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finerenone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.618 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.262 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 58.345 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.188 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 10.490 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.570 | % | High | 1 |
| herg | hERG pIC50 | 4.802 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.875 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 53.827 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 7.160 | % | High | 1 |
| kinase-safety-class | PDK1,PDK2,PDK4 | 3 | |||
| kinase-selectivity-class | BRAF | 1 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 5.346 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.741 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.572 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 8.480 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 22.182 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 15.700 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.120 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 25.351 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 55.050 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 8.450 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 10.765 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 9, 2021 | FDA | BAYER HLTHCARE | |
| Feb. 16, 2022 | EMA | BAYER AG | |
| 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 | 347.67 | 47.67 | 67 | 704 | 16865 | 90610811 |
| Hyperkalaemia | 262.85 | 47.67 | 68 | 703 | 64896 | 90562780 |
| Urine albumin/creatinine ratio increased | 198.27 | 47.67 | 26 | 745 | 532 | 90627144 |
| Blood potassium increased | 130.02 | 47.67 | 31 | 740 | 20718 | 90606958 |
| Blood creatinine increased | 115.35 | 47.67 | 40 | 731 | 101346 | 90526330 |
| Renal impairment | 52.84 | 47.67 | 23 | 748 | 105398 | 90522278 |
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 | 417.18 | 40.95 | 97 | 1219 | 16254 | 42603765 |
| Hyperkalaemia | 310.09 | 40.95 | 109 | 1207 | 80349 | 42539670 |
| Blood creatinine increased | 280.40 | 40.95 | 110 | 1206 | 109893 | 42510126 |
| Blood potassium increased | 249.58 | 40.95 | 66 | 1250 | 18470 | 42601549 |
| Urine albumin/creatinine ratio increased | 172.92 | 40.95 | 27 | 1289 | 511 | 42619508 |
| Renal impairment | 122.68 | 40.95 | 62 | 1254 | 110166 | 42509853 |
| Urine albumin/creatinine ratio decreased | 44.95 | 40.95 | 6 | 1310 | 34 | 42619985 |
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 | 494.90 | 43.16 | 109 | 1586 | 28847 | 110558757 |
| Hyperkalaemia | 348.23 | 43.16 | 114 | 1581 | 135682 | 110451922 |
| Blood creatinine increased | 285.08 | 43.16 | 106 | 1589 | 182783 | 110404821 |
| Blood potassium increased | 266.64 | 43.16 | 68 | 1627 | 33181 | 110554423 |
| Urine albumin/creatinine ratio increased | 201.96 | 43.16 | 31 | 1664 | 1082 | 110586522 |
| Renal impairment | 160.62 | 43.16 | 71 | 1624 | 188374 | 110399230 |
| Urine albumin/creatinine ratio decreased | 57.64 | 43.16 | 8 | 1687 | 135 | 110587469 |
| Product prescribing issue | 50.35 | 43.16 | 15 | 1680 | 12757 | 110574847 |
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 |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C03DA Aldosterone antagonists 5 drugs
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 | July 9, 2026 | NEW CHEMICAL ENTITY |
| 20MG | KERENDIA | BAYER HLTHCARE | N215341 | July 9, 2021 | RX | TABLET | ORAL | July 9, 2026 | NEW CHEMICAL ENTITY |
| 40MG | KERENDIA | BAYER HLTHCARE | N215341 | July 11, 2025 | RX | TABLET | ORAL | July 9, 2026 | NEW CHEMICAL ENTITY |
| 10MG | KERENDIA | BAYER HLTHCARE | N215341 | July 9, 2021 | RX | TABLET | ORAL | July 11, 2028 | TO REDUCE THE RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE VISITS IN ADULT PATIENTS WITH HEART FAILURE WITH LEFT VENTRICULAR EJECTION FRACTION (LVEF) >= 40% |
| 20MG | KERENDIA | BAYER HLTHCARE | N215341 | July 9, 2021 | RX | TABLET | ORAL | July 11, 2028 | TO REDUCE THE RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE VISITS IN ADULT PATIENTS WITH HEART FAILURE WITH LEFT VENTRICULAR EJECTION FRACTION (LVEF) >= 40% |
| 40MG | KERENDIA | BAYER HLTHCARE | N215341 | July 11, 2025 | RX | TABLET | ORAL | July 11, 2028 | NEW STRENGTH |
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 |
| CHEBI:747008 | CHEBI |
| CHEMBL2181927 | ChEMBL_ID |
| 60150535 | PUBCHEM_CID |
| DB16165 | DRUGBANK_ID |
| 9634 | INN_ID |
| C576501 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8678 | IUPHAR_LIGAND_ID |
| 1163346008 | SNOMEDCT_US |
| 1163350001 | SNOMEDCT_US |
| 4040689 | VANDF |
| 348317 | MMSL |
| 39693 | MMSL |
| d09772 | MMSL |
| 018805 | NDDF |
| 2562811 | RXNORM |
| DE2O63YV8R | INXIGHT DRUGS |
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 | 30 sections |
| Kerendia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-541 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 30 sections |
| Kerendia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-542 | TABLET | 40 mg | ORAL | NDA | 30 sections |