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

Hardcover | August 3, 2006

EditorRonald Borchardt, Ronald T. Borchardt, Edward H. Kerns

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This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.

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This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume ...

Format:HardcoverDimensions:522 pages, 10 × 7.01 × 0.04 inPublished:August 3, 2006Publisher:SpringerLanguage:English

The following ISBNs are associated with this title:

ISBN - 10:0387340564

ISBN - 13:9780387340562

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Table of 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 and Lead Optimization.- Biopharmaceutics Modeling and the Role of Dose Formulation on Oral Exposure.- Application of Physiochemical Data to Support Lead Optimization by Discovery.- 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.- Optimization Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Development.- The Relevance of Transporters in Determining Drug Disposition.