Esaxerenone

Esaxerenone (INNTooltip International Nonproprietary Name) (brand name Minnebro; developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and developed by Daiichi Sankyo Company and is approved in Japan for the treatment of hypertension.^[1][2][3] 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.^[1][2][3]

Trade namesMinnebro

Other namesCS-3150; XL-550

Routes of
administrationBy mouth

Drug classAntimineralocorticoid

Quick facts Clinical data, Trade names ...

Esaxerenone

Clinical data
Trade names	Minnebro
Other names	CS-3150; XL-550
Routes of administration	By mouth
Drug class	Antimineralocorticoid
Identifiers
IUPAC name (5P)-1-(2-hydroxyethyl)-N-[4-(methanesulfonyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
CAS Number	1632006-28-0
PubChem CID	25052023
ChemSpider	28666733
UNII	N62TGJ04A1
KEGG	D10892
ChEMBL	ChEMBL2181932
CompTox Dashboard (EPA)	DTXSID601336896
Chemical and physical data
Formula	C22H21F3N2O4S
Molar mass	466.48 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
InChI InChI=1S/C22H21F3N2O4S/c1-14-18(21(29)26-15-7-9-16(10-8-15)32(2,30)31)13-27(11-12-28)20(14)17-5-3-4-6-19(17)22(23,24)25/h3-10,13,28H,11-12H2,1-2H3,(H,26,29) Key:NOSNHVJANRODGR-UHFFFAOYSA-N

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Daiichi Sankyo Company, Limited on January 8, 2019 announced the receipt of marketing approval in Japan for MINNEBROTM Tablets 1.25 mg, 2.5 mg and 5 mg (generic name: esaxerenone) for the treatment of hypertension. As of January 2019, esaxerenone is in phase III clinical trials for diabetic nephropathies.^[1][4]