3rd Edition
Drug Stereochemistry Analytical Methods and Pharmacology, Third Edition
Drug Stereochemistry: Analytical Methods and Pharmacology, Third Edition covers all aspects of chiral drugs from academic, governmental, industrial, and clinical perspectives, reflecting the many advances in techniques and methodology.
Topics include:
- The use of enzymes in the synthesis and resolution of enantiometrically pure compounds in drug discovery
- How stereochemistry impacts decisions made in the absorption, distribution, metabolism, excretion, and toxicity (ADMET) stages of drug discovery
- Pharmacokinetics and pharmacodynamics and the issues faced during the final stages of the drug development process
- The impact of the International Conference on Harmonisation (ICH) on the use of single isomer drugs
- Chiral switches
- The concept of molecular chiral recognition and how it affects the separation and behavior of stereochemically pure drugs
- Patent issues surrounding chiral switches and the marketing of single enantiomer switches
The book provides a solid background on stereochemistry, from its early history, including an overview of terms and concepts, to the current drug development process, legal and regulatory issues, and the new stereoisomeric drugs. It is a one-stop reference for pharmaceutical scientists and chemists working with chiral drug molecules.
INTRODUCTION
The early history of stereochemistry: From the discovery of molecular asymmetry and the first resolution of a racemate by Pasteur to the asymmetrical chiral carbon of van’t Hoff and Le Bel, Dennis E. Drayer
Stereochemistry—basic terms and concepts, Krzysztof Jo´z´wiak
Molecular basis of chiral recognition, Krzysztof Jo´z´wiak
PART II: THE SEPARATION, PREPARATION, AND IDENTIFICATION OF
STEREOCHEMICALLY PURE DRUGS
Separation and resolution of enantiomers and their dissociable diastereomers through direct crystallization, Harry G. Brittain
Indirect methods for the chromatographic resolution of drug enantiomers, Władysław Gołkiewicz and Beata Polak
HPLC chiral stationary phases for the stereochemical resolution of enantiomeric compounds: The current state of the art, W. John Lough
Preparative and production scale chromatography in enantiomer separations, Geoffrey B. Cox
Enantioselective separations by electromigration techniques, Michał J. Markuszewski
Alternative analytical techniques for determination or isolation of drug enantiomers, W. John Lough
PART III: PHARMACOKINETIC AND PHARMACODYNAMIC
DIFFERENCES BETWEEN DRUG STEREOISOMERS
Stereoselective transport of drugs, Prateek Bhatia and Ruin Moaddel
Enantioselective binding of drugs to plasma proteins, Thomas H. Kim
Clinical pharmacokinetics and pharmacodynamics of stereoisomeric drugs, Scott A. Van Wart and Donald E. Mager
PART IV: PERSPECTIVES ON THE DEVELOPMENT AND USE OF SINGLE
ISOMER DRUGS
Regulatory perspective on the development of new stereoisomeric drugs, Sarah K. Branch and Andrew J. Hutt
Molecular analysis of agonist stereoisomers at b2-adrenoceptors, Roland Seifert and Stefan Dove
Development of chiral drugs from a U.S. legal patentability perspective:Enantiomers and racemates, Svetlana M. Ivanova
The importance of chiral separations in single enantiomer patent cases, Charlotte Weekes
Index
Biography
Professor Krzysztof Jóźwiak is head of laboratory of medicinal chemistry and neuroengineering of Medical University of Lublin, Poland
Dr W John Lough is reader in pharmaceutical analysis in the Department of Pharmacy, Health and Well-Being at the University of Sunderland, UK
Irving W. Wainer, Ph.D. is senior investigator, in the Bioanalytical Chemistry and Drug Discovery Section, Laboratory for Clinical Investigation, National Institute of Aging/National Institutes of Health
