Dennis A. Smith - Böcker

With a focus on case studies of R&D programs in a variety of disease areas, the book highlights fundamental productivity issues the pharmaceutical industry has been facing and explores potential ways of improving research effectiveness and efficiency. Takes a comprehensive and holistic approach to the problems and potential solutions to drug compound attritionTackles a problem that adds billions of dollars to drug development programs and health care costsGuides discovery and development scientists through R&D stages, teaching requirements and reasons why drugs can failDiscusses potential ways forward utilizing new approaches and opportunities to reduce attrition

A reference on drug metabolism and metabolite safety in the development phase, this book reviews the analytical techniques and experimental designs critical for metabolite studies. It features case studies of lessons learned and real world examples, along with regulatory perspectives from the US FDA and EMA.•    Reviews the analytical techniques and experimental designs critical for metabolite studies•    Covers methods including chirality, species differences, mass spectrometry, radiolabels, and in vitro / in vivo correlation•    Discusses target pharmacology, in vitro systems aligned to toxicity tests, and drug-drug interactions•    Includes perspectives from authors with firsthand involvement in industry and the study of drug metabolites, including viewpoints that have influenced regulatory guidelines

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.