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Biomedical Sciences - Pharmacology & Toxicology | Optimizing the "Drug-Like" Properties of Leads in Drug Discovery

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

Borchardt, R., Kerns, E., Hageman, M., Thakker, D., Stevens, J. (Eds.)

2006, X, 512 p. 190 illus., 39 illus. in color.

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Recognizing changes in the paradigm by which drugs are discovered, the American Association of Pharmaceutical Scientists (AAPS) has recently organized and sponsored two focused workshops in the area of profiling drug-like properties during drug discovery. The most recent of these, entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery" took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery.

This book arises from the workshop. The book outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process. The emphasis is on advancing higher quality drug candidates into preclinical and clinical development, resulting in more efficacious and safer drugs.

The organizers of this workshop believe that if the strategies and methodologies presented here were to be adopted by pharmaceutical and biotechnology companies, more higher-quality drug candidates would advance into preclinical and clinical development ,resulting in more efficacious and safer drugs.

Content Level » Professional/practitioner

Keywords » Borchardt - Discovery - Drug - Leads - Like - Optimizing - Properties - lead

Related subjects » Pharmacology & Toxicology

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 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.

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