Key result
Vanoxerine blocked hERG, hCav1.2, and hNav1.5 channels at clinically relevant concentrations without producing proarrhythmia markers, explaining its lack of torsadogenicity.
Population
Heterologously expressed human cardiac ion channels in HEK 293 and CHO cells, and human induced pluripotent…
Comparison
Vanoxerine vs Dofetilide, verapamil, and bepridil
Design
Preclinical
Authors
Loading...
Supports multi-channel blockade mitigating torsadogenicity in animal models; leaves open translation to clinical safety assessment.
Vanoxerine's potent hERG blockade is offset by its blockade of calcium and sodium channels (Multiple Ion Channel Effects), explaining its lack of torsadogenic liability and supporting its safety profile.
Obejero‐Paz et al. (2015) studied Cardiac arrhythmias (Atrial fibrillation/flutter). Vanoxerine vs. Dofetilide, verapamil, bepridil was evaluated on IC50 for hERG channel block (nM) (95% CI 7.2-11.8). Vanoxerine blocked hERG, hCav1.2, and hNav1.5 channels at clinically relevant concentrations without producing proarrhythmia markers, explaining its lack of torsadogenicity.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: