Azimilide

The agents from this heterogeneous group have an effect on the repolarization, they prolong the duration of the action potential and the refractory period.

Azimilide dihydrochloride is a chlorophenylfuranyl compound, which slows repolarization of the heart and prolongs the QT interval of the electrocardiogram.

Prolongation of atrial or ventricular repolarization can provide an anti-arrhythmic benefit in patients with heart rhythm disturbances, and this has been the primary interest in the clinical development azimilide.

Most recent clinical trials have investigated the use of azimilide in reducing the frequency and severity of arrhythmias in patients with implanted cardiac pacemakers-defibrillators, where rare pro-arrhythmic events are rescued by the device.

Azimilide binds on the extracellular domain of the hERG channel, this propagates a conformational change and inhibits the current.

The metabolic clearance is mediated through several pathways: F-1292 is the major metabolite of azimilide, it is formed cleavage of the aromethine bond.