: Ronald T. Borchardt, Edward H. Kerns, Michael J. Hageman, Dhiren R. Thakker, James L. Stevens
: Ronald Borchardt, Edward Kerns, Michael Hageman, Dhrien Thakker, James Stevens
: Optimizing the 'Drug-Like' Properties of Leads in Drug Discovery
: Springer-Verlag
: 9780387449616
: 1
: CHF 189.50
:
: Pharmazie
: English
: 512
: Wasserzeichen/DRM
: PC/MAC/eReader/Tablet
: PDF

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.
Preface6
Contents9
Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds11
Role of Mechanistic Transport Studies in Lead Optimization35
Metabolic Activation-Role inToxicity and Idiosyncratic Reactions59
Case History Use of ADME Studies for Optimization of Drug Candidates91
Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization109
Lipid-based Systems, Drug Exposure and Lead Optimization141
Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure161
Application of Physicochemical Data to Support Lead Optimization by Discovery Teams177
Computational Models Supporting Lead Optimization in Drug Discovery205
Prodrug Strategies for Improving Drug-Like Properties231
The Application of Multivariate Data Analysis to Compound Property Optimization253
Case History:Toxicology Biomarker Development Using Toxicogenomics265
Predicting Idiosyncratic Drug Reactions281
Elementary Predictive Toxicology for Advanced Applications311
The Application of PK/PD Modeling and Simulations During Lead Optimization333
Early Preclinical Evaluation of Brain Exposure in Support of Hit Identification and Lead Optimization365
Optimizing Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Development421
The Relevance of Transportersin Determining Drug Disposition433
Index471