The past fifteen years have seen a revolution in the field of stereochemistry, with breakthrough analytical techniques in enantiomeric separation profoundly affecting drug development and use. This practical reference written by leading researchers focuses on the important roles chirality and stereoisomerism play in drug development efforts--presenting for the first time a comprehensive overview of this rapidly evolving area of pharmacological research. The book explores analytical, pharmacological, and regulatory topics in dealing with the theory and practice of stereochemistry in the pharmaceutical industry today. This exciting, broad-appeal treatment extends from the analytical viewpoint in enantiomeric separation to the regulatory issues involved in the "racemate-versus-enantiomer" debate. The authors include numerous examples and case studies, and integrate material from a wide range of studies, publications, and workshops. The introductory chapters outline the pharmacological effects of stereochemistry, cover stereochemistry in drug metabolism, and discuss problems inherent in the duality of enantiomers--chemically identical yet spatially different molecules. Contributions on the specific aspects of chirality and drug activity explore the toxicological effects of stereoselectivity, illustrate how an understanding of the stereochemical composition of certain drugs can help avoid problems, and offer tips on new clinical applications for existing drugs. A full chapter is devoted to research opportunities in the development of new chirally pure drugs. Other practical research topics range from the preparation of chirally pure compounds to the analytical determination of stereochemical composition, to applications of circular dichroism (CD) spectroscopy. Regulatory issues concerning the development and approval of stereoisomeric drugs are discussed in the final chapters. This section offers an international perspective as well as a historical review of the ongoing debate surrounding regulatory guidelines. Impact of Stereochemistry on Drug Development and Use is an essential reference for medicinal and analytical chemists, pharmacologists, drug metabolism and pharmacokinetic scientists, and personnel of regulatory agencies. It is also a useful text for graduate students in stereochemistry, and for anyone who wants to keep up with the swift pace of change in this dynamic field. Impact of Stereochemistry on Drug Development and Use is an essential reference for medicinal and analytical chemists, pharmacologists, drug metabolism and pharmacokinetic scientists, and personnel of regulatory agencies. It is also a useful text for graduate students in stereochemistry, and for anyone who wants to keep up with the swift pace of change in this dynamic field. IMPACT OF STEREOCHEMISTRY ON DRUG DEVELOPMENT AND USE Twenty-three expert contributions on the "stereochemical revolution" of the last fifteen years--covering analytical, pharmacological, and regulatory topics--show that "drug development can no longer occur without consideration of drug stereochemistry." "We have...come full circle and stand alongside Pasteur in amazement of nature's duality, symmetry and dissymmetry, and its chemical and pharmacological consequences."--from the Preface