Introduction to Small Molecule Drug Metabolism and Applications to Discovery and Development


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Tuesday, January 12, 2021 | 1:00 PM 4:00 PM


Instructor:

John C. L. ErveJohn C. L. Erve, PhD, Jerve Scientific Consulting, Inc.


This seminar focuses on small molecule drug metabolism and will cover topics relevant to both discovery and development. Topics to be covered include assays to access metabolic clearance, chemistry strategies for modifying structures to overcome metabolic clearance, the role of metabolite identification in preclinical and clinical development and characterization of by mass spectrometry. Drugs that undergo bioactivation to reactive metabolites, structure-toxicity relationships and idiosyncratic toxicity will also be discussed.

Topics to be Covered:

  • Historical background on the field of drug metabolism
  • Basic drug biotransformation reactions and the enzymes responsible
  • Newly recognized drug biotransformation reactions
  • In vitro assays used to access metabolism-based clearance
  • Medicinal chemistry strategies for overcoming poor metabolic stability
  • Bioactivation pathways to reactive drug metabolites
  • Role of reactive metabolites in drug toxicity, including idiosyncratic toxicity
  • Role of metabolite identification studies in discovery and development
  • Four steps for identifying and characterizing drug metabolites by mass spectrometry

Who Should Attend

Scientists who have recently entered the pharmaceutical industry and are looking to gain an understanding of drug metabolism as well as scientists working in smaller biotech companies who need a stronger foundation in this topic. Graduate students or academics wishing to understand drug metabolism from a pharmaceutical industry perspective.

Instructor Biography:

John C. L. Erve, PhD, Jerve Scientific Consulting, Inc.
John Erve is from Chicago and studied Chemistry (BS, MS) at the University of Chicago and earned a PhD in Toxicology at Oregon State University. Following postdoctoral work at Vanderbilt (1995-1999) he joined BD-Biosciences (Woburn, MA) as a Study Director. In 2002, he joined AstraZeneca (Sweden) where he characterized reactive metabolites. In 2004 he joined Wyeth (Collegeville, PA) as a Principal Scientist responsible for metabolite identification. In 2010, John joined Novartis (Cambridge, MA) as a Lab Head in Analytical Sciences. John returned to drug metabolism at Elan Pharmaceuticals (San Francisco, CA) in 2012 and later formed Jerve Scientific Consulting, Inc to help small biotech companies in the Bay area with drug discovery efforts. John was a certified D.A.B.T. from 2004 to 2019.