About the Book
Understanding the biochemistry of drug metabolism is today one of the most critical aspects of new drug development to assure safe and efficacious medicines of the future. The present work provides an exemplary scientific basis for the biochemistry of drug metabolism upon which both experienced and newly initiated drug-metabolism scientists may depend. It documents the progresse and major advances in our understanding of drug metabolism in an encyclopedic, but very readable format. The figures in this volume represent a Powerpoint presentation to simulate a well-organized, comprehensive, and readily understandable series of slides as would be given in an oral presentation. the text provides the reader with the sound bites that the lectu4rers present to explicate the slides. But as an added bonus, the text contains all the thoroughly referenced citations to the discussion for further examination by the reader. I find the presentation technique to be delightful and expect that other readers will have the same experience.' - Leslie Z. Benet
The present volume features the principles of drug metabolism, followed by the enzymes and reactions of oxidation, reduction, and hydrolysis. A continuation is in preparation.
The first of the two volumes is divided into three parts. Part One begins by introducing xenobiotics in the broad context of physiological metabolism, and continues with an overview of the processes of drug disposition and metabolism. It then goes on to summarize the macroscopic and microscopic locations of drug metabolism in animals and humans. This is followed by an introduction to the all-important issue of the consequences of drug and xenobiotic metabolism, providing an initial overview of pharmacokinetic, pharmacological and toxicological consequences. The last chapter examines drug metabolism in the context of drug research, with a focus on medicinal chemistry.
The second part is a major component of the book, corresponding to the role of oxidoreductases as major agents of metabolism. Cytochromes P450 receive particular attention, namely their multiplicity, structure, catalytic mechanisms, and the various reactions they catalyze, while other oxidoreductases are also presented, such as flavin monooxygenases, monoamine oxidases and other amine oxidases, aldehyde oxidase and xanthine dehydrogenase, peroxidases, and dehydrogenases-reductases. Each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials.
Part Three begins with a survey of the classification, properties and catalytic mechanism of the innumerable hydrolases known or suspected to play a role in xenobiotic metabolism. The focus then shifts to a systematic presentation of the various substrate classes, namely carboxylic esters, amides and peptides, lactams and lactones, esters of inorganic acids, alkene and arene epoxides, and some miscellaneous hydrolyzable moieties.
With a foreword by Prof Leslie Z. Benet, the world's best and best-known biopharmaceutical scientist