K-201

K-201 (also known as JTV-519) is an experimental small molecule 1,4-benzothiazepine derivative that functions as a multi-channel blocker and a stabilizer of the ryanodine receptor 2 (RyR2). Originally developed by Japan Tobacco, K-201 was designed to treat cardiac conditions by preventing the abnormal leakage of calcium from the sarcoplasmic reticulum, a process often mediated by the dissociation of calstabin2 (FKBP12.6) from the RyR2 complex under stress. By stabilizing this interaction, K-201 exerts potent antiarrhythmic and cardioprotective effects. Additionally, the drug acts as a non-selective inhibitor of sodium, potassium, and L-type calcium channels, contributing to its broad electrophysiological profile. While it demonstrated efficacy in preclinical models of heart failure and atrial fibrillation, its clinical development was largely superseded by more specific RyR2 stabilizers known as Rycals.

Other names

1,4-benzothiazepine derivative4-[3-(4-benzylpiperidin-1-yl)propionyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine