Chemical Toxicology: A Chemist’s Roadmap to Reduce Bioactivation Liabilities in Drug Candidates
| Type | Course |
|---|---|
| Language | English |
| Date |
August 15, 2009 from 08:30 am to 05:00 pm |
| Venue |
Four Points By Sheraton 1201 K Street NW Washington, DC 20005 US |
| Chemistry Specialties |
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| Chemistry Techniques |
|
| Contact |
American Chemical Society 1155 Sixteenth Street, NW Washington, DC 20036 US (800) 227-5558 shortcourses@acs.org |
| Add event to calendar |
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Increase your overall knowledge of mechanisms of drug metabolism mediated toxicity.
How You'll Benefit from this Course
* 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.
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.
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.
Speakers
* Kaushik Mitra, Department of Drug Metabolism, Merck Research Laboratories
* Griff Humphreys, Department of Biotransformation, Bristol-Myers Squibb
* Fred Guengerich, Harry Pearson Broquist Professor of Biochemistry, Vanderbilt University School of Medicine
* Christine Fandozzi, Merck
Session titles
* 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
