The Encyclopedia of Drug Metabolism and Interactions provides essential support during all phases of drug development, from drug design to drug action and interaction in patients.

Table of Contents

• Part 1: Basics Overview of Drug Metabolism
• Chapter 1 Review of Drug Metabolism in Drug Discovery and Development
• Chapter 2 In Vitro and In Vivo Models of Drug Metabolism
• Chapter 3 Enzyme Kinetics of Drug-Metabolizing Reactions and Drug–Drug Interactions
• Chapter 4 Sex Differences in Drug Metabolism
• Chapter 5 Species Differences of Drug-Metabolizing Enzymes
• Part II: Enzyme Systems Involved in Drug Metabolism and Interactions in Animals and Humans
• Chapter 6 Structure and Function of Cytochrome P450 Enzymes
• Chapter 7 Mechanisms of Cytochrome P450-Mediated Reactions
• Chapter 8 Transcriptional Regulation of Cytochrome P450 Genes
• Chapter 9 Cytochrome P450 Polymorphisms
• Chapter 10 Flavin-Containing Monooxygenase: The Role of Flavin-Containing Monooxgenase in Lead Design and Selection
• Chapter 11 Molybdenum-Containing Hydroxylases
• Chapter 12 Amine Oxidases and Reductases
• Chapter 13 Epoxide Hydrolases
• Chapter 14 Carboxylesterases
• Chapter 15 UDP-Glucuronosyltransferases: Pharmacogenetics, Functional Characterization, and Clinical Relevance
• Chapter 16 Sulfotransferases
• Chapter 17 Functional Genomics of the Human Glutathione Transferases
• Chapter 18 Amino Acid Conjugation: A Novel Route of Xenobiotic Carboxylic Acid Metabolism in Man
• Part III: General principals of ADME. Drug Transporters and Other Mechanisms of Transport
• Chapter 1 ADME Profiling in Drug Discovery and Development: An Overview
• Chapter 2 Anatomical and Physiological Parameters that Influence Gastrointestinal Absorption
• Chapter 3 Oral Absorption: from Physiology to Regulatory
• Chapter 4 General Principles of Drug Distribution
• Chapter 5 ABC Drug Transporters and Their Impact on Drug Disposition/Drug Sensitivity and Resistance
• Chapter 6 Solute Carrier (SLC) Family Transporters
• Chapter 7 Mechanisms of Drug Metabolism
• Chapter 8 Extrahepatic Drug-Metabolizing Enzymes and Their Significance
• Chapter 9 Mass Balance Studies in Animals and Humans
• Chapter 10 Bioavailability and Bioequivalence
• Chapter 11 Interspecies Pharmacokinetic Scaling and the Prediction of Human Pharmacokinetics Using Animal and Cell Models
• Chapter 12 The Significance and Determination of Plasma Protein Binding
• Chapter 13 Excretion Systems
• Chapter 14 Pharmacokinetics and Toxicokinetics in Drug Discovery and Development
• Chapter 15 Pharmacokinetic Data Analysis and Modeling of ADME Processes
• Chapter 16 Physiologically Based Pharmacokinetic (PBPK) Modeling: Usefulness and Applications
• Chapter 17 Pharmacodynamics
• Chapter 18 Translational Drug Discovery Research: Integration of Medicinal Chemistry, Computational Modeling, Pharmacology, ADME, and Toxicology
• Part IV: ADME of Some Specific Groups of Drugs and Delivery Systems
• Chapter 19 ADME of Herbal Dietary Supplements
• Chapter 20 ADME of Anticancer Drugs
• Chapter 21 ADME of Cardiovascular Drugs
• Chapter 22 Disposition of Biological Therapeutics: Monoclonal Antibodies, Proteins, and Peptides
• Chapter 23 ADME of Natural Toxins
• Chapter 24 Influence of Changes in Physiology, Transporters, and Enzyme Expression on Disposition and Metabolism of Drugs during Pregnancy and Clinical Implications
• Part V: Drug Design and Development
• Chapter 1 When and How to Apply ADMET Principles to Drug Discovery and Development
• Chapter 2 Molecular Challenges in Front-Loading Toxicity Testing of Anticancer Drugs in Drug Discovery
• Chapter 3 Role of ADME Studies in Selecting Drug Candidates: Dependence of ADME Parameters on Physicochemical Properties
• Chapter 4 Effective Early Drug Development
• Chapter 5 Identification of Drug Metabolites
• Chapter 6 Drug Bioactivation and Oxidative Stress
• Chapter 7 Drug Metabolism in Drug Safety Evaluation
• Part VI: Methods and Protocols for Prediction and Evaluation of Drug Metabolism and Drug Interaction Studies
• Chapter 8 In Silico Models of Drug Metabolism and Drug Interactions
• Chapter 9 Methods for Determination of Enzyme Kinetics and Metabolic Rates
• Chapter 10 Utility of Molecular-Based In Vitro Assays in Metabolic Liability of Drug Candidates
• Chapter 11 Applications Using Caco-2 and TC7 Cells for Drug Metabolism Studies
• Chapter 12 In Vitro Liver Systems to Study Induction/Inhibition: Prediction of In Vivo Metabolism and Drug–Drug Interactions
• Chapter 13 Assessing the Hepatic Disposition and Toxicity of Xenobiotics Using Primary Hepatocytes
• Chapter 14 Monoclonal Antibody Analyses of Microsomal Human Drug Metabolism and Multifunctional Cytochrome P450
• Chapter 15 Precision-Cut Tissue Slices: A Suitable In Vitro System for the Study of the Induction of Drug-Metabolizing Enzyme Systems
• Chapter 16 The Impact of Solubility and Dissolution Assessment on Formulation Strategy and Implications for Oral Drug Disposition
• Chapter 17 Integrated Approaches to Blood–Brain Barrier
• Chapter 18 Why Do We Need In Vivo Models in Drug Metabolism?
• Chapter 19 Utility of Genetically Modified Animal Models for Drug Metabolism and Drug Transporters
• Part VII: Role of Metabolism in Toxicology and Pharmacology
• Chapter 1 Introduction: An Overview of the Role of Metabolism in Drug Toxicity
• Chapter 2 Bioactivation I: Bioactivation by Cytochrome P450s
• Chapter 3 Bioactivation II: Phase I (Non-P450)
• Chapter 4 Bioactivation by Phase-II-Enzyme-Catalyzed Conjugation of Xenobiotics
• Chapter 5 Covalent Drug–Protein Adducts: An Exploration of Their Role in Drug-Induced Liver and General Organ Toxicity
• Chapter 6 Safety Testing of Drug Metabolites: A Practical Approach for the Implementation of the MIST Guidance in PKDM
• Chapter 7 In Vitro Toxicity Screening in Early Drug Discovery: Importance of Metabolism and Reactive Metabolites
• Chapter 8 The Application of Preclinical Toxicogenomics for Predicting and Understanding Drug-Induced Toxicity and Metabolism
• Chapter 9 Metabonomics in Understanding Drug Metabolism and Toxicology
• Chapter 10 Proteomics in Drug Discovery and Development
• Chapter 11 Stereochemical Elements Associated with Drug Metabolism and Toxicity
• PART VIII: Influence of Physiological Conditions, Diseases, Drug–Food Interactions, Age, Sex, and Other Factors on Drug Metabolism and Effect
• Chapter 12 Genetics of Drug Disposition
• Chapter 13 Drug–Drug Interactions 1: Inhibition
• Chapter 14 Clinical Implications of CYP Induction-Mediated Drug–Drug Interactions
• Chapter 15 Age-Dependent Expression of Human Drug-Metabolizing Enzymes
• Chapter 16 Phytochemical Modulators of Human Drug Metabolism: Drug Interactions with Fruits, Vegetables, and Botanical Dietary Supplements
• Chapter 17 Idiosyncratic Drug Reactions
• Chapter 18 Animal Models of Idiosyncratic, Drug-Induced Liver Injury: Emphasis on the Inflammatory Stress Hypothesis
• Chapter 19 Regulation of Drug Metabolizing Enzymes and Transporters in Infection, Inflammation, and Cancer
• Part IX: Bioanalytical Methods of Studying Metabolism
• Chapter 1 Bioanalytical Support for Both In Vitro and In Vivo Assays Across Drug Discovery and Drug Development
• Chapter 2 General Principles of Mass Spectrometry: GC-MS, LC-MS, and LC-MS/MS
• Chapter 3 Infusion Nanoelectrospray Ionization Mass Spectrometry
• Chapter 4 A Perspective on the Evolving Field of Ambient Ionization Mass Spectrometry
• Chapter 5 Matrix-Assisted Laser Desorption/Ionization
• Chapter 6 Triple Quadrupole and Quadrupole Ion Trap Mass Spectrometers
• Chapter 7 Hybrid Mass Analyzers in Drug Metabolism Applications
• Chapter 8 Imaging Mass Spectrometry
• Chapter 9 Gas-Phase Ion Mobility-Mass Spectrometry (IM-MS) and Tandem IM-MS/MS Strategies for Metabolism Studies and Metabolomics
• Chapter 10 Inductively Coupled Plasma Mass Spectrometry for Analysis of Metal-Containing Pharmaceuticals
• Chapter 11 On-Line Electrochemical/LC-MS Techniques for Profiling and Characterizing Metabolites
• Chapter 12 Nuclear Magnetic Resonance Spectroscopy for the Study of Drug Metabolism
• Chapter 13 Whole-Body Autoradiography and Microautoradiography in Drug Discovery and Development
• Chapter 14 Ligand-Binding Assays
• Chapter 15 Micellar Electrokinetic Chromatography
• Chapter 16 Direct Biofluid Analysis Systems
• Chapter 17 Analytical Method Development and Validation in Accordance to the Regulatory Guidelines
• Chapter 18 Leveraging Advances in HPLC and Sample Preparation to Maximize DMPK Data Quality
• Chapter 19 High Throughput Quantitative Mass Spectrometry
• Chapter 20 The Role of Biomarkers in Drug Discovery and Development: Enabling PK/PD
• Chapter 21 Bioanalytics for Human Microdosing
• Chapter 22 Bioactivation and Reactive Metabolite Assays
• Chapter 23 Plasma Protein Binding Methods in Drug Discovery and Development: Bioanalysis
• Part X: Clinical Aspects of Drug Metabolism and Interactions
• Chapter 1 Clinical Aspects of Drug Biotransformation: An Overview
• Chapter 2 CYP450 Enzymes in Drug Discovery and Development: An Overview
• Chapter 3 DDI Risk Assessment and Evaluation in Pharmaceutical Development: Interfacing Drug Metabolism and Clinical Pharmacology
• Chapter 4 Current and Future Tools for Predicting Clinical Drug–Drug Interactions
• Chapter 5 Predicting Human Biotransformation Pathways
• Chapter 6 Conjugation, Transport, and Elimination of Drugs in Humans
• Chapter 7 Role and Clinical Consequences of Human UDP-Glucuronosyltransferases
• Chapter 8 Herb–Drug and Food–Drug Interactions
• Chapter 9 Effects of Liver Disease on Drug Metabolism in Humans
• Chapter 10 Role of Phase I Metabolism in Drug Activation and Clinical Treatment Outcomes
• Chapter 11 Role of Metabolism in Toxicity of Drugs in Humans
• Chapter 12 Idiosyncratic Drug Reactions and the Potential Role of Metabolism
• Part XI Metabolism of Specific Drug Groups and Patient Populations
• Chapter 13 Metabolism of Psychotropic Drugs
• Chapter 14 Metabolism-Based Consequences of Polytherapy with Antiepileptic Drugs
• Chapter 15 Oral Chemotherapeutic Agents
• Chapter 16 Drug Metabolism and Interactions in Pediatric Patients
• Chapter 17 Population-Based Pharmacokinetic Modeling and Simulation
• Chapter 18 Clinical Pharmacology in Drug Labeling. The Impact of Drug Metabolism and Clinical Pharmacology on Recommended Dose of Drugs