finerenone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| mineralocorticoid receptor (MR, MCR, aldosterone receptor) antagonists | 5465 | 1050477-31-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 16, 2022 | EMA | BAYER AG | |
| July 9, 2021 | FDA | BAYER HLTHCARE | |
| March 28, 2022 | PMDA | Bayer Yakuhin, Ltd. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Glomerular filtration rate decreased | 119.72 | 49.76 | 22 | 155 | 13419 | 63475426 |
| Hyperkalaemia | 74.04 | 49.76 | 19 | 158 | 54184 | 63434661 |
| Blood potassium increased | 53.98 | 49.76 | 12 | 165 | 18297 | 63470548 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Glomerular filtration rate decreased | 130.82 | 59.15 | 26 | 156 | 12935 | 34943814 |
| Blood creatinine increased | 83.53 | 59.15 | 27 | 155 | 94949 | 34861800 |
| Hyperkalaemia | 65.90 | 59.15 | 21 | 161 | 69368 | 34887381 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Glomerular filtration rate decreased | 112.14 | 48.77 | 23 | 216 | 22679 | 79721470 |
| Blood creatinine increased | 64.33 | 48.77 | 22 | 217 | 155035 | 79589114 |
| Blood potassium increased | 52.42 | 48.77 | 13 | 226 | 29262 | 79714887 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 10MG | KERENDIA | BAYER HLTHCARE | N215341 | July 9, 2021 | RX | TABLET | ORAL | Sept. 1, 2025 | INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF FIGARO-DKD STUDY |
| 20MG | KERENDIA | BAYER HLTHCARE | N215341 | July 9, 2021 | RX | TABLET | ORAL | Sept. 1, 2025 | INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF FIGARO-DKD STUDY |
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mineralocorticoid receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 7.77 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| DE2O63YV8R | UNII |
| D10633 | KEGG_DRUG |
| C4045511 | UMLSCUI |
| CHEMBL2181927 | ChEMBL_ID |
| 60150535 | PUBCHEM_CID |
| DB16165 | DRUGBANK_ID |
| 9634 | INN_ID |
| 8678 | IUPHAR_LIGAND_ID |
| 018805 | NDDF |
| 1163346008 | SNOMEDCT_US |
| 1163350001 | SNOMEDCT_US |
| 4040689 | VANDF |
| 2562811 | RXNORM |
| 348317 | MMSL |
| 39693 | MMSL |
| d09772 | MMSL |
| C576501 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Kerendia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-540 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 28 sections |
| 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 |
| Kerendia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-541 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 28 sections |