Early afterdepolarisation tendency as a simulated pro-arrhythmic risk indicator
Abstract
Drug-induced Torsades de Pointes (TdP) arrhythmia is of major interest in predictive toxicology. Drugs which cause TdP block the hERG cardiac potassium channel. However, not all drugs that block hERG cause TdP. As such, further understanding of the mechanistic route to TdP is needed. Early afterde-polarisations (EADs) are a cell-level phenomenon in which the membrane of a cardiac cell depolarises a second time before repolarisation, and EADs are seen in hearts during TdP. Therefore, we propose a method of predicting TdP using induced EADs combined with multiple ion channel block in simulations using biophysically-based mathematical models of human ventricular cell electrophysiology. EADs were induced in cardiac action potential models using interventions based on diseases that are known to cause EADs, including: increasing the conduction of the L-type calcium channel, decreasing the conduction of the hERG channel, and shifting the inactivation curve of the fast sodium channel. The threshold of intervention that was required to cause an EAD was used to classify drugs into clinical risk categories. The metric that used L-type calcium induced EADs was the most accurate of the EAD metrics at classifying drugs into the correct risk categories, and increased in accuracy when combined with action potential duration measurements. The EAD metrics were all more accurate than hERG block alone, but not as predictive as simpler measures such as simulated action potential duration. This may be because different routes to EADs represent risk well for different patient subgroups, something that is difficult to assess at present.
02 /Specification & Classification
Click any tag to browse matching papers- Organism
- Assay
- Research Focus
- Approach
Reproducibility ledger
Nobody has reported trying to reproduce this paper yet. Did you replicate an experiment or run the code? Your report saves the next lab a week.
Sign in to file a reproducibility report.
Related papers
- Independent derivations of the axis of arrhythmia for predicting drug-induced torsades de pointes
Stewart Heitmann, Jamie I. Vandenberg, Adam Parker Hill·British Journal of PharmacologyPeer-reviewed·Jun 1, 2025
- Sex-specific classification of drug-induced Torsade de Pointes susceptibility using cardiac simulations and machine learning
A. Fogli Iseppe, H. Ni, … E. Grandi·Clinical Pharmacology & TherapeuticsPeer-reviewed·Apr 19, 2021
- Transmural and rate-dependent profiling of drug-induced arrhythmogenic risks through in silico simulations of multichannel pharmacology
- Intrinsic structure of model-derived metrics for in silico proarrhytmic risk assessment identified by global sensitivity analysis
J. Parikh, P. Di Achille, … V. Gurev·bioRxiv·Apr 16, 2019
- Prediction of TdP Arrhythmia Risk Through Molecular Simulations of Conformation-specific Drug Interactions with the hERG K+, NaV1.5, and CaV1.2 Channels
Kyle C. Rouen, Kush Narang, … Igor V. Vorobyov·bioRxiv·Sep 25, 2025
- Estimating the Probability of Early Afterdepolarization and Predicting Arrhythmic Risk associated with Long QT Syndrome Type 1 Mutations
Q. Jin, J. L. Greenstein, R. L. Winslow·bioRxiv·Apr 9, 2020