Overview
- Editors:
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Zhengyin Yan
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Johnson & Johnson Pharmaceutical Research & Development, Spring House
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Gary W. Caldwell
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Johnson & Johnson Pharmaceutical Research & Development, Spring House
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Table of contents (25 protocols)
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- Ming Hu, Jie Ling, Huimin Lin, Jun Chen
Pages 19-35
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- Jeffrey A. Ruell, Alex Avdeef
Pages 37-64
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- Eun Ju Jeong, Yan Liu, Huimin Lin, Ming Hu
Pages 65-76
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- Seong-Hee Park, Sung-Hack Lee, Yaming Su, Patrick J. Sinko
Pages 77-87
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- S. Orlowski, J. Nugier, Eric Ezan
Pages 89-102
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- Yaming Su, Patrick J. Sinko
Pages 103-110
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- Gary W. Caldwell, Zhengyin Yan
Pages 123-149
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- David C. Ackley, Kevin T. Rockich, Timothy R. Baker
Pages 151-162
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- Wu-Nan Wu, Linda A. McKown
Pages 163-184
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- Daniel R. Mudra, Andrew Parkinson
Pages 203-214
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- Zhengyin Yan, Gary W. Caldwell
Pages 231-244
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- Amin A. Nomeir, Jairam R. Palamanda, Leonard Favreau
Pages 245-262
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- Naomi Suzuki, Padmaja M. Prabhu, Shinya Shibutani
Pages 263-278
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- Bojana Žegura, Metka Filipič
Pages 301-313
About this book
Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addition to potency, which include optimal physicochemical properties, reasonable ph- macokinetic parameters, and good safety profiles. Therefore, research tools must be available in drug discovery to rapidly screen for compounds with favorable drug-like properties, and thus adequate resources can be directed to projects with high potential. Optimization in Drug Discovery: In Vitro Methods is a compilation of detailed experimental protocols necessary for setting up a variety of assays important in compound evaluation. A total of 25 chapters, contributed by many experts in their research areas, cover a wide spectrum of subjects including physicochemical properties, abso- tion, plasma binding, metabolism, drug interactions, and toxicity. A good pharmacokinetic profile has long been recognized as an imp- tant drug-like characteristic. Pharmacokinetic parameters are affected by many properties of drug molecules such as physicochemical nature, abso- tion, metabolic stability, and so on.
Reviews
"This book covers most of the currently used techniques in lead optimization with respect to ADME and safety profiles. . .would be very useful addition to the library of any drug scientist interested in an introduction to these important methods. Each chapter treats its topic in a concise manner and provides ample references to lead the reader to more detailed information."-Doody's Health Sciences Book Review Journal
"...very useful technically...invaluable to those changing roles or joining a pharmaceutical company, it is also very helpful for scientists in the biotech industry who are new to drug discovery." - Immunology News
"The book provides a wealth of relevant information...the tome is neatly designed, well constructed and easy to read." - ISSX Newsletter
"...a useful reference handbook for in vitro ADMET assays." - ChemBioChem
