Drug intelligence / Profile preview

clofilium

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intravenous
01

Overview

Clofilium is a quaternary ammonium small molecule that functions as a Class III antiarrhythmic agent. It primarily acts by blocking delayed rectifier potassium channels in cardiac tissue, which results in the prolongation of the cardiac action potential duration and an increase in the effective refractory periods of both the atria and ventricles. Notably, clofilium achieves these effects without significantly altering cardiac conduction velocity. Developed historically by Eli Lilly, the compound was investigated for its potential to treat life-threatening arrhythmias such as ventricular tachycardia and ventricular fibrillation, and was shown to reduce the energy requirements for electrical defibrillation. However, its clinical development was hampered by potential proarrhythmic risks, and it is now primarily utilized as a pharmacological research tool to study potassium channel kinetics and drug-induced arrhythmias.

Other names
clofilium tosylateclofilium phosphate4-chloro-N,N-diethyl-N-heptylbenzenebutanaminium
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)KCNT1 (Potassium channel subfamily T member 1)KCNH1Kv1 (Potassium voltage-gated channel subfamily A)KCNA5 (Ultra-rapid delayed rectifier potassium channel)KCNT2

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