Esaxerenone

Esaxerenone
Clinical data
Routes of
administration		 Oral
Drug class Antimineralocorticoid
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C22H21F3N2O4S
Molar mass 466.475 g/mol
3D model (JSmol)

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.[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] 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.[1]

See also

References

  1. 1 2 3 http://adisinsight.springer.com/drugs/800021527
  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.



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