Antitargets and drug safety / edited by Laszlo Urban, Vinod F. Patel and Roy J. Vaz.

Includes bibliographical references and index.

Print version record.

General Concept for Target-based Safety Assessment. Side Effects of Marketed Drugs: The Utility and Pitfalls of Pharmacovigilance / Steven Whitebread, Mateusz Maciejewski, Alexander Fekete, Eugen Lounkine, László Urbán -- Prediction of Drug Side Effects / Michael J Keiser -- Translational Value of Preclinical Safety Assessment: System Organ Class (SOC) Representation of Off-Targets / Mateusz Maciejewski, Eugen Lounkine, Andreas Hartmann, Steven Whitebread, László Urbán -- Pathological Conditions Associated with the Disturbance of the 5-HT System / Daniel Hoyer -- Hepatic Side Effects. Drug-Induced Liver Injury: Clinical and Diagnostic Aspects / John R Senior -- Mechanistic Safety Biomarkers for Drug-Induced Liver Injury / Daniel J Antoine -- Models for the Prediction of Drug-Induced Liver Injury in Lead Discovery / Frederic Moulin, Oliver Flint -- Transporters in the Liver / Bruno Stieger, Gerd A Kullak-Ublick -- Mechanistic Modeling of Drug-Induced Liver Injury (DILI) / Kyunghee Yang, Jeffrey L Woodhead, Lisl K Shoda, Yuching Yang, Paul B Watkins, Kim LR Brouwer, Brett A Howell, Scott Q Siler -- Cardiovascular Side Effects. Functional Cardiac Safety Evaluation of Novel Therapeutics / Jean-Pierre Valentin, Brian Guth, Robert L Hamlin, Pierre Lainée, Dusty Sarazan, Matt Skinner -- Safety Aspects of the Ca1.2 Channel / Berengere Dumotier, Martin Traebert -- Cardiac Sodium Current (Na1.5) / Gary Gintant -- Circulating Biomarkers for Drug-Induced Cardiotoxicity: Reverse Translation from Patients to Nonclinical Species / Gül Erdemli, Haisong Ju, Sarita Pereira -- The Mechanistic Basis of hERG Blockade and the Proarrhythmic Effects Thereof / Robert A Pearlstein, K Andrew MacCannell, Qi-Ying Hu, Ramy Farid, José S Duca -- Kinase Antitargets. Introduction to Kinase Antitargets / Mark C Munson -- Clinical and Nonclinical Adverse Effects of Kinase Inhibitors / Douglas A Keller, Richard J Brennan, Karen L Leach -- Cardiac Side Effects Associated with Kinase Proteins and Their Signaling Pathways / Roy J Vaz, Vinod F Patel -- Case Studies: Selective Inhibitors of Protein Kinases : Exploiting Demure Features / Ellen R Laird -- Examples of Clinical Translation. Torcetrapib and Dalcetrapib Safety: Relevance of Preclinical and Models / Eric J Niesor, Andrea Greiter-Wilke, Lutz Müller -- Targets Associated with Drug-Related Suicidal Ideation and Behavior / Andreas Hartmann, Steven Whitebread, Jacques Hamon, Alexander Fekete, Christian Trendelenburg, Patrick Y Müller, László Urbán.

With its focus on emerging concerns of kinase and GPCR-mediated antitarget effects, this vital reference for drug developers addresses one of the hot topics in drug safety now and in future. Divided into three major parts, the first section deals with novel technologies and includes the utility of adverse event reports to drug discovery, the translational aspects of preclinical safety findings, broader computational prediction of drug side-effects, and a description of the serotonergic system. The main part of the book looks at some of the most common antitarget-mediated side effects, focusing.