Reactive Drug Metabolites / Methods and Principles in Medicinal Chemistry Bd.55 (PDF)

Origin and Historical Perspective on Reactive Metabolites Role of Reactive Metabolites in Genotoxicity Bioactivation and Inactivation of Cytochrome P450 and Other Drug Metabolizing Enzymes Role of Reactive Metabolites in Drug-Induced Toxicity - The Tale of Acetaminophen, Halothane, Hydralazine and Tienilic Acid Pathways of Reactive Metabolite Formation with Toxicophores/Structural Alerts Intrinsically Electrophilic Compounds as a Liability in Drug Discovery Role of Reactive Metabolites in Pharmacologic Action Retrospective Analysis of Structure-Toxicity Relationships of Drugs Bioactivation and Natural Products Experimental Approaches to Reactive Metabolite Detection Case Studies on Eliminating/Reducing Reactive Metabolite Formation in Drug Discovery Structural Alert and Reactive Metabolite Analysis for the Top 200 Drugs in the United States Market by Prescription Mitigating Toxicity Risks with Affinity Labeling Drug Candidates Dealing with Reactive Metabolite Positive compounds in Drug Discovery Managing IADRs - a Risk-Benefit Analysis

Amit Kalgutkar received his PhD in Organic Chemistry from Virginia Polytechnic Institute (USA) and conducted a post-doctoral fellowship at the Department of Biochemistry, Vanderbilt University School of Medicine. He joined Pfi zer in 1999, where he is currently a Research Fellow in the Drug Metabolism Group (Groton Laboratories). In addition, Dr. Kalgutkar is an adjunct Professor in the Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island.

Deepak Dalvie received his PhD in Medicinal Chemistry from State University at New York, Buffalo (USA) and was a post-doctoral fellow at the Department of Chemistry in University of Virginia and Virginia Polytechnic Institute (USA). He joined Pfi zer in 1992, where he is currently a Research Fellow in the Pharmacokinetics, Dynamics and Metabolism Department at Pfi zer's La Jolla site. In addition, Dr. Dalvie is an Associate Editor for Drug Metabolism and Disposition and on the editorial board of Xenobiotica.

Scott Obach received his PhD in biochemistry from Brandeis University and was a post-doctoral fellow at the New York State Department of Health Research Labs. He joined Pfi zer in 1992, where he is currently a Senior Research Fellow in the Pharmacokinetics, Dynamics, and Drug Metabolism Department at Pfizer in Groton (USA). In addition Dr. Obach is on the editorial boards of Drug Metabolism and Disposition, Chemical Research in Toxicology, Xenobiotica, and Drug Metabolism and Pharmacokinetics.

Dennis Smith worked in the pharmaceutical industry for more than 30 years since gaining his PhD from the University of Manchester (UK). For 20 years he was at Pfi zer Global Research and Development, Sandwich, where he was Vice President-Pharmacokinetics, Dynamics and Metabolism. During this time he has helped in the Discovery and Development of eight marketed NCEs. Now retired, he is still active in
an academic (Visiting Professor, University of Liverpool; Honary Professor, University of Capetown)

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