The best magazine
Novel Therapeutic Targets in the Management of Atrial Fibrillation
Atrial-selective Agents
An important limitation of multichannel blockers for the treatment of AF is the risk of ventricular arrhythmias. This limitation has necessitated the development of ''atrialselective'' agents with a promising efficacy and a better safety profile. Blockage of IKACh and IKur has been considered to be a promising atrial-selective approach for the management of AF. AVE-0118 is a potent inhibitor of IKACh and prolongs the ERP, which contributes to its efficacy in suppressing AF. Since IKACh is constitutively expressed in AF and also tends to be atrial selective, AVE-0118 offers the benefit of being a selective target drug without affecting ventricular depolarization. XEN D 0101 is another ''atrial-selective'' agent which increases the APD by its inhibition of Kv 1.5 and IKur. Both these agents are in phase I of their development.
Recently, there has been a renewed interest in the role of ranolazine as an antiarrhythmic agent for AF suppression. Ranolazine, although a multichannel blocker, has also been shown to be a potent inhibitor of the activity of INa in the atrial myocytes. The clinical efficacy of ranolazine as a primary agent as well as in combination with dronedarone for treatment of paroxysmal AF is being investigated in the HARMONY (a study to evaluate the effect of ranolazine and dronaderone when given alone and in combination in patients with paroxysmal atrial fibrillation) trial.
Source: ...