Apararenone

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;
PubChemCID	24744336;
ChemSpider	28663572;
UNII	832663U2NB;
ChEMBL	ChEMBL2181929;
Chemical and physical data
Formula	C17H17FN2O4S
Molar mass	364.39g·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 nameMT-3995) is anonsteroidal antimineralocorticoidwhich is under development byMitsubishi Tanabe Pharmafor the treatment ofdiabetic nephropathiesandnon-alcoholic steatohepatitis.^[1]^[2]^[3]It was also previously being developed for the treatment ofhypertension,but development was discontinued for this indication.^[1]Apararenone acts as a highlyselective antagonistof themineralocorticoid receptor(K_i< 50 nM), thereceptorforaldosterone.^[1]^[2]^[3]As of 2017, it is inphase II clinical trials.^[1]

References[edit]

^^a ^b ^c ^d"Apararenone - Mitsubishi Tanabe Pharma - AdisInsight".
^^a ^bYang 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 ^bKolkhof 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 Mineralocorticoidsandantimineralocorticoids(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 ^‡Withdrawnfrom market Clinical trials: ^†Phase III ^§Never to phase III See also Mineralocorticoid receptor modulators Glucocorticoids and antiglucocorticoids List of corticosteroids