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Drug Stereochemistry. Analytical Methods and Pharmacology. Edition No. 3. Drugs and the Pharmaceutical Sciences
Informa Healthcare, April 2012, Pages: 332
This revised third edition has been updated to cover all aspects of chiral drugs from the academic, governmental industrial and clinical perspective reflecting the many advances in techniques and methodology. The title will cover new material including the use of enzymes for the synthesis and resolution of enantiomeric compounds as well, as their use in drug discovery; how stereochemistry impacts on decisions taken during the ADMET (absorption, distribution, metabolism, excretion, toxicity) stage of drug discovery; issues faced during the final stages of the drug development process; the impact of ICH (International Conference on Harmonisation) on the use of single isomer drugs; racemic switches; and legal perspectives looking at IP and patent issues surrounding chiral switches and marketing single enantiomer switches.
This Third Edition comprehensively presents all aspects of chiral drugs from scientific, academic, governmental, industrial, and clinical points of view. This one-stop text covers the lifespan of 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.
New 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
- A chapter on pharmacokinetics and pharmacodynamics that discusses the issues faced during the final stages of the drug development process
- The impact of International Conference on Harmonisation 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
- A chapter on the legal perspectives of patent issues surrounding chiral switches and the marketing of single enantiomer switches
- This will be a one-stop shop 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. Stereochemical Terms and Concepts: An Overview. Molecular Chiral Recognition: An Introduction and Overview. The Role of Stereo-Chemistry in the Development of ACE Inhibitors: Nature to Clinic. The Separation, Preparation and Identification of Stereochemically Pure Drugs: Indirect Methods for the Chromatographic Resolution of Drug Enantiomers: Synthesis and Separation of Diastereo-Metric Derivatives. The Direct Resolution of Enantiometric Drugs by Chiral Phase Gas Chromatography. HPLC Chiral Stationary Phases for the Stereochemical Resolution of Enantiometric Compounds: The Current State of the Art. Enantioselective Separations by Capillary Electrophoresis. Recent Advances in the Synthesis of Enantiomerically Pure Compounds. Production Scale Preparation of Enantiomerically Pure Compounds by Chromatography and Synthetic Approaches. Spectrometric Identification and Characterization of Chiral Molecules. Pharmacokinetic and Pharmacodynamic Differences Between Drug Stereoisomers: Stereochemical Considerations in the ADMET Stage of Drug Development. Stereoselective Biotransformations: Toxico-Logical Consequences and Implications. Stereoselective Interactions with Enzymes and Their Use in Drug Development. Stereoselective Transport of Drugs Across Epithelia. Clinical Pharmacokinetics and pharmacodynamics of Stereoisomeric Drugs. Industrial and Regulatory Perspectives on Single Isomer Drugs: Regulatory Perspective of the Development of New Stereoisomeric Drugs. Stereochemically Pure Drugs Versus Racemates: An Overview. The Development and Marketing of Single Isomer Drugs vs Racemates: A Legal Perspective.
Professor Krzysztof Józwiak is Head of Laboratory of Medicinal Chemistry and Neuroengineering of Medical University of Lublin, 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.