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Optimizing the "Drug-Like" Properties of Leads in Drug Discovery

Title
Optimizing the "Drug-Like" Properties of Leads in Drug Discovery [electronic resource] / edited by Ronald Borchardt, Edward Kerns, Michael Hageman, Dhrien Thakker, James Stevens.
ISBN
9780387449616
Edition
1st ed. 2006.
Publication
New York, NY : Springer New York : Imprint: Springer, 2006.
Physical Description
1 online resource (X, 512 p.) 190 illus., 39 illus. in color.
Local Notes
Access is available to the Yale community.
Access and use
Access restricted by licensing agreement.
Summary
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.
Variant and related titles
Springer ENIN.
Other formats
Printed edition:
Printed edition:
Printed edition:
Format
Books / Online
Language
English
Added to Catalog
September 20, 2019
Series
Biotechnology (Arlington, Va.) ; IV.
Biotechnology: Pharmaceutical Aspects ; IV
Contents
Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds
Role of Mechanistic Transport Studies in Lead Optimization
Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions
Case History — Use of ADME Studies for Optimization of Drug Candidates
Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization
Lipid-based Systems, Drug Exposure and Lead Optimization
Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure
Application of Physicochemical Data to Support Lead Optimization by Discovery Teams
Computational Models Supporting Lead Optimization in Drug Discovery
Prodrug Strategies for Improving Drug-Like Properties
The Application of Multivariate Data Analysis to Compound Property Optimization
Case History: Toxicology Biomarker Development Using Toxicogenomics
Predicting Idiosyncratic Drug Reactions
Elementary Predictive Toxicology for Advanced Applications
The Application of PK/PD Modeling and Simulations During Lead Optimization
Early Preclinical Evaluation of Brain Exposure in Support of Hit Identification and Lead Optimization
Optimizing Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Development
The Relevance of Transporters in Determining Drug Disposition.
Subjects
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