Sino-American Pharmaceutical Professionals Association-New England (sapa-ne)
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- The Role of ADME/PK in Drug Discovery
AbstractA common characteristic of most biochemical processes is a high degree of specificity. For example, most enzymes and receptors will only bind compounds with very specific characteristics. However, some biochemical processes have evolved to be versatile. For example, drug-metabolizing enzymes can bind and metabolize a wide variety of substrates. In general, most processes involved in ADME (absorption, distribution, metabolism, and elimination) tend to be nonselective. Consequently, modeling these processes requires unique approaches. Camitro is developing an integrated platform of computational models for the prediction of ADME/Tox properties of pharmaceutical drug candidates. Our models permit the high-throughput analysis of virtual compounds or libraries before synthesis at very early stages in the drug discovery process, thereby reducing the need for and complementing the interpretation of iterative compound synthesis and experimentation cycles. An overview of our modeling efforts will be provided, focusing on models for the cytochrome P450 enzymes. BiographyKen Korzekwa is Vice President of Research at Camitro Corporation. He joined Camitro from the University of Pittsburgh, where he was Associate Professor of Medicine in the Center for Clinical Pharmacology and Director of the Center’s Drug Discovery Program from 1995-1999. His research activities at Pittsburgh focused on four major areas: enzyme kinetics of drug metabolism, in vitro-iv vivo correlations in drug metabolism, predictive models for toxicological risk assessment, and steroid metabolism. While at Pittsburgh he also provided consulting on multiple occasions to pharmacokinetics/drug metabolism groups at major pharmaceutical companies. Prior to joining the University of Pittsburgh, he spent three years as a Staff Fellow and PRAT Fellow in the Laboratory of Chemical Pharmacology, NHLBI, NIH, under Dr. James Gillette, and five years as a Senior Staff Fellow in the Laboratory of Molecular Carcinogenesis, National Cancer Institute, NIH. Dr. Korzekwa has been actively involved in theoretical and experimental studies of P450 metabolism for more than 10 years. He has published extensively on the enzymology and mechanism of cytochrome P450 mediated human drug metabolism and toxicity. He was the recipient of the Best Paper Award in 1990 in Drug Metabolism and Disposition awarded by the Drug Metabolism Division of the American Society for Pharmacology and Experimental Therapeutics. Dr. Korzekwa serves on the Editorial Review Board for the journals Chemical Research and Toxicology and Journal of Biochemical Toxicology. He received his Ph.D. in Medicinal Chemistry from the University of Washington and his undergraduate degree in Chemical Engineering from the University of New Mexico. Regulation of Drug-Metabolizing Enzymes by Nuclear Receptor Activation: Serious Considerations in Drug Development B  ingfang Yan, D.V.M., Ph.D. Associate Professor
Department of Biomedical Sciences University of Rhode Island 41 Lower College Road Kingston, RI 02881 Tel: (401) 874-5032 Fax: (401) 874-5048Email: byan@uri.edu AbstractCytochrome P450 (CYP) enzymes rank first among the phase I biotransformation enzymes in terms of catalytic versatility and the number of xenobiotics they metabolize. Therefore, CYP enzymes determine the intensity and duration of action of drugs and play key roles in the detoxication and bioactivation of xenobiotics. Many therapeutical agents are shown to increase the expression of CYP enzymes, thus cause serious drug-drug interactions. The Food and Drug Administration requests all new drugs be tested for CYP induction, and pharmaceutical industries are very interested in establishing CYP induction profiles of drug candidates early so that appropriate decisions can be made for further development. Studies of molecular signaling have demonstrated that CYP induction is primarily achieved by receptor-mediated transactivation. These receptors include the aryl hydrocarbon receptor, the constitutive androstane receptor, the pregnane X receptor and the peroxisome proliferator-activated receptor-. In this presentation, the mechanisms of action of these receptors will be discussed, and receptor-based screening procedures will be described.Biography Bingfang Yan is an associate professor of Biomedical Sciences at the University of Rhode Island. He received D.V.M. degree in 1982 from Huazhong Agricultural University and Ph.D. degree in 1994 from the University of Kansas Medical Center. His research interest is in drug-metabolizing enzymes in general, cytochrome P450 systems and carboxylesterases in particular. His lab uses cellular and molecular techniques and animal models to study catalysis, prodrug activation and xenobiotic-regulation mediated by nuclear receptors. Currently he is the principal investigator for two major projects supported by the National Institutes of Health. The Role of ADME/PK in Drug DiscoveryKelvin W. Chan, Ph.D. Head, eADME Drug Metabolism & Pharmacokinetics Aventis Pharmaceuticals, Inc. Route 202-206 P.O. Box 6800
Bridgewater, NJ 08807-0800Tel: (908) 231-3878 Fax: (908) 231-2594 Email: kelvin.chan@aventis.com
Chris H. Senanayake, Ph. D. Senior Director of Chemical Process Research, Sepracor Inc. 111 Locke Drive Marlborough, MA 01752-7231 Phone: 508-357-7459 Fax: 508-357-7408 Email: csenanay@sepracor.com Directory: conference conference -> Tilte : a critical examination of the police relations with bbc conference -> Eavesdropping on a virtuous circle Richard Whately and the Oriel Noetics. Elena Pasquini Douglas uwa business School conference -> Simulation and Prediction of Storm Surges, Waves, and Morphological Changes due to Tropical Cyclones by Using a pc-based Integrated Coastal Process Model conference -> Panel 0511 Disability and Difference I: Post-War Journeys through Disability conference -> Do remittances have a flip side? A general equilibrium analysis of remittances, labor supply responses and policy options for Jamaica* Maurizio Bussolo and Denis Medvedev conference -> Conference approval process made easy for acm in cooperation conferences conference -> Proceedings of gt2009 asme turbo Expo 2009: Power for Land, Sea and Air Orlando, Florida, USA gt2009-59981 dynamics of premixed h2/CH4 flames under near blowoff conditions conference -> South Korea’s Economic Future: Industrial Policy, or Economic Democracy? conference -> Asset rotator Cuff Rehabilitation Course Faculty Dr. Spero Karas conference -> Acm word Template for sig site Download 122.5 Kb. Share with your friends:
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