This book is intended for a broad readership, in particular, those working or interested in drug discovery coming from various disciplines such as medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics, and toxicology. It provides, for the first time, a completely integrated look at multiple aspects of ADME sciences (absorption, distribution, metabolism, and excretion) in a summary format that is clear, concise, and self-explanatory. DMPK in Drug Discovery - Guide to Data Interpretation and integration leverages the prior knowledge from the first book that covers the basics of each concept (Drug Metabolism and Pharmacokinetics Quick Guide). This reference book is meant to be used day to day and provides many useful tables (used for data interpretation), figures, and case studies that can facilitate drug discovery. The case studies are intended to be short and relevant to the topic discussed and present another dimension to the discussions.

Highlights assays, parameters to be optimized, candidate properties, and assessment Contains a large amount of reference data that are useful for day-to-day interpretation of ADME studies Multi disciplinary approach

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

This book is intended for a broad readership, in particular, those working or interested in drug discovery coming from various disciplines such as medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics, and toxicology. It provides, for the first time, a completely integrated look at multiple aspects of ADME sciences (absorption, distribution, metabolism, and excretion) in a summary format that is clear, concise, and self-explanatory. DMPK in Drug Discovery - Guide to Data Interpretation and integration leverages the prior knowledge from the first book that covers the basics of each concept (Drug Metabolism and Pharmacokinetics Quick Guide). This reference book is meant to be used day to day and provides many useful tables (used for data interpretation), figures, and case studies that can facilitate drug discovery. The case studies are intended to be short and relevant to the topic discussed and present another dimension to the discussions.

Inhalt
Goals for DMPK during drug optimizations.- Drug Properties.- DMPK in lead optimization.- Candidate tranlational characterization.- Q&A of DMPK issues and tools for drug discovery.- ADME assays.- Regulatory documents for IND to Support FIH.- Appendix: Chemical nomenclature.