Course Catalog

Chemical Toxicology: A Chemist's Roadmap to Reduce Bioactivation Liabilities in Drug Candidates

Increase your overall knowledge of mechanisms of drug metabolism mediated toxicity.

Course Details

Key Topics

  • Mechanisms of bioactivation
  • Enzyme systems involved in bioactivation
  • Methods for screening for reactive metabolite formation
  • Case studies of structural optimization to reduce the risk of metabolism-mediated toxicity
  • Mechanisms leading to metabolism-mediated genotoxicity
  • Covalent binding & relevance to toxicity
  • In vivo models to study reactive intermediate generation

Information

Increase your overall knowledge of mechanisms of drug metabolism mediated toxicity.

Who Should Attend

Medicinal chemists, drug metabolism scientists and other scientists interested in learning more about the background of mechanistic drug metabolism mediated toxicology and how to apply these learnings to drug discovery and development.

Benefits

  • Understand and gain confidence in the field of metabolism-mediated toxicology
  • Be able to better recognize structures with the potential for bioactivation
  • See how others have utilized reactive metabolite data and redesigned molecules to avoid the liability of bioactivation
  • Become familiar with existing and new in vitro and in vivo techniques for identifying risks of chemically mediated toxicology

Agenda

  • Introduction to drug metabolism and mechanisms of bioactivation
  • Overview of the enzymes important in bioactivation, important species and inter-subject differences in enzyme expression
  • Methods for investigation of reactive metabolites as part of drug discovery programs; case studies of optimization of molecular structure to reduce risk of toxicity
  • Mechanisms leading to metabolism-mediated genotoxicity
  • Strategies useful for evaluation of reactive intermediates as part of a candidate optimization program
  • Covalent binding & relevance to toxicity; kinase signaling & relevance to toxicity/apoptosis/adaption
  • In vivo models to study reactive intermediate generation

Course Locations

Date

TBA

Check-in opens at 7:30 a.m. on the first day of the course.

Course runs from 8:30 a.m. to 5:00 p.m. each day.

Register Online Register Via Mail

Venue


Pricing
  Member Non-Member
Advanced $795 $995
Standard $1,095 $1,295

The course fee includes a course binder and a continental breakfast each day.

Five for Four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. Note: This discount is only available if you register by fax or mail and mention this discount. May not be combined with any other offer.

About the Instructors

  • Kaushik Mitra

    works for the Department of Drug Metabolism, Merck Research Laboratories.

  • Griff Humphreys

    works for the Department of Biotransformation, Bristol-Myers Squibb.

  • Fred Guengerich

    is the Harry Pearson Broquist Professor of Biochemistry, Vanderbilt University School of Medicine.