SLAS2015 Short Courses
Pharmacokinetics and Pharmacodynamics in Drug Discovery
This course is designed to equip biologists and chemists with an understanding of the principles of pharmacology as applied to the drug discovery process. Specifically, the two days will center on Pharmacokinetics (day 1) and Pharmacodynamics (day 2). This can be considered as being loosely based on the dose-response relationship as knowledge of both of these variables are needed in the assessment of therapeutic value.
Who Should Attend
- Pharmacologists and biologists involved in drug discovery
- Medicinal chemists
- All Scientists involved in the drug discovery process
How You Will Benefit From This Course:
- Participants will gain a knowledge of the general concepts of Pharmacokinetics and Safety Pharmacology
- Students will understand the scientific basis for true drug-like activity
- Students will be familiarized with and understand early stage in vitro assays aimed at determining pharmacokinetic properties of molecules and possible pharmacologic safety issues
- Students will learn optimal strategies for choice of drug candidates in discovery and development programs
- Absorption how much of the dose given enters the body?
- Distribution Once in the central compartment, where does the molecule go in the body?
- Clearance how long does the drug stay in the body?
- Repeat dosing what repeat dosing regimen does the PK support?
- The course will discuss these assays, how and why they are run, and the limitations and interpretation of the data that emerges from them.
- The course continues with discussion of drug response and addresses the major reason why drugs presently fail (50%), namely lack of efficacy.
- The premise is that improved understanding of the effects of drugs at their primary targets will assist in the identification of fruitful candidates.
- For instance, while target validation presently is used, pathway validation may enhance this process (biased signaling).
- As well as desired therapeutic molecular activity, the assessment of undesired effects leading to Pharmacologic safety issues also will be discussed (i.e. cytotoxicity, hepatotoxicity, mutagenicity, hERG and off-target effects).
- Reference material will be given (CD) for further study and application.
Terry Kenakin Ph.D.
University of North Carolina School of Medicine, Chapel Hill, NC
Beginning his career as a synthetic chemist, Terry Kenakin received a Ph.D. in Pharmacology at the Unversity of Alberta, Edmonton Canada. He joined Burrough-Wellcome as an associate Scientist and worked in drug discpovery at Glaxo Inc., GlaxoWellcome and finally GlaxoSmithKline Research and Development laboratories at Research Triangle Park, N.C. USA. Dr Kenakin currently is a professor of Pharmacology in the Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill NC. He is a member of numerous editorial boards as well as co-editor in Chief of the Journal of Receptors and Signal Transduction and Current Opinion in Pharmacology. He also has written numerous articles and 10 books on Pharmacology.