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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H22N4O3
Molecular Weight 378.4244
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FINERENONE

SMILES

CCOC1=NC=C(C)C2=C1[C@H](C3=CC=C(C=C3OC)C#N)C(C(N)=O)=C(C)N2

InChI

InChIKey=BTBHLEZXCOBLCY-QGZVFWFLSA-N
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

HIDE SMILES / InChI
Molecular Formula C21H22N4O3
Molecular Weight 378.4244
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

FINERENONE is a potent and selective nonsteroidal mineralocorticoid receptor antagonist. Results in preclinical studies showed that lower doses of FINERENONE were needed to achieve similar cardiorenal protective effects compared to both spironolactone and eplerenone. It is in phase III clinical trials for the treatment of diabetic kidney disease.

Originator

Approval Year

2021
470
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 16.0 nM [IC50]
PubMed

PubMed

TitleDatePubMed
Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases.
2012 Aug
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.
2012 Sep 27
Safety and tolerability of the novel non-steroidal mineralocorticoid receptor antagonist BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease: a randomized, double-blind trial.
2013 Aug
Renin-angiotensin system blockade: Finerenone.
2017 Apr
Patents

Patents

20100136142
1
8436180
1
9051316
1
WO2008104306A2
1

Sample Use Guides

In Vivo Use Guide
10 mg or 20 mg once daily.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Sat Dec 16 05:41:51 GMT 2023
Edited
by admin
on Sat Dec 16 05:41:51 GMT 2023
Record UNII
DE2O63YV8R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FINERENONE
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
finerenone [INN]
Common Name English
1,6-NAPHTHYRIDINE-3-CARBOXAMIDE, 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-1,4-DIHYDRO-2,8-DIMETHYL-, (4S)-
Systematic Name English
BAY 94-8862
Code English
FINERENONE [ORANGE BOOK]
Common Name English
FINERENONE [USAN]
Common Name English
KERENDIA
Brand Name English
FINERENONE [JAN]
Common Name English
Finerenone [WHO-DD]
Common Name English
BAY-94-8862
Code English
(4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
Systematic Name English
Code System Code Type Description
EPA CompTox
DTXSID10146928
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
USAN
BC-45
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
NCI_THESAURUS
C169981
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
CAS
1050477-31-0
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
WIKIPEDIA
Finerenone
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
ChEMBL
CHEMBL2181927
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
SMS_ID
100000169992
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
INN
9634
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
PUBCHEM
60150535
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
FDA UNII
DE2O63YV8R
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
EVMPD
SUB183743
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
RXCUI
2562811
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
DAILYMED
DE2O63YV8R
Created by admin on Sat Dec 16 05:41:51 GMT 2023 , Edited by admin on Sat Dec 16 05:41:51 GMT 2023
PRIMARY
Related Record Type Details
Structure of FINERENONE
EXCRETED UNCHANGED
URINE
MINERALOCORTICOID RECEPTOR
TARGET -> INHIBITOR
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Structure of FINERENONE
EXCRETED UNCHANGED
FECAL
Related Record Type Details
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-8-(HYDROXYMETHYL)-2-METHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
URINE
Structure of 1,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID, 3-(AMINOCARBONYL)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2-METHYL-, (4S)-
METABOLITE -> PARENT
PLASMA
Structure of 1,6-NAPHTHYRIDINE-3-CARBOXAMIDE, 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-8-(HYDROXYMETHYL)-2-METHYL-, (4S)-
METABOLITE -> PARENT
URINE
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-8-(HYDROXYMETHYL)-2-METHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
PLASMA
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
PLASMA
Structure of 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
MINOR
FECAL
Structure of 1,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID, 3-(AMINOCARBONYL)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2-METHYL-, (4S)-
METABOLITE -> PARENT
URINE
Structure of 1,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID, 3-(AMINOCARBONYL)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2-METHYL-, (4S)-
METABOLITE -> PARENT
FECAL
Structure of 1,6-NAPHTHYRIDINE-3-CARBOXAMIDE, 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-8-(HYDROXYMETHYL)-2-METHYL-, (4S)-
METABOLITE -> PARENT
FECAL
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
PLASMA
Structure of 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
MAJOR
PLASMA
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-8-(HYDROXYMETHYL)-2-METHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
FECAL
Structure of (4S)-3-CARBAMOYL-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-2-METHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID
METABOLITE -> PARENT
URINE
Structure of (4S)-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE
METABOLITE -> PARENT
URINE
Structure of 1,6-NAPHTHYRIDINE-3-CARBOXAMIDE, 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-8-(HYDROXYMETHYL)-2-METHYL-, (4S)-
METABOLITE -> PARENT
PLASMA
Structure of (4S)-3-CARBAMOYL-4-(4-CYANO-2-METHOXY-PHENYL)-5-ETHOXY-2,3-DIHYDROXY-2-METHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID
METABOLITE -> PARENT
FECAL
Related Record Type Details
Structure of FINERENONE
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