Apararenone information

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]

^ ^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.

[AdisInsight-1] "Apararenone - Mitsubishi Tanabe Pharma - AdisInsight".

[pmid26939027-2] 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.

[pmid26083526-3] 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.

Apararenone information

and 28 Related for: Apararenone information

Apararenone

Benzoxazine

Mineralocorticoid receptor antagonist

Corticosteroid

Spironolactone

Cortisol

Steroid

Fludrocortisone

Progesterone

Amlodipine

Prednisone

Aldosterone

Mometasone

Finerenone

Eplerenone

Tibolone

Esaxerenone

List of steroids

Mineralocorticoid

Glycyrrhizin

Prednisolone

Drospirenone

Dydrogesterone

Nifedipine

Pharmacokinetics of progesterone

Nimodipine

Pharmacodynamics of spironolactone

Felodipine

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