Esaxerenone

Last updated
Esaxerenone
Esaxerenone.svg
Clinical data
Trade names Minnebro
Other namesCS-3150; XL-550
Routes of
administration 		By mouth
Drug class Antimineralocorticoid
Identifiers
  • 1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C22H21F3N2O4S
Molar mass 466.48 g·mol−1
3D model (JSmol)
  • CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
  • 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 (INN Tooltip 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]

Contents

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]

See also

References

  1. 1 2 3 "Esaxerenone - Daiichi Sankyo - AdisInsight".
  2. 1 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.
  3. 1 2 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. ↑ "Daiichi Sankyo Announces Approval of MINNEBRO(TM) Tablets for the Treatment of Hypertension in Japan". Daiichi Sankyo. January 8, 2019.


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