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Drug intelligence / Profile preview
bepridil
- Development stage
- Unknown
- Lead developer
- Organon
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Bepridil is a long-acting, non-selective calcium channel blocker with significant anti-anginal activity. It acts as a vasodilator, anti-arrhythmic, and antihypertensive agent. Bepridil inhibits both slow (L-type) calcium and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage-operated and receptor-operated calcium channels. This results in reduced myocardial oxygen consumption, increased coronary blood flow, modest peripheral vasodilation, and weak antihypertensive effects. Bepridil is also classified as a Class 1 anti-arrhythmic drug but has been associated with serious ventricular arrhythmias such as torsades de pointes due to QT interval prolongation. It was primarily indicated for chronic stable angina refractory to other agents but has been withdrawn from the US market due to safety concerns[1][2][3][4][5].
- Brand names
- VascorBepadin
- Other names
- bepridil hydrochlorideN-Benzyl-N-(3-isobutoxy-2-(pyrrolidin-1-yl)propyl)aniline
02
Targets
SCN5A (Sodium channel protein type 5 subunit alpha)CaV3 (Caveolin-3)KCNK2 (Potassium channel subfamily K member 2)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)CaM (Calmodulin)
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