Finerenone

File:Finerenone.svg
Systematic (IUPAC) name
(4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
Clinical data
Legal status	Investigational
Routes of administration	Oral
Identifiers
CAS Number	1050477-31-0
ATC code	none
PubChem	CID: 60150535
ChemSpider	28669387
UNII	DE2O63YV8R
KEGG	D10633
ChEMBL	CHEMBL2181927
Synonyms	BAY 94-8862
Chemical data
Formula	C21H22N4O3
Molecular mass	378.42 g/mol
SMILES CCOc1c2c(c(cn1)C)NC(=C([C@H]2c3ccc(cc3OC)C#N)C(=O)N)C
InChI InChI=1S/C21H22N4O3/c1-5-28-21-18-17(14-7-6-13(9-22)8-15(14)27-4)16(20(23)26)12(3)25-19(18)11(2)10-24-21/h6-8,10,17,25H,5H2,1-4H3,(H2,23,26)/t17-/m1/s1 Key:BTBHLEZXCOBLCY-QGZVFWFLSA-N

Finerenone (INN, USAN) (developmental code name BAY-94-8862) is a non-steroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure as of October 2015. It has less relative affinity to other steroid hormone receptors than currently available antimineralocorticoids such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low sex drive.

Pharmacology

Finerenone blocks mineralocorticoid receptors, which makes it a potassium-sparing diuretic.

This table compares inhibitory (blocking) concentrations (IC₅₀, unit: nM) of three antimineralocorticoids. Mineralocorticoid receptor inhibition is responsible for the desired action of the drugs, whereas inhibition of the other receptors potentially leads to side effects. Lower values mean stronger inhibition.

	Spironolactone	Eplerenone	Finerenone
Mineralocorticoid receptor	24	990	18
Glucocorticoid receptor	2400	22,000	>10,000
Androgen receptor	77	21,200	>10,000
Progesterone receptor	740	31,200	>10,000

The above-listed drugs have insignificant affinity for the estrogen receptor.

Chemistry

Unlike currently marketed antimineralocorticoids, finerenone is not a steroid but a dihydropyridine derivative.

Research

The drug is also being investigated in early trials for the treatment of diabetic nephropathy.

See also

• Esaxerenone
• Mapracorat
• AZD5423
• Tanaproget
• Prinaberel