Pharmacokinetic Profiling in Drug Research focuses on the profiling of ADME properties (absorption, distribution, metabolism, and excretion)

Features:

• Offers state-of-the-art presentations of concepts, methods, and technologies now in use or development in drug research
• Includes a CD-ROM containing the invited lectures, oral communications, and posters (in full version) Presented at the Third LogP Symposium, 'Physicochemical and Biological Profiling in Drug Research'

Contents

Setting the Scene

• Pharmaceutical Research: For What, for Whom? Science and Social Policies
• Property-Based Lead Optimization

Biological Strategies

• Membranes - From Barriers to Magic Bullets
• Cell Culture Absorption Models - State of the Art
• Metabolic Studies in Drug Research and Development
• In vitro, in vivo and in silico Approaches to Predict Induction of Drug Metabolism
• Coordination of Uptake and Efflux Transporters in Drug Disposition
• The Role of Plasma Protein Binding in Drug Discovery
• In vivo Pharmacokinetic Profiling of Drugs

Physicochemical Strategies

• Automated Parallel Synthesis in Support of Early Drug Discovery: Balancing Accessibility of Chemistry with the Design of Drug-like Libraries
• New Insights into the Lipophilicity of Ionized Species
• Physicochemical and Biological Profiling in Drug Research. ElogD(7.4) 20,000 Compounds later: Refinements, Observations and Applications
• Lipid Bilayers in ADME: Permeation Barriers and Distribution Compartments
• High-throughput Solubility, Permeability, and the MAD PAMPA Model
• Correlations between PAMPA Permeability and Log P
• Predicting the Intestinal Solubility of Poorly Soluble Drugs
• Accelerated Stability Profiling in Drug Discovery
• Physicochemical Characterisation of the Solid State in Drug Development

Computational Strategies

• Calculation of Lipophilicity: A Classification of Methods
• The Concept of Property Space: The Case of Acetylcholine
• Prediction of Site of Metabolism in Humans: Case Studies of Cytochromes P450 2C9, 2D6 and 3A4
• Use of Pharmacophores in Predictive ADME
• The BioPrint® Approach for the Evaluation of ADME-T Properties: Application to the Prediction of Cytochrome P450 2D6 Inhibition
• Using Computer Reasoning about Qualitative and Quantitative Information to Predict Metabolism and Toxicity
• Physiologically Based Pharmacokinetic Models
• Processing of Biopharmaceutical Profiling Data in Drug Discovery

Concluding Chapters

• Educational and Communication Issues Related to Profiling Compounds for Their Drug-Like Properties (R. T. Borchardt).
• Present and Future Significance of ADMET Profiling in Industrial Drug Research

Index

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