Table of Contents

Enzyme Kinetics in Drug Metabolism – Fundamentals and Applications.- Fundaments of Enzyme Kinetics.- Different Enzyme Kinetic Models.- Reversible Mechanisms of Enzyme Inhibitors and Resulting Clinical Significance.- Irreversible Enzyme Inhibition Kinetics and Drug-Drug Interactions.- Multi-Enzyme Kinetics and Sequential Metabolism.- Consideration of the Unbound Drug Concentration in Enzyme Kinetics.- Enzyme Kinetics of Oxidative Metabolism – Cytochromes P450.- Enzyme Kinetics, Pharmacokinetics, Inhibition, and Regioselectivity of Aldehyde Oxidase.- Enzyme Kinetics of Conjugative Enzymes – PAPS.- Enzyme Kinetics of Uridine Diphosphate Glucuronosyltransferases (UGTs).- Principles and Experimental Considerations for in vitro Transporter Interaction Assays.- Rationalising Under-Prediction of Drug Clearance from Enzyme and Transporter Kinetic Data – from in vitro Tools to Mechanistic Modeling.- The Structural Model for the Mass Action Kinetic Analysis of P-gp Mediated Transport Through Confluent Cell Monolayers.- Systems Biology Approaches to Enzyme Kinetics: Analyzing Network Models of Drug Metabolism.- Variability in Human in vitro Enzyme Kinetics.- Sources of Interindividual Variability.- Case Study 1. Practical Considerations with Experimental Design and Interpretation.- Case Study 2. Practical Analytical Considerations for Conducting in vitro Enzyme Kinetic Studies.- Case Study 3. Application of Basic Enzyme Kinetics to Metabolism Studies – Real Life Examples.- Case Study 4. Predicting the Drug Interaction Potential for Inhibition of CYP2C8 by Montelukast.- Case Study 5. Deconvoluting Hyperbilirubinemia: Differentiating Between Hepatotoxicity and Reversible Inhibition of UGT1A, MRP2 or OATP1B1 in Drug Development.- Case Study 6. Drug Transporters: in vitro Solutions for Translatable Outcomes.- Case Study 7. Compiled Aha Moments in Enzyme Kinetics: Authors’ Experiences.