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M201-A is a novel small molecule ryanodine receptor 2 (RyR2) inhibitor developed primarily for the treatment of heart failure, atrial fibrillation (including paroxysmal atrial fibrillation), and chronic kidney disease. It is a 1,4-benzothiazepine-1-oxide derivative that acts by inhibiting diastolic calcium leak through RyR2 channels in cardiac and renal cells. Preclinical studies demonstrated that M201-A improves cardiac lusitropy and natriuresis while enhancing renal function. In clinical trials, intravenous administration of M201-A increased natriuresis, glomerular filtration rate, and creatinine clearance with an acceptable safety profile. The drug has shown potential as an atrial-selective antiarrhythmic agent with minimal risk of ventricular proarrhythmia. Development is led by Aetas Pharma in collaboration with Kitasato University[1][3][4][5][7].
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