Enzyme Kinetics in Drug Metabolism : Fundamentals and Applications - Nagar, Swati; Argikar, Upendra A.; Tweedie, Donald J.; SpringerLink (Online service) (Totowa, NJ : Humana Press : Imprint: Humana, 2014)
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.
Keywords: Pharmacology; Enzymology; Pharmacology/Toxicology.; Enzymology