Drug intelligence / Profile preview

azimilide

Development stage
Phase 3
Lead developer
Procter & Gamble
Modality
Small Molecules
Administration
Oral
01

Overview

Azimilide is an investigational class III antiarrhythmic drug developed to control abnormal heart rhythms, particularly supraventricular and ventricular arrhythmias such as atrial fibrillation, atrial flutter, and paroxysmal supraventricular tachycardia. Its primary mechanism of action is the blockade of both the rapidly activating (I(Kr)) and slowly activating (I(Ks)) components of the delayed rectifier potassium channels in cardiac myocytes. This dual blockade prolongs cardiac repolarization, increases the duration of the action potential, and extends refractory periods in both atrial and ventricular tissue. Azimilide also exhibits weaker inhibitory effects on sodium (I(Na)), calcium (I(CaL)), Na+/Ca2+ exchanger currents, and other potassium currents at higher concentrations. Unlike some other class III antiarrhythmics, it demonstrates minimal reverse use-dependence—its efficacy does not diminish at higher heart rates—and has predictable pharmacokinetics with excellent oral absorption. The drug was developed by Procter & Gamble but has not been approved for use in any country; it reached phase III clinical trials for arrhythmia indications[1][2][4][5][6][7].

Brand names
Stedicor
Other names
azimilide dihydrochloride
02

Targets

KCNQ (Potassium voltage-gated channel subfamily Q (Kv7))CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)NCX1 (Sodium/calcium exchanger 1)SCN5A (Sodium channel protein type 5 subunit alpha)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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