Apararenone

Apararenone (INN) (developmental code name MT-3995) is a nonsteroidal antimineralocorticoid which is under development by Mitsubishi Tanabe Pharma for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.[1][2][3] It was also previously being developed for the treatment of hypertension, but development was discontinued for this indication.[1] Apararenone acts as a highly selective antagonist of the mineralocorticoid receptor (Ki < 50 nM), the receptor for aldosterone.[1][2][3] As of 2017, it is in phase II clinical trials.[1]

Apararenone
Clinical data
Other namesMT-3995
Routes of
administration		Oral
Drug classAntimineralocorticoid
Identifiers
IUPAC name
  • N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC17H17FN2O4S
Molar mass364.39 g·mol−1
3D model (JSmol)
SMILES
  • CC1(C(=O)N(C2=C(O1)C=C(C=C2)NS(=O)(=O)C)C3=CC=C(C=C3)F)C
InChI
  • InChI=1S/C17H17FN2O4S/c1-17(2)16(21)20(13-7-4-11(18)5-8-13)14-9-6-12(10-15(14)24-17)19-25(3,22)23/h4-10,19H,1-3H3
  • Key:AZNHWXAFPBYFGH-UHFFFAOYSA-N

See also

References
  1. "Apararenone - Mitsubishi Tanabe Pharma - AdisInsight".
  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. 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.



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