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canrenone 🐶 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 | 478 | 976-71-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic pregnadiene compound with anti-aldosterone activity.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 25 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.932 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.646 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 65.163 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 31.769 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 4.920 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 10.280 | % | High | 1 |
| herg | hERG pIC50 | 4.717 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.083 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 15.885 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 5.680 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,STK33,TEK | 23 | |||
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.486 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 84.918 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.100 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.714 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 6.280 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 52.360 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 42.800 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 5.730 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 36.475 | uM | High | 1 |
Approvals:
None
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 |
|---|---|---|---|---|---|---|
| Drug interaction | 166.18 | 46.66 | 78 | 1129 | 276375 | 90350865 |
| Hyperkalaemia | 118.73 | 46.66 | 41 | 1166 | 64923 | 90562317 |
| Sopor | 106.16 | 46.66 | 30 | 1177 | 24614 | 90602626 |
| Hyponatraemia | 48.49 | 46.66 | 27 | 1180 | 133511 | 90493729 |
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 |
|---|---|---|---|---|---|---|
| Sopor | 110.42 | 39.10 | 32 | 1204 | 13170 | 42606929 |
| Hyperkalaemia | 79.46 | 39.10 | 41 | 1195 | 80417 | 42539682 |
| Drug interaction | 47.98 | 39.10 | 48 | 1188 | 266951 | 42353148 |
| Varicella virus test positive | 41.28 | 39.10 | 7 | 1229 | 238 | 42619861 |
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 |
|---|---|---|---|---|---|---|
| Sopor | 200.72 | 35.01 | 61 | 2533 | 36485 | 110550220 |
| Hyperkalaemia | 188.75 | 35.01 | 82 | 2512 | 135714 | 110450991 |
| Drug interaction | 185.00 | 35.01 | 125 | 2469 | 500058 | 110086647 |
| Anaemia | 55.47 | 35.01 | 66 | 2528 | 547020 | 110039685 |
| Syncope | 52.37 | 35.01 | 41 | 2553 | 202495 | 110384210 |
| Hyponatraemia | 51.88 | 35.01 | 42 | 2552 | 217611 | 110369094 |
| Acute kidney injury | 50.67 | 35.01 | 68 | 2526 | 635362 | 109951343 |
| Hypotension | 47.88 | 35.01 | 60 | 2534 | 523789 | 110062916 |
| Melaena | 45.24 | 35.01 | 25 | 2569 | 68732 | 110517973 |
| Bradycardia | 43.49 | 35.01 | 33 | 2561 | 155484 | 110431221 |
| Varicella virus test positive | 39.29 | 35.01 | 7 | 2587 | 395 | 110586310 |
| Multiple organ dysfunction syndrome | 37.65 | 35.01 | 30 | 2564 | 151680 | 110435025 |
| Dehydration | 35.52 | 35.01 | 38 | 2556 | 279473 | 110307232 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C03DA03 | CARDIOVASCULAR SYSTEM DIURETICS ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS Aldosterone antagonists |
| MeSH PA | D000451 | Mineralocorticoid Receptor Antagonists |
| MeSH PA | D004232 | Diuretics |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D045283 | Natriuretic Agents |
| 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|
None
🐶 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 | 6.52 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| N0000167426 | NUI |
| D03363 | KEGG_DRUG |
| 1982 | RXNORM |
| C0006882 | UMLSCUI |
| CHEBI:135445 | CHEBI |
| CHEMBL1463345 | ChEMBL_ID |
| DB12221 | DRUGBANK_ID |
| D002192 | MESH_DESCRIPTOR_UI |
| 13789 | PUBCHEM_CID |
| 13963 | IUPHAR_LIGAND_ID |
| 2445 | INN_ID |
| 78O20X9J0U | UNII |
| 96291007 | SNOMEDCT_US |
| 005943 | NDDF |
| 78O20X9J0U | INXIGHT DRUGS |
Pharmaceutical products:
None