Key result
hERG blockade increases risk of QT prolongation and life-threatening torsades de pointes.
Why the study?
HERG channels play a critical role in cardiac electrophysiology and have important functions in neurocardiology and other tissues, but their diverse roles and implications require comprehensive review.
HERG channels play a crucial role in cardiac action potentials and pacemaking, and their blockade is associated with QT prolongation and torsade de pointes.
May warrant QT monitoring with HERG-blocking drugs; leaves open precise real-world risk quantification.
Human ether-a-go-go-related gene K(+) channels [HERG](hERG; Kv11.1, KCNH2) encode the rapid delayed-rectifier K + -current (I Kr ) and are expressed in various tissue including heart, various brain regions and a wide range of tumor cell lines [1].The heart HERG slow activation and deactivation kinetics, coupled to their rapid voltage-dependent inactivation and recovery from inactivation, is crucial for determining the duration of the action potential plateau phase and also contribute to pacemaking activity in sinoatrial (SA) and atrioventricular node cells and to diastolic depolarization [1].Extra-cardiac HERG role has suggested in cancer, and in spike-frequency adaptation and burst duration regulation in neurons as well as in regulation of resting membrane potential and action potential firing frequency in smooth muscle and endocrine cells [1].Heart HERG -blockade can lead to QT prolongation with increased risk of potentially life-threatening torsade de pointes arrhythmia (TdP).Several HERG-blockers have withdrawn
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Salvatore Patanà (2014) reported a review. HERG-blockers was evaluated. Heart HERG-blockade can lead to QT prolongation with an increased risk of potentially life-threatening torsade de pointes arrhythmia.
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