Drug intelligence / Profile preview

nifekalant

Development stage
Phase 4
Lead developer
Mitsubishi Tanabe Pharma
Modality
Small Molecules
Administration
Intravenous
01

Overview

Nifekalant is a Class III antiarrhythmic agent primarily used for the acute management of life-threatening ventricular tachyarrhythmias, such as ventricular tachycardia and ventricular fibrillation. Developed by Mitsui Pharmaceuticals in Japan, it functions as a selective blocker of the rapid component of the delayed rectifier potassium current ($I_{Kr}$), which is mediated by the hERG channel. By inhibiting this current, nifekalant prolongs the action potential duration and the effective refractory period in cardiac myocytes without significantly affecting the conduction velocity or possessing significant beta-adrenergic or calcium channel blocking properties. It is typically administered intravenously in emergency or intensive care settings to stabilize heart rhythm and is notable for its relatively pure Class III profile compared to other agents in its class.

Brand names
Shinbit
Other names
nifekalant hydrochloride尼非卡兰
02

Targets

KCNJ2 (Inward rectifier potassium channel Kir2.1)CHRM2 (M2)KCNH2 (Voltage-gated potassium channel subfamily H member 2)KATP channel (ATP-sensitive potassium channel)CHRM3 (M3)

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