Optimizing the "Drug-Like" Properties of Leads in Drug Discovery - Borchardt, Ronald; Kerns, Edward; Hageman, Michael; Thakker, Dhrien; Stevens, James; SpringerLink (Online service) (New York, NY : Springer New York : Imprint: Springer, 2006)
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.
Keywords: Pharmacology; Pharmacology/Toxicology.