Evolution of strategies to improve preclinical cardiac safety testing
G Gintant, PT Sager, N Stockbridge - Nature reviews Drug discovery, 2016 - nature.com
The early and efficient assessment of cardiac safety liabilities is essential to confidently
advance novel drug candidates. This article discusses evolving mechanistically based …
advance novel drug candidates. This article discusses evolving mechanistically based …
[HTML][HTML] The comprehensive in vitro proarrhythmia assay (CiPA) initiative—update on progress
T Colatsky, B Fermini, G Gintant, JB Pierson… - … of pharmacological and …, 2016 - Elsevier
The implementation of the ICH S7B and E14 guidelines has been successful in preventing
the introduction of potentially torsadogenic drugs to the market, but it has also unduly …
the introduction of potentially torsadogenic drugs to the market, but it has also unduly …
Comprehensive in vitro Proarrhythmia Assay, a novel in vitro/in silico paradigm to detect ventricular proarrhythmic liability: a visionary 21st century initiative
I Cavero, H Holzgrefe - Expert opinion on drug safety, 2014 - Taylor & Francis
Introduction: The Comprehensive in vitro Proarrhythmia Assay (CiPA) is a novel safety
screening proposal intended to replace the 2005 regulatory strategy recommended by the …
screening proposal intended to replace the 2005 regulatory strategy recommended by the …
An automated fitting procedure and software for dose-response curves with multiphasic features
In cancer pharmacology (and many other areas), most dose-response curves are
satisfactorily described by a classical Hill equation (ie 4 parameters logistical). Nevertheless …
satisfactorily described by a classical Hill equation (ie 4 parameters logistical). Nevertheless …
Optimization of an In silico Cardiac Cell Model for Proarrhythmia Risk Assessment
Drug-induced Torsade-de-Pointes (TdP) has been responsible for the withdrawal of many
drugs from the market and is therefore of major concern to global regulatory agencies and …
drugs from the market and is therefore of major concern to global regulatory agencies and …
Improving the in silico assessment of proarrhythmia risk by combining hERG (human ether-à-go-go-related gene) channel–drug binding kinetics and multichannel …
Background—The current proarrhythmia safety testing paradigm, although highly efficient in
preventing new torsadogenic drugs from entering the market, has important limitations that …
preventing new torsadogenic drugs from entering the market, has important limitations that …
Systems toxicology: real world applications and opportunities
Systems Toxicology aims to change the basis of how adverse biological effects of
xenobiotics are characterized from empirical end points to describing modes of action as …
xenobiotics are characterized from empirical end points to describing modes of action as …
Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells
J Kramer, HM Himmel, A Lindqvist, S Stoelzle-Feix… - Scientific reports, 2020 - nature.com
Automated patch clamp (APC) instruments enable efficient evaluation of electrophysiologic
effects of drugs on human cardiac currents in heterologous expression systems. Differences …
effects of drugs on human cardiac currents in heterologous expression systems. Differences …
Natural products modulating the hERG channel: heartaches and hope
Covering: 1996–December 2016 The human Ether-à-go-go Related Gene (hERG) channel
is a voltage-gated potassium channel playing an essential role in the normal electrical …
is a voltage-gated potassium channel playing an essential role in the normal electrical …
In Silico Classifiers for the Assessment of Drug Proarrhythmicity
Drug-induced torsade de pointes (TdP) is a life-threatening ventricular arrhythmia
responsible for the withdrawal of many drugs from the market. Although currently used TdP …
responsible for the withdrawal of many drugs from the market. Although currently used TdP …