The Drug Metabolism and Pharmacokinetics Quick Guide

Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key topics useful at the drug discovery stage, which would serve as a quick reference with several examples from the literature to illustrate the concept.

Covers a number of aspects of drug assessment at drug discovery and development stages Includes topics in pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations Covers key concepts, with useful tables on physiological parameters, chemical structure, nomenclature, and moieties leading to bioactivation

Autorentext

Dr. Siamak Cyrus Khojasteh received his BS from University of California at Berkeley and his PhD from University of Washington in Medicinal Chemistry under the direction of Dr. Sidney D. Nelson. Dr. Khojasteh leads the Metabolism efforts at Genentech (South San Francisco) and leads a team of about 20 scientists and prior to that he was a Senior Research Scientist at Pfizer (Groton, CT). His research interest is mechanism of biotransformation particularly with formation of reactive metabolites by P450 or non-P450 enzymes.

Harvey Wong graduated from the University of British Columbia with a Ph.D. in Pharmacokinetics and Biopharmaceutics. Following graduation, he worked at the DuPont Pharmaceutics Company followed by Bristol-Myers Squibb in the area of Neuroscience Drug Discovery. Currently, Harvey is a Senior Scientist in the Department of Drug Metabolism and Pharmacokinetics at Genentech, Inc. working in the areas of oncology and immunology. He is involved in pharmacokinetic modeling and defining preclinical PK-PD relationships for drug candidates in both therapeutic areas. Harvey has published over 70 publications and abstracts.

Dr. Cornelis E.C.A. Hop is supervising the Small Molecule Drug Metabolism & Pharmacokinetics Department at Genentech (South San Francisco) and leads a team of about 55 scientists involved in acquisition and interpretation of ADME data in support of drug discovery and development. Before that he was a senior director at Pfizer (Groton, CT) and a Senior Research Fellow at Merck (Rahway, NJ). Dr. Hop has extensive experience in ADME sciences and biotransformation, PK prediction and bioanalysis in particular. He has authored more than 100 publications in refereed journals and several book chapters and made more than 50 external oral presentations at conferences and universities.

Klappentext

Drug Metabolism and Pharmacokinetics Quick Guide is intended for broad readership of those interested in the discipline of drug metabolism and pharmacokinetics who work in drug discovery coming from the various disciplines, a background such as of medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics or toxicology.

This guide provides, for the first time, a completely integrated look at multiple aspects of absorption, distribution, metabolism, and excretion (ADME) science in a summary format that is clear, concise and self-explanatory.

This book will be used and referenced frequently as it provides detailed figures and tables for data interpretation. Also included are brief yet relevant factoids that bring a real-world dimension to the discussion of drug metabolism and pharmacokinetics.

Key topics covered:

1. Pharmacokinetics

2. Drug metabolizing enzymes

3. Oral absorption

4. Transporters

5. Metabolism-based drug interactions

6. Biotransformation and bioactivation

7. Prediction of human pharmacokinetics

8. Bioanalysis

9. Physicochemical properties and drug-like properties

10. In silico tools

11. Approved drugs

12. Chemical nomenclature

Inhalt
Pharmacokinetics.- Drug Metabolizing Enzymes.- Oral Absorption.- Transporters.- Metabolism-Based Drug Interactions.- Biotransformation and Bioactivation.- Prediction of Human Pharmacokinetics.- Advances in Bioanalysis as it Relates to ADME.- ADME Properties and Their Dependence on Physicochemical Properties.- In Silico ADME Tools.- Approved Drugs.- Chemical Nomenclature.