabolism in particular.

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