Evaluation of Drug Candidates for Preclinical Development Pharmacokinetics, Metabolism, Pharmaceutics, and Toxicology

by Han, Chao; Davis, Charles B.; Wang, Binghe

• ISBN13: 9780470044919
• ISBN10: 0470044918
• Edition: 1st
• Format: Hardcover
• Copyright: 2010-01-19
• Publisher: Wiley

Summary

Explaining the assessment of potential drug compounds, this is an ideal introductory reference for those new to drug discovery. It includes sections on pharmacokinetics and drug metabolism, integration of pharmaceutical development, and predictive safety assessment. Topics include: cost analysis, drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, assessing stability, ways to optimize drug formulation, toxicology and toxicokinetics, and more. Readers will understand why absorption-distribution-metabolism-excretion-toxicology (ADMET) is key in drug development. This is an enlightening reference for scientists, medicinal chemists, and others working in drug discovery.

Author Biography

Chao Han, PhD, is Associate Director of Pharmacokinetics, Modeling and Simulation, Clinical Pharmacology Sciences, Centocor RD. He has been working in drug discovery and early development for more than ten years, published over thirty research articles in peer-reviewed journals, and written three book chapters. Charles B. Davis, PhD, heads Drug Metabolism and Pharmacokinetics for the Cancer Metabolism Drug Discovery Unit within Cancer Research at GlaxoSmithKline. He has more than twenty years experience in preclinical and clinical development and has served on the leadership teams of three of GSK's Centers of Excellence in Drug Discovery. Binghe Wang, PhD, is Professor and Georgia Research Alliance Eminent Scholar in Drug Discovery in the Department of Chemistry, Georgia State University and Georgia Cancer Coalition Distinguished Scientist. He also serves as editor in chief of Medicinal Research Reviews and is lead editor of Drug Delivery: Principles and Applications (Wiley).

Table of Contents

Preface	p. vii
Contributors	p. ix
Introduction	p. 1
Pharmacokinetics in Preclinical Drug Development: An Overview	p. 11
The Role of Membrane Transporters in Drug Disposition	p. 39
Cytochrome P450: Structure, Function, and Application in Drug Discovery and Development	p. 55
The Role of Drug Metabolism and Metabolite Identification in Drug Discovery	p. 109
Protein Binding in Drug Discovery and Development	p. 135
Prediction of the Pharmacokinetics in Humans	p. 169
Pharmaceutics Developability Assessment	p. 187
Safety Assessment in Drug Discovery	p. 221
Assessment Of Strategies Utilized to Minimize the Potential For Induction of Acquired Long QT Syndrome and Torsade De Pointes	p. 253
Index	p. 281
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