finerenone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
aldosterone antagonists, spironolactone derivates 5465 1050477-31-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • finerenone
  • kerendia
  • BAY 94-8862
Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR), which is activated by aldosterone and cortisol and regulates gene transcription. Finerenone blocks MR mediated sodium reabsorption and MR overactivation in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, and blood vessels) tissues. MR overactivation is thought to contribute to fibrosis and inflammation. Finerenone has a high potency and selectivity for the MR and has no relevant affinity for androgen, progesterone, estrogen, and glucocorticoid receptors.
  • Molecular weight: 378.43
  • Formula: C21H22N4O3
  • CLOGP: 4.51
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 110.26
  • ALOGS: -4.03
  • ROTB: 5

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 16, 2022 EMA BAYER AG
July 9, 2021 FDA BAYER HLTHCARE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03DA05 CARDIOVASCULAR SYSTEM
DIURETICS
ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS
Aldosterone antagonists
FDA MoA N0000000139 Mineralocorticoid Receptor Antagonists
FDA EPC N0000193970 Nonsteroidal Mineralocorticoid-Receptor Antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic kidney disease (CKD) associated with type 2 diabetes (T2D) indication 771000119108
Addison's disease contraindication 363732003 DOID:13774
Adrenal insufficiency contraindication 386584007 DOID:10493




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG KERENDIA BAYER HLTHCARE N215341 July 9, 2021 RX TABLET ORAL July 9, 2026 NEW CHEMICAL ENTITY
20MG KERENDIA BAYER HLTHCARE N215341 July 9, 2021 RX TABLET ORAL July 9, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mineralocorticoid receptor Nuclear hormone receptor ANTAGONIST IC50 7.77 DRUG LABEL DRUG LABEL

External reference:

IDSource
DE2O63YV8R UNII
D10633 KEGG_DRUG
C4045511 UMLSCUI
CHEMBL2181927 ChEMBL_ID
60150535 PUBCHEM_CID
DB16165 DRUGBANK_ID
8678 IUPHAR_LIGAND_ID
2562811 RXNORM
348317 MMSL
39693 MMSL
d09772 MMSL
1163346008 SNOMEDCT_US
1163350001 SNOMEDCT_US
4040689 VANDF
018805 NDDF
C576501 MESH_SUPPLEMENTAL_RECORD_UI
9634 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Kerendia HUMAN PRESCRIPTION DRUG LABEL 1 50419-540 TABLET, FILM COATED 10 mg ORAL NDA 28 sections
Kerendia HUMAN PRESCRIPTION DRUG LABEL 1 50419-541 TABLET, FILM COATED 20 mg ORAL NDA 28 sections