Drug Metabolism in Drug Design and Development Basic Concepts and Practice
Thomas M. Guenther, Department of Pharmacology, College of Medicine, University of Illinois at Chicago, 835 South Wolcott Avenue ...
Adrienne Tymiak,Bristol-Myers Squibb Co., P.O. Box 4000, Princeton, NJ 08543
[email protected]
Timothy S. Tracy, Departmen ...
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PART I BASIC CONCEPTS OF DRUG METABOLISM ...
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1 OVERVIEW: DRUG METABOLISM IN THE MODERN PHARMACEUTICAL INDUSTRY SCOTTJ. GROSSMAN 1.1 INTRODUCTION It is interesting to contras ...
of known metabolic effects (e.g., metabolic activation to toxic reactive metabolites), or incomplete integration of existing inf ...
1.3 BREADTH OF SCIENCE 1.3.1 Chemistry Biotransformation is fundamentally a chemical process. Likewise, the most frequently empl ...
through informed molecular design. Fortunately, their common under- standing of bioorganic chemistry also greatly facilitates th ...
The means by which enzyme systems are regulated are now being appreciated and studied in a mechanistic fashion. Tools available ...
Pharmacokinetic optimization can be greatly aided with further biotrans- formation information. A limited disposition study can ...
well-developed basis for anticipating structural features that may predispose a molecule to form reactive metabolites. Once disc ...
document, and evaluate in the risk/benefit decision-making process. Global regulatory bodies are charged with promulgating these ...
The cumulative cost of bringing a drug to market is staggering. Without some assurance that these costs will be recovered throug ...
information learned from the drug’s discovery and development is shared in the public domain. A carefully crafted patent protect ...
Grossman, SJ. Are most toxicities caused by reactive metabolites? In: Molecular Toxicology, Josephy PD, Mannervik AB, editors. N ...
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2 OXIDATIVE, REDUCTIVE, AND HYDROLYTIC METABOLISM OF DRUGS F. PETERGUENGERICH 2.1 INTRODUCTION Oxidation, reduction, and hydroly ...
Another issue is that the use of the terms Phase I, Phase II, and Phase III is discouraged, for a number of reasons (Josephy et ...
In modern pharmaceutical development, early screening is done with new candidate drugs for the nature of metabolites, identifica ...
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