Esaxerenone (INN) (developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and is now under development by Daiichi Sankyo Company for the treatment of hypertension, essential hypertension, hyperaldosteronism, and diabetic nephropathies. It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone. As of 2017, esaxerenone is in phase III clinical trials for hypertension, essential hypertension, and hyperaldosteronism and is in phase II clinical trials for diabetic nephropathies.
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