| Iupac name | N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide |
|---|---|
| Routes of administration | Oral |
| Cas number | 945966-46-1 |
| Class | Antimineralocorticoid |
| Pubchem | 24744336 |
| Chemspiderid | 28663572 |
| Unii | 832663U2NB |
| Chembl | 2181929 |
| C | 17 |
| H | 17 |
| F | 1 |
| N | 2 |
| O | 4 |
| S | 1 |
| Smiles | CC1(C(=O)N(C2=C(O1)C=C(C=C2)NS(=O)(=O)C)C3=CC=C(C=C3)F)C |
| Stdinchi | 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 |
| Stdinchikey | AZNHWXAFPBYFGH-UHFFFAOYSA-N |
| Synonyms | MT-3995 |
Apararenone (INN; development code 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]
See also
References
- ^ "Apararenone - Mitsubishi Tanabe Pharma - AdisInsight"
- ^ 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
- ^ 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