Esaxerenone

Esaxerenone
Clinical data
Trade names	Minnebro
Other names	CS-3150; XL-550
Routes of; administration	By mouth
Drug class	Antimineralocorticoid
Identifiers
	IUPAC name 1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]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;

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]

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]

References

^ ^a ^b ^c "Esaxerenone - Daiichi Sankyo - AdisInsight".
^ ^a ^b Yang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin Pharmacol. 27: 78–85. doi:10.1016/j.coph.2016.02.005. PMID 26939027.
^ ^a ^b Kolkhof P, Nowack C, Eitner F (2015). "Nonsteroidal antagonists of the mineralocorticoid receptor". Curr. Opin. Nephrol. Hypertens. 24 (5): 417–24. doi:10.1097/MNH.0000000000000147. PMID 26083526. S2CID 22113501.
^ https://www.daiichisankyo.com/media/press_release/detail/index_3212.html#:~:text=Tokyo%2C%20Japan%20(January%208%2C,for%20the%20treatment%20of%20hypertension

External links

Esaxerenone - AdisInsight

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[AdisInsight-1] "Esaxerenone - Daiichi Sankyo - AdisInsight".

[pmid26939027-2] Yang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin Pharmacol. 27: 78–85. doi:10.1016/j.coph.2016.02.005. PMID 26939027.

[pmid26083526-3] Kolkhof P, Nowack C, Eitner F (2015). "Nonsteroidal antagonists of the mineralocorticoid receptor". Curr. Opin. Nephrol. Hypertens. 24 (5): 417–24. doi:10.1097/MNH.0000000000000147. PMID 26083526. S2CID 22113501.

[4] ttps://www.daiichisankyo.com/media/press_release/detail/index_3212.html#:~:text=Tokyo%2C%20Japan%20(January%208%2C,for%20the%20treatment%20of%20hypertension

[1]

[2]

[3]

[4]

Esaxerenone

See also

References

External links

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