Overview

A panel of researchers and experts from leading universities and major pharmaceutical companies from all over the world systematically describe cutting-edge experimental protocols for the early in vitro evaluation of new chemical entities (NCE). These readily reproducible assays measure such critical parameters as physicochemical properties, adsorption, plasma binding, metabolism, drug interactions, and toxicity. By uncovering early in the discovery stage the defects that can eliminate candidate drugs from preclinical and clinical development, these techniques can save millions of dollars in time and effort.

Full Product Details

Author:   Zhengyin Yan ,  Gary W. Caldwell
Publisher:   Humana Press Inc.
Imprint:   Humana Press Inc.
Edition:   Softcover reprint of hardcover 1st ed. 2004
Dimensions:   Width: 15.20cm , Height: 2.40cm , Length: 22.90cm
Weight:   0.637kg
ISBN:  

9781617374999

ISBN 10:   1617374997
Pages:   420
Publication Date:   09 November 2010
Audience:   Professional and scholarly ,  Professional & Vocational
Format:   Paperback
Publisher's Status:   Active
Availability:   In Print  
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Table of Contents

pKa, Solubility, and Lipophilicity.- Use of Caco-2 Cell Monolayers to Study Drug Absorption and Metabolism.- Absorption Screening Using the PAMPA Approach.- In Situ Single-Pass Perfused Rat Intestinal Model for Absorption and Metabolism.- In Vitro Permeation Study With Bovine Brain Microvessel Endothelial Cells.- An Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and Inhibitors.- Evaluation of Drug-Transporter Interactions Using In Vitro Cell Models.- Plasma Protein-Binding Methods in Drug Discovery.- Isothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood Proteins.- Metabolic Stability Assessed by Liver Microsomes and Hepatocytes.- In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes.- In Vitro Identification of UDP-Glucuronosyltransferases (UGTs) Involved in Drug Metabolism.- In Vitro CYP Induction in Human Hepatocytes.- High-Throughput Screening of Human Cytochrome P450 Inhibitors Using Fluorometric Substrates.- Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes.- Identification of CYP Mechanism-Based Inhibitors.- Detection of DNA Adducts by 32P-Postlabeling Analysis.- Covalent DNA Adduct Formation Mediated by Cytochrome P450.- Application of In Vitro Comet Assay for Genotoxicity Testing.- Assessing DNA Damage Using a Reporter Gene System.- Improvement of the Ames Test Using Human Liver S9 Preparation.- Screening for Chemical Mutagens Using the Mouse Lymphoma Assay.- A High-Throughput Binding Assay for HERG.- In Vitro Drug Metabolism.- In Vitro Screening Assay of the Reactivity of Acyl Glucuronides.

Reviews

This book covers most of the currently used techniques in lead optimization with respect to ADME and safety profiles. . .would be very useful addition to the library of any drug scientist interested in an introduction to these important methods. Each chapter treats its topic in a concise manner and provides ample references to lead the reader to more detailed information. -Doody's Health Sciences Book Review Journal ...very useful technically...invaluable to those changing roles or joining a pharmaceutical company, it is also very helpful for scientists in the biotech industry who are new to drug discovery. - Immunology News The book provides a wealth of relevant information...the tome is neatly designed, well constructed and easy to read. - ISSX Newsletter ...a useful reference handbook for in vitro ADMET assays. - ChemBioChem

Aus den Rezensionen: ! Wo liegen die Schwierigkeiten, woran sind fruhere Entwicklungen gescheitert? Dies sind Fragen, die ! mit grossem Sachverstand beantwortet werden. ! Je Spater ein Arzneimittelkandidat in der Entwicklung scheitert, desto grosser ist der finanzielle Verlust fur den pharmazeutischen Unternehmer. ! dieser Verlust kann ! uber den Verkauf von zugelassenen Arzneimitteln wieder wettgemacht werden. Um diese Risiken moglicher niedrig zu halten, ist das ! Buch eine gute Wissensquelle, um die Entwicklung der Arzneimittel zu optimieren. ! Der lange Weg zum Lebensretter -- ein Blick hinter die Kulissen der Medikamentenentwicklung. (Stefan Hockertz, Methods in Pharmacology and Toxicology, in: Arzneimittel - Forschung, 2005, Vol. 55, Issue 7, S. 428)

This book covers most of the currently used techniques in lead optimization with respect to ADME and safety profiles...would be very useful addition to the library of any drug scientist interested in an introduction to these important methods. Each chapter treats its topic in a concise manner and provides ample references to lead the reader to more detailed information. -Doody's Health Sciences Book Review Journal ...very useful technically...invaluable to those changing roles or joining a pharmaceutical company, it is also very helpful for scientists in the biotech industry who are new to drug discovery. - Immunology News The book provides a wealth of relevant information...the tome is neatly designed, well constructed and easy to read. - ISSX Newsletter ...a useful reference handbook for in vitro ADMET assays. - ChemBioChem

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