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Reactive Drug Metabolites (Hardcover): Amit S. Kalgutkar, Deepak Dalvie, Dennis A. Smith, R. Scott Obach Reactive Drug Metabolites (Hardcover)
Amit S. Kalgutkar, Deepak Dalvie, Dennis A. Smith, R. Scott Obach; Series edited by Raimund Mannhold, …
R3,224 R2,566 Discovery Miles 25 660 Save R658 (20%) Shipped within 7 - 12 working days

Closing a gap in the scientific 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 herbal constituents and IADRs. The next part covers current strategies and approaches to evaluate the reactive metabolite potential of new drug candidates, both by predictive and by bioanalytical methods. There then follows an in-depth analysis of the toxicological potential of the top 200 prescription drugs, illustrating the power and the limits of the toxicophore concept, backed by numerous case studies. Finally, a risk-benefit approach to managing the toxicity risk of reactive metabolite-prone drugs is presented. Since the authors carefully develop the knowledge needed, from fundamental considerations to current industry standards, no degree in pharmacology is required to read this book, making it perfect for medicinal chemists without in-depth pharmacology training.

Pharmacokinetics and Metabolism in Drug Design (Hardcover, 3rd Edition): Dennis A. Smith, Charlotte Allerton, Hugo Kubinyi, Han... Pharmacokinetics and Metabolism in Drug Design (Hardcover, 3rd Edition)
Dennis A. Smith, Charlotte Allerton, Hugo Kubinyi, Han Van De Waterbeemd, Han Walker, …
R2,592 R2,167 Discovery Miles 21 670 Save R425 (16%) Shipped within 7 - 12 working days

In this new edition of a bestseller, all the contents have been brought upto- date by addressing current standards and best practices in the assessment and prediction of ADMET properties. Although the previous chapter layout has been retained, substantial revisions have been made, with new topics such as pro-drugs, active metabolites and transporters covered in detail in a manner useful to the Drug Discovery scientist. The authors discuss the parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. Uniquely comprehensive, the book relates physicochemistry and chemical structure to pharmacokinetic properties and ultimately drug efficacy and safety. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects.

Metabolism, Pharmacokinetics and Toxicity of Functional Groups - Impact of Chemical Building Blocks on ADMET (Hardcover,... Metabolism, Pharmacokinetics and Toxicity of Functional Groups - Impact of Chemical Building Blocks on ADMET (Hardcover, Edition.)
Dennis A. Smith; Series edited by David E Thurston, David Fox; Contributions by Alexander A. Alex, Kevin Beaumont, …
R3,786 Discovery Miles 37 860 Shipped within 7 - 11 working days

Until now, the area of drug metabolism and pharmacokinetics has been lacking in texts written for the Medicinal Chemist. This outstanding book, aimed at postgraduate medicinal chemists and those working in industry, fills this gap in the literature. Written by medicinal chemists and ADMET scientists with a combined experience of around 300 years, this aid to discovering drugs addresses the absorption, distribution, metabolism, excretion and toxicity (ADMET) issues associated with drugs. The book starts by describing drug targets and their structural motifs before moving on to explain ADMET for the medicinal chemist. It is the functional groups which most profoundly influence the drug molecules of which they form a part. They characterise the pharmacology, are essential to the activity, and alter the ADMET characteristics of each drug. Their effects follow a pattern, thus allowing medicinal chemists to predict and overcome potential challenges. For this reason, the Editors have taken the unique approach of dividing the remainder of the book into chapters which each focus on a different functional group. They describe drugs containing the functional group under consideration, explain why the group is there, and outline its physicochemical properties before going on to detail the ADMET issues. Where possible, prodrugs and bioisosteres, which may give alternative ADMET outcomes, are described. The chapters cross refer where similar matters are covered but individual chapters can be used in a stand alone manner. The book ends with a discussion of future targets and chemistry needs.

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