Apararenone References

Apararenone
Clinical data
Other names	MT-3995
Routes of; administration	Oral
Drug class	Antimineralocorticoid
Identifiers
	IUPAC name N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide;
CAS Number	945966-46-1;
PubChem CID	24744336;
ChemSpider	28663572;
UNII	832663U2NB;
ChEMBL	ChEMBL2181929;
Chemical and physical data
Formula	C17H17FN2O4S
Molar mass	364.39 g·mol−1
3D model ( JSmol)	Interactive image;
	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;

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 (K_i < 50 nM), the receptor for aldosterone.^[1]^[2]^[3] As of 2017, it is in phase II clinical trials.^[1]

References

^ ^a ^b ^c ^d "Apararenone - Mitsubishi Tanabe Pharma - 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.

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v t e Mineralocorticoids and antimineralocorticoids ( H02)
Mineralocorticoids	Desoxycortone (desoxycorticosterone) Desoxycortone esters Hydrocortisone (cortisol) Hydrocortisone esters Fludrocortisone Fludrocortisone acetate Methylprednisolone Methylprednisolone esters Prednisolone Prednisolone esters Prednisone Prednisone esters
Antimineralocorticoids	Steroidal: Canrenoate potassium (potassium canrenoate) Canrenone Drospirenone Dydrogesterone Eplerenone Gestodene Medrogestone Progesterone Spironolactone Trimegestone Nonsteroidal: Amlodipine Apararenone^§ Benidipine Esaxerenone^† Felodipine Finerenone Nifedipine Nimodipine Nitrendipine
Synthesis modifiers	Acetoxolone Aminoglutethimide Carbenoxolone Enoxolone Ketoconazole Metyrapone Mitotane Trilostane
^# WHO-EM ^‡ Withdrawn from market Clinical trials: ^† Phase III ^§Never to phase III See also Mineralocorticoid receptor modulators Glucocorticoids and antiglucocorticoids List of corticosteroids

Clinical data

Other names	MT-3995
Routes of administration	Oral
Drug class	Antimineralocorticoid
Identifiers
IUPAC name N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide
CAS Number	945966-46-1
PubChem CID	24744336
ChemSpider	28663572
UNII	832663U2NB
ChEMBL	ChEMBL2181929
Chemical and physical data
Formula	C₁₇H₁₇FN₂O₄S
Molar mass	364.39 g·mol⁻¹
3D model ( JSmol)	Interactive image
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