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The importance of metabolite identification in discovery DMPK

This webinar will show the importance of metabolite identification studies in discovery DMPK and how medicinal chemists use it to improve drug design.

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Agenda

• How metabolism impacts DMPK properties?
  • General overview of metabolism and how it impacts discovery
• How do we determine the structures of metabolites in discovery?
  • How do we determine metabolite structures from in vitro and in vivo matrices in discovery projects
• How do we use metabolite identification data to mitigate metabolism issues in design?
  • General principles of using metabolism identification to mitigate DMPK issues in design built around case studies from the drug discovery group and examples from the literature

Moderated by: Ray Cooke, Ph.D., MBA – Principal Scientist, Metabolism at Pharmaron

Speakers

Gordon Dear, Ph.D. – Global Director, Disposition & Biotransformation at GSK

Gordon is currently Global Director of Disposition and Biotransformation within DMPK at GlaxoSmithKline, and has 30 years experience in the Pharma industry, progressing through roles of increasing responsibility covering areas including biotransformation, drug disposition, metabolite identification, investigative toxicology, together with the broad application of bioanalytical sciences. His educational background includes a PhD in the field of Drug Metabolism and Spectroscopy (Imperial College, London), with a focus on the application of LC/MS and NMR techniques to drug metabolite identification. He has authored or co-authored >70 peer reviewed articles, reviews, abstracts, application notes and book chapters. Gordon has been an external instructor and coach in the DMPK community for approximately 20 years, contributing as a course tutor and organizer to a DMDG affiliated course on drug metabolism and bioanalytical methods, accredited by the Royal Society of Biology and is currently representing GSK as part of the IQ Translational and ADME Sciences Leadership Group (TALG).

Guoquing Shen, Ph.D. – Director, in vitro ADME at Pharmaron

Dr. Shen is Director in in vitro ADME department of Pharmaron with 12-year experience in drug discovery and development. Since he joined Pharmaron in 2011, he has made significant contributions in building up the in vitro ADME platforms, especially for drug metabolism and metabolite identification. Dr. Shen has comprehensive knowledge of in vitro and in vivo ADME/PK technologies and mass spec instruments. His experiences cover from the early stage of drug discovery to late-stage regulatory DMPK and bioanalysis studies. His responsibility now includes reactive metabolite screening, metabolite identification and LC-MS bioanalysis for both small molecules and biologics. Dr. Shen holds a Ph.D. degree in Pharmaceutical Analysis from Peking Union Medical College studying metabolomics and drug metabolism.

Tammy Ladduwahetty, Ph.D. – Director, Medicinal Chemistry at Pharmaron

Dr. Ladduwahetty joined Pharmaron in 2019. She brings over 30 years of experience in medicinal chemistry from her work in pharma, biotech and CRO sectors. As a Senior Research Fellow at Merck Sharp and Dohme in the UK, where she spent over 18 years, Tammy led teams working in a number of programs in CNS disease, and was a key contributor to the NK1 antagonist Emendâ. Tammy spent 10 years at Charles River Laboratories in the UK leading teams involved in drug discovery, library design and PROTACs working on Huntington’s disease, Malaria and antibacterials. At Cellzome, she worked in the immunology area. Tammy is the co-author of over 65 patents and peer-reviewed publications.

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