edited by Ronald T. Borchardt
Optimizing the "Drug-Like" Properties of Leads in Drug Discovery is focused on the optimization of the drug-like properties of leads in drug discovery.
If the strategies and the methodologies presented in Optimizing the "Drug-Like" Properties of Leads in Drug Discovery were to be adopted by pharmaceutical and biotechnology companies, it is the belief of the workshop’s organizers that more higher quality drug candidates would be advancing into preclinical and clinical development resulting in more efficacious and safer drugs.
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 Optimizing
- 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 Physiochemical 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
CD-ROM included
Index