Optimizing the "Drug-Like" Properties of Leads in Drug Discovery
Editors: Borchardt, R., Kerns, E., Hageman, M., Thakker, D., Stevens, J. (Eds.)
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- About this book
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Drug discovery and development is a very complex, costly, and ti- consuming process. Because of the uncertainties associated with predicting the pharmacological effects and the toxicity characteristics of new chemical entities in man, their clinical development is quite prone to failure. In recent years, phar- ceutical companies have come under increasing pressure to introduce new blockbuster drugs into the marketplace more rapidly. Companies have responded to these pressures by introducing new technologies and new strategies to expedite drug discovery and development. Drug discovery and development have traditionally been divided into three separate processes (i. e. , discovery research, preclinical development, and clinical development) that ideally should be integrated both organizationally and functionally. Instead, separate and distinct discovery research, preclinical development, and clinical development divisions were created within many companies during the 1980s and 1990s, Because of their isolation, scientists in the discovery research divisions often were advancing drug candidates into preclinical development that had marginal drug-like properties. For the purpose of this presentation, “drug-like” properties refer to the molecule’s physicochemical, absorption-distribution-metabolism-excretion (ADME), and toxicological properties. Lacking optimal drug-like properties often caused these drug candidates to fail in preclinical or clinical development.
- Table of contents (18 chapters)
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Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds
Pages 1-23
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Role of Mechanistic Transport Studies in Lead Optimization
Pages 25-47
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Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions
Pages 49-80
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Case History — Use of ADME Studies for Optimization of Drug Candidates
Pages 81-97
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Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization
Pages 99-130
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Table of contents (18 chapters)
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Bibliographic Information
- Bibliographic Information
-
- Book Title
- Optimizing the "Drug-Like" Properties of Leads in Drug Discovery
- Editors
-
- Ronald Borchardt
- Edward Kerns
- Michael Hageman
- Dhrien Thakker
- James Stevens
- Series Title
- Biotechnology: Pharmaceutical Aspects
- Series Volume
- IV
- Copyright
- 2006
- Publisher
- Springer-Verlag New York
- Copyright Holder
- Springer-Verlag New York
- eBook ISBN
- 978-0-387-44961-6
- DOI
- 10.1007/978-0-387-44961-6
- Hardcover ISBN
- 978-0-387-34056-2
- Softcover ISBN
- 978-1-4939-5047-8
- Edition Number
- 1
- Number of Pages
- X, 512
- Topics
