Drug intelligence / Profile preview

bepridil

Development stage
Discontinued
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 It was primarily indicated for chronic stable angina refractory to other agents but has been withdrawn from the US market due to safety concerns[1][2][3][4][5].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

KCNK2 (Potassium channel subfamily K member 2)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)CaV3 (Caveolin-3)SCN5A (Sodium channel protein type 5 subunit alpha)

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