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El. knyga: Evaluation of Drug Candidates for Preclinical Development: Pharmacokinetics, Metabolism, Pharmaceutics, and Toxicology

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Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation

It is believed that selecting the "right" drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development.

Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical—pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment—this unique resource encourages integrated thinking in drug discovery. The contributors to this volume:





Cover drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, stability, drug formulation, preclinical safety assessment, toxicology, and toxicokinetics



Address developability issues that challenge pharma companies, moving beyond isolated experimental results



Reveal connections between the key scientific areas that are critical for successful drug discovery and development



Inspire forward-thinking strategies and decision-making processes in preclinical evaluation to maximize the potential of drug candidates to progress through development efficiently and meet the increasing demands of the marketplace





Evaluation of Drug Candidates for Preclinical Development serves as an introductory reference for those new to the pharmaceutical industry and drug discovery in particular. It is especially well suited for scientists and management teams in small- to mid-sized pharmaceutical companies, as well as academic researchers and graduate students concerned with the practical aspects related to the evaluation of drug developability.

Recenzijos

"This is a useful reference source for those new to, or aspiring to join the pharmaceutical industry, for academics, and for students of pharmacy and pharmaceutical sciences." (Chromatographia, 1 December 2010)

"In conclusion, the book brings the areas of ADME, toxicology and pharmaceutical science together to describe the approaches used to select safe compounds with the required pharmacokinetic and physiochemical properties for progressing into clinical development". (British Toxicology Society, Winter 2010)

Preface vii
Contributors ix
Introduction
1(10)
Charles B. Davis
Pharmacokinetics in Preclinical Drug Development: An Overview
11(28)
Dion Brocks
The Role of Membrane Transporters In Durg Disposition
39(16)
Fanfan Zhou
Peng Duan
Guofeng You
Cytochrome P450: Structure, Function, and Application in Drug Discovery and Development
55(54)
Ramesh B. Bambal
Stephen E. Clarke
The Role of Drug Metabolism and Metabolite Identification in Drug Discovery
109(26)
Xiangming Guan
Protein Binding in Drug Discovery And Development
135(34)
Vikram Ramanathan
Nimish Vachharajani
Prediction of The Pharmacokinetics in Humans
169(18)
Chao Han
Ramesh Bambal
Pharmaceutics Developability Assessment
187(34)
Lian Huang
Jinquan Dong
Shyam Karki
Safety Assessment in Drug Discovery
221(32)
Vito G. Sasseville
William R. Foster
Bruce D. Car
Assessment of Strategies Utilized to Minimize The Potential For Induction of Acquired Long Qt Syndrome And Torsade De Pointes
253(28)
Khuram W. Chaudhary
Barry S. Brown
Index 281
Chao Han, PHD, is Associate Director of Pharmacokinetics, Modeling and Simulation, Clinical Pharmacology Sciences, Centocor R&D. 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 Want, 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).
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