Comprehensive Medicinal Chemistry II

1st Edition

Volume 5: ADME-TOX APPROACHES

Authors:

  • Bernard Testa
  • Han van de Waterbeemd
    • Print ISBN 9780080445182

    Description

    To be effective a drug must be Absorbed then Distributed to the site of action. It must also be Metabolised and Excreted without any measurable Toxicity (ADMET). This volume examines major ADMET issues, tools to measure these properties in vivo and in vitro and in-silico tools to predict and analyse effects. It concludes with a review of tools that can assist drug discovery in its early development stage.

    Key Features

    * valuable content available May 2009 as an individual volume
    * separate volumes will appeal to a wider chemistry, biochemistry and medicinal audience
    * priced for individual researcher as well as library purchase

    Readership

    For students and researchers in chemistry, biochemistry, medicinal chemistry and pharmacology and scientists working in the pharmaceutical industries.

    Table of Contents

    Volume 5 ADME-Tox Approaches
    Introduction
    5.01 The Why and How of Absorption, Distribution, Metabolism, Excretion, and Toxicity Research
    Biological and In Vivo Aspects of Absorption, Distribution, Metabolism, Excretion, and Toxicity
    5.02 Clinical Pharmacokinetic Criteria for Drug Research
    5.03 In Vivo Absorption, Distribution, Metabolism, and Excretion Studies in Discovery and Development
    5.04 The Biology and Function of Transporters
    5.05 Principles of Drug Metabolism 1: Redox Reactions
    5.06 Principles of Drug Metabolism 2: Hydrolysis and Conjugation Reactions
    5.07 Principles of Drug Metabolism 3: Enzymes and Tissues
    5.08 Mechanisms of Toxification and Detoxification which Challenge Drug Candidates and Drugs
    5.09 Immunotoxicology
    Biological In Vitro Tools in Absorption, Distribution, Metabolism, Excretion, and Toxicity
    5.10 In Vitro Studies of Drug Metabolism
    5.11 Passive Permeability and Active Transport Models for the Prediction of Oral Absorption
    5.12 Biological In Vitro Models for Absorption by Nonoral Routes
    5.13 In Vitro Models for Examining and Predicting Brain Uptake of Drugs
    5.14 In Vitro Models for Plasma Binding and Tissue Storage
    5.15 Progress in Bioanalytics and Automation Robotics for Absorption, Distribution, Metabolism, and Excretion Screening
    Physicochemical tools in Absorption, Distribution, Metabolism, Excretion, and Toxicity
    5.16 Ionization Constants and Ionization Profiles
    5.17 Dissolution and Solubility
    5.18 Lipophilicity, Polarity, and Hydrophobicity
    5.19 Artificial Membrane Technologies to Assess Transfer and Permeation of Drugs in Drug Discovery
    5.20 Chemical Stability
    5.21 Solid-State Physicochemistry
    In Silico Tools in Absorption, Distribution, Metabolism, Excretion, and Toxicity
    5.22 Use of Molecular Descriptors for Absorption, Distribution, Metabolism, and Excretion Predictions
    5.23 Electrotopological State Indices to Assess Molecular and Absorption, D

    Details

    No. of pages:
    1181
    Language:
    English
    Copyright:
    © 2007
    Published:
    Imprint:
    Elsevier Science
    Print ISBN:
    9780080445182