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Closing a gap in the scientifi c literature, this first comprehensive introduction to the topic is based on current best practice in one of the largest pharmaceutical companies worldwide. The first chapters trace the development of our understanding of drug metabolite toxicity, covering basic concepts and techniques in the process, while the second part details chemical toxicophores that are prone to reactive metabolite formation. This section also reviews the various drug-metabolizing enzymes that can participate in catalyzing reactive metabolite formation, including a discussion of the structure-toxicity relationships for drugs. Two chapters are dedicated to the currently hot topics of her...
Critical in the elimination of drugs and other xenobiotics from the body, cytochrome P450 has strong bearing on scientific assessments of genetic polymorphism in metabolism, possible drug-drug interactions, and bioavailability of candidate drugs. This text systematizes findings on P450 and similar enzymes - as well as parallel issues shaping the pharmaceutical industry - to promote the next generation of safer, more effective drugs.
Written by medicinal chemists and ADMET scientists with a combined experience of over 300 years this aid to discovering drugs provides detailed coverage on absorption, distribution, metabolism, excretion and toxicology issues associated with new drugs.
Medicinal chemistry is a complex science that lies at the very heart of drug discovery. Poor solubility, complex metabolism, tissue retention and slow elimination are just some of the properties of investigational compounds that present a challenge to the design and conduct of ADMET studies. Medicinal chemistry experience and knowledge relating to how a lead structure was modified to solve a specific problem is generally very challenging to retrieve. Presented in a visual and accessible style, this book provides rapid solutions to overcome the universal challenges to optimizing ADMET.
Drug-Drug Interactions in Pharmaceutical Development comprehensively reviews the relevant science, industrial practice, and regulatory agency positions on drug-drug interactions. It focuses on the evaluation of potential drug-drug interactions, allowing researchers to address risk factors before a drug is put to market. The book covers both clinical and nonclinical aspects for understanding drug-drug interactions as well as in vitro and in vivo studies for use in studying interactions at the drug discovery stage.
If you’re working on or studying the effects of drug metabolisms, then this reference is for you! Handbook of Metabolic Pathways of Xenobiotics is an essential new reference which presents the metabolic fate of xenobiotics in animals and plants, and shows the metabolic pathways in the environment. Presenting a comprehensive guide to understanding the metabolisms of xenobiotics, the Handbook of Metabolic Pathways of Xenobiotics spans five volumes: Volumes 1-2 are Review Articles and Volumes 3-5 are Compound Articles. Review Articles present detailed reviews on the techniques and methods used to establish in vitro and in vivo metabolic pathways. Compound Articles are carefully selected lists...
Practical Utility of Biomarkers in Drug Discovery and Development covers all aspects of biomarker research applied to drug discovery and development and contains state-of-the-art appraisals on the practical utility of genomic, biochemical, and protein biomarkers. Case histories and lessons from successful and unsuccessful applications of biomarkers are included along with key chapters on GLP validation, safety biomarkers and proteomics biomarkers. Regulatory agency perspectives and initiatives both in the US and internationally are also discussed.
Drug metabolism and transport are very important facets within the discipline of pharmaceutical sciences, with enzyme kinetic concepts utilized regularly in characterizing and modeling the disposition and elimination of drugs. Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications focuses on very practical aspects of applying kinetic principles to drug metabolizing enzymes and transporters. Divided into five convenient sections, topics include the fundamental principles of enzyme kinetics, the kinetics of oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for both drug metabolizing enzymes and transporters including novel systems biology...