Optimizing the Drug-Like Properties of Leads in Drug Discovery

ISBN-13: 9781493950478 / Angielski / Miękka / 2016 / 512 str.

Ronald Borchardt;Edward Kerns;Michael Hageman

Opis

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.

Spis treści

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.