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Esaxerenone is a novel, oral, non-steroidal and highly selective mineralocorticoid receptor (MR) antagonist. It acts by selectively binding to and inhibiting the mineralocorticoid receptor—the nuclear receptor for aldosterone—thereby blocking aldosterone-induced sodium and water retention, potassium excretion, and increased blood pressure[1][3][7]. Esaxerenone demonstrates over 1,000-fold selectivity for the MR compared to other steroid hormone receptors and has higher affinity than existing antimineralocorticoids such as spironolactone or eplerenone[7]. It is approved in Japan for the treatment of hypertension and is under development for diabetic nephropathy[3][5][7]. The drug was discovered by Exelixis and developed by Daiichi Sankyo.
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