1448754-43-5

Usage

Uses

Used in Cardiology:
Eleclazine (hydrochloride) is used as an antiarrhythmic agent for the treatment of patients with certain types of arrhythmias. It helps regulate irregular heartbeats by blocking the ion channels responsible for heart rhythm regulation, thus preventing abnormal heart rhythms.
Used in Pharmaceutical Industry:
Eleclazine (hydrochloride) is utilized in the development of medications for the management of cardiac arrhythmias. Its formulation and dosage are determined by healthcare providers based on individual patient needs, ensuring safe and effective treatment.

Upstream product

• 1443211-72-0 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 
• 49660-57-3 6-bromochroman-4-one 
• 5755-05-5 7-bromo-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 

Relevant academic research and scientific papers

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinical development for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia-ventricular fibrillation (VT-VF). We will describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improved from the first generation late INa inhibitor 1 (ranolazine). Compound 4 was 42 times more potent than 1 in reducing ischemic burden in vivo (S-T segment elevation, 15 min left anteriorior descending, LAD, occlusion in rabbits) with EC50 values of 190 and 8000 nM, respectively. Compound 4 represents a new class of potent late INa inhibitors that will be useful in delineating the role of inhibitors of this current in the treatment of patients.

COMBINATION THERAPIES USING LATE SODIUM ION CHANNEL BLOCKERS AND POTASSIUM ION CHANNEL BLOCKERS

Described herein is a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising administration of an effective amount of one or more of a potassium channel blocker and an effective amount of one or more of a late sodium channel blocker. Also provided are methods for modulating ventricular and atrial rhythm and rate. Also provided are pharmaceutical formulations that are suitable for such combined administration.