Drug intelligence / Profile preview

cibenzoline

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cibenzoline is a small molecule antiarrhythmic drug classified as a Class Ia agent. It acts primarily by blocking sodium channels in cardiac myocytes, thereby suppressing abnormal myocardial excitation and controlling irregular heart rhythms. In addition to its main Class I activity, cibenzoline exhibits limited Class III (potassium channel blockade) and Class IV (calcium channel blockade) effects[1][7]. Its mechanism of action includes reducing left ventricular pressure gradient (LVPG), mainly through decreased myocardial contractility[3][5]. Unlike some other antiarrhythmics such as disopyramide, cibenzoline has minimal anticholinergic side effects[5][6]. The drug is used for the treatment of tachyarrhythmias—including both ventricular and supraventricular arrhythmias—and has demonstrated efficacy in patients with hypertrophic obstructive cardiomyopathy (HOCM)[2][3][5]. It can be administered orally or intravenously and is typically dosed twice daily due to its elimination half-life of 8–12 hours[1].

Brand names
CibenzolineCibenzoline succinateCIBENZOLINE SUCCINATE TABLETS 100mg "TOWA"
Other names
cifenline
02

Targets

KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)CHRM2 (M2)KCNA5 (Ultra-rapid delayed rectifier potassium channel)CaV (Voltage-gated calcium channel protein complex)SCN5A (Sodium channel protein type 5 subunit alpha)KCNQ1 (Potassium voltage-gated channel subfamily KQT member 1)

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