The Drug Metabolism and Pharmacokinetics Quick Guide

Pharmacokinetics.- Drug Metabolizing Enzymes.- Biotransformation.- Transporters.- Drug-Drug Interaction.- Bioactivation and Toxicophores.- Use of Protein, Tissue and Microsomal Binding.- Prediction of Human Pharmacokinetics.- PK/PD Modeling.- Bioanalyticals.- Physicochemical Properties and Drug-like Properties.- In Silico Tools.- Data Mining.- Chemical Nomenclature.- References

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.

From the reviews:

"The authors have to be complimented with this comprehensive book of reference on various important topics in the field of pharmacokinetics and drug metabolism. It contains a large collection of figures and tables providing relevant and well-organized information. ... In conclusion, this is a valuable reference for workers in the field of pharmacokinetics and drug metabolism, providing a storehouse of information in a comprehensive book." (Johannes H. Proost, International Journal of Clinical Pharmacology and Therapeutics, Vol. 50 (6), June, 2012)

"The authors intend the book to inform important decisions in a timely fashion 'for synthesis of superior compounds that have the potential for being a safe and effective drug'. The summary format was designed to be clear, concise and self-explanatory, so it could be used on a daily basis to inform those design decisions. It achieves this goal. It is intended for all drug-discovery scientists, and researchers in all disciplines will certainly find it useful. ... In summary, this is a valuable little book." (Andy Davis, ChemMedChem, Vol. 7, 2012)"This guide can be used on a day-to-day basis as a useful reference for almost anyone, including students first learning these concepts, as well as scientists in the pharmaceutical industry hoping to apply these principles in their research. ... This is a nicely organized quick reference on basic concepts in pharmacokinetics and drug metabolism. It will be a useful addition to the libraries of a variety of readers, from students in the pharmaceutical sciences to accomplished researchers in drug development."­­­ (Melissa M. Ranieri, Doody's Book Reviews, December, 2011)

From the reviews:

"The authors have to be complimented with this comprehensive book of reference on various important topics in the field of pharmacokinetics and drug metabolism. It contains a large collection of figures and tables providing relevant and well-organized information. ... In conclusion, this is a valuable reference for workers in the field of pharmacokinetics and drug metabolism, providing a storehouse of information in a comprehensive book." (Johannes H. Proost, International Journal of Clinical Pharmacology and Therapeutics, Vol. 50 (6), June, 2012)

"The authors intend the book to inform important decisions in a timely fashion 'for synthesis of superior compounds that have the potential for being a safe and effective drug'. The summary format was designed to be clear, concise and self-explanatory, so it could be used on a daily basis to inform those design decisions. It achieves this goal. It is intended for all drug-discovery scientists, and researchers in all disciplines will certainly find it useful. ... In summary, this is a valuable little book." (Andy Davis, ChemMedChem, Vol. 7, 2012)"This guide can be used on a day-to-day basis as a useful reference for almost anyone, including students first learning these concepts, as well as scientists in the pharmaceutical industry hoping to apply these principles in their research. ... This is a nicely organized quick reference on basic concepts in pharmacokinetics and drug metabolism. It will be a useful addition to the libraries of a variety of readers, from students in the pharmaceutical sciences to accomplished researchers in drug development." (Melissa M. Ranieri, Doody's Book Reviews, December, 2011)