Enzyme Kinetics in Drug Metabolism

 Fundamentals of Enzyme Kinetics – Michaelis-Menten and Non-Michaelis Type (Atypical) Enzyme Kinetics.- Reversible Mechanisms of Enzyme Inhibition 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.- Numerical Methods for Modeling Enzyme Kinetics.- Crystal Structures of Drug-Metabolizing CYPs.- The Structure and Mechanism of Drug Transporters.- Enzyme Kinetics of Oxidative Metabolism – Cytochromes P450.- Enzyme Kinetics, Pharmacokinetics, and Inhibition of Aldehyde oxidase.- Enzyme Kinetics of PAPS-sulfotransferase.- Enzyme Kinetics of Uridine Diphosphate Glucuronosyltransferases (UGTs).- Principles and Experimental Considerations for In Vitro Transporter Interaction Assays.- Prediction of Drug Clearance from Enzyme and Transporter Kinetics.- Systems Biology Approaches to Enzyme Kinetics.- Variability in Human In Vitro Enzyme Kinetics.- Sources of Interindividual Variability.- Ontogeny of Drug Metabolizing Enzymes.- How Science is Driving Regulatory Guidances.- 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: Criticality of High-Quality Curve Fitting: Getting a Km,app isn’t as Simple as it May Seem.- Case Study 4 Application of Basic Enzyme Kinetics To Metabolism Studies  – Real Life Examples.- Case Study 5. Predicting the Drug Interaction Potential for Inhibition of CYP2C8 by Montelukast.- Case Study 6: Deconvoluting Hyperbilirubinemia: Differentiating between Hepatotoxicity and Reversible Inhibition of UGT1A1, MRP2 or OATP1B1 in Drug Development.- Case Study 7. Transporters Case Studies: In Vitro Solutions for Translatable Outcomes­.- Case Study 8: Status of the Structural Mass Action Kinetic Model of P-gp MediatedTransport through Confluent Cell Monolayers.- Case Study 9: Probe-Dependent Binding Explains Lack of CYP2C9 Inactivation by 1-Aminobenzotriazole (ABT).- Case Study 10: A Case to Investigate Acetyl Transferase Kinetics.- Case Study 11.  Considerations for Enzyme Mapping Experiments: Interaction between the Aldehyde Oxidase Inhibitor Hydralazine and Glutathione.- Case Study 12: Roadmap to Quantifying Ago2-Mediated siRNA Metabolic Activation Kinetics.