Antitargets: Prediction and Prevention of Drug Side Effects / Edition 1

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Overview

This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes several highly instructive case studies that may be used as guidelines on how to improve drug development projects.
With its large section on ADME-related effects, this is key knowledge for every drug developer.

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Product Details

Meet the Author

Roy Vaz is the head of investigative pharmacokinetics at theBridgewater, NJ (USA) location of Sanofi-Aventis Pharmaceuticals.He received his Ph.D. in Organic Chemistry from the University ofFlorida, Gainesville (USA), after graduating from the IndianInstitute of Technology in Mumbai (India). Prior to his presentappointment, he has worked with Bristol-Myers-Squibb and Tripos. Heis a specialist on the prediction and modeling ofcytochrome-mediated drug metabolism.

Thomas Klabunde obtained his PhD in chemistry from the Universityof M√ľnster (Germany). After a postdoctoral fellowship at theTexas A&M University, he was appointed Assistant Professor atthe Institute for Bioscience and Technology in Houston (USA). Lateron, he joined the pharmaceutical research of Sanofi-Aventis inFrankfurt (Germany), where he is currently a group leader. His maininterest lies with drug design approaches for G protein-coupledreceptors, notably in the areas of lead finding andchemogenomics.

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Table of Contents

PART I: GENERAL ASPECTS
Why drugs fail: study on side effects in New ChemicalEntities
Use of Broad Biological Profiling as a Relevant Descriptor toDescribe and Differentiate Compounds: Structure-In Vitro(Pharmacology-ADME)-In Vivo (Safety) Relationships
PART II: ANTITARGETS: ION CHANNELS AND GPCRs
Pharmacological and regulatory aspects of QT prolongation hERG Channel Physiology and Drug-Binding Structure-ActivityRelationships
Qsar and Pharmacophores for Drugs Involved in hERG Blockage
GPCR Antitarget Modeling: Pharmacophore Models to AvoidGPCR-Mediated Side Effects
The Emergence of Serotonin 5-HT2B Receptors as Drug"Antitargets"
Computational Modeling of Selective Pharmacophores at thea1-Adrenergic Receptors
PART III: ANTITARGETS: CYTOCHROME P450s AND TRANSPORTERS
Cytochrome P450s: drug-drug interactions
Site of Metabolism Predictions: Facts and Experiences
Irreversible Cytochrome P450 Inhibition: Common Sub-Structures andImplications for Drug Development
MetaSite: Understanding CYP Antitarget Modeling for Early ToxicityDetection
Orphan Nuclear Receptor PXR-Mediated Gene Regulation in DrugMetabolism and Endobiotic Homeostasis
Ligand Features Essential for Cytochrome P450 Induction
Transporters and Drugs -
An Overview
Computational Models for P-Glycoprotein Substrates andInhibitors
PART IV: CASE STUDIES OF DRUG OPTIMIZATION AGAINSTANTITARGETS
Selective Dipeptidyl Peptidase IV Inhibitors for the Treatment ofType 2 Diabetes: The Discovery of JANUVIA (Sitagliptin)
Strategy and Tactics for hERG Optimizations
Structure-Based In Silico Driven Optimization: Discovery of theSelective 5-HT1A Agonist PRX-00023

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