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esaxerenone 🐶 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 | 5490 | 1632006-28-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Esaxerenone is an oral, selective nonsteroidal mineralocorticoid receptor antagonist used for the treatment of hypertension and diabetic nephropathies.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.302 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 8.299 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 40.832 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.090 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 2.610 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 6.090 | % | High | 1 |
| herg | hERG pIC50 | 4.847 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.630 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.013 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 2 | % | High | 1 |
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 33.884 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 35.400 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.204 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.540 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 84.528 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 6.550 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.008 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.776 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 21.520 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.450 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 50.119 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 1, 2021 | PMDA | DAIICHI SANKYO COMPANY, LIMITED |
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 |
|---|---|---|---|---|---|---|
| Compartment syndrome | 115.71 | 68.05 | 17 | 207 | 2895 | 90625328 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Compartment syndrome | 57.07 | 46.76 | 11 | 418 | 5899 | 110582971 |
| Cardiac failure | 47.44 | 46.76 | 20 | 409 | 187606 | 110401264 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertension | indication | 38341003 | DOID:10763 |
| Diabetic nephropathy | indication | 127013003 |
🐶 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)
None
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 | 8.43 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:755615 | CHEBI |
| E6R | PDB_CHEM_ID |
| CHEMBL3545393 | ChEMBL_ID |
| C000607547 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9894 | IUPHAR_LIGAND_ID |
| DB15207 | DRUGBANK_ID |
| C5139864 | UMLSCUI |
| D10892 | KEGG_DRUG |
| 10230 | INN_ID |
| 25052023 | PUBCHEM_CID |
| N62TGJ04A1 | UNII |
Pharmaceutical products:
None