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carbenoxolone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids not used as glucocorticosteroids | 493 | 5697-56-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.15 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.401 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.494 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 107.647 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.260 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.670 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 6.250 | % | High | 1 |
| herg | hERG pIC50 | 4.620 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.750 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.656 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.830 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK,TGFBR1 | 18 | |||
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.754 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 12.531 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 4.660 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.275 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.360 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 11.830 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 53.390 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.350 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 829.851 | uM | High | 1 |
Approvals:
None
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:
| Source | Code | Description |
|---|---|---|
| ATC | A02BX01 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) |
| ATC | A02BX51 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) |
| ATC | A02BX71 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) |
| MeSH PA | D000897 | Anti-Ulcer Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
Related Drugs by ATC class:
A02BX Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Peptic ulcer | indication | 13200003 | DOID:750 |
| Ulcer of esophagus | indication | 30811009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.29 | acidic |
| pKa2 | 5.02 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Enzyme | INHIBITOR | IC50 | 7.08 | CHEMBL | KEGG DRUG | |||
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Enzyme | IC50 | 6.97 | CHEMBL | |||||
| Corticosteroid 11-beta-dehydrogenase isozyme 2 | Enzyme | IC50 | 7.09 | CHEMBL | |||||
| Pannexin-1 | Ion channel | IC50 | 5 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166341 | NUI |
| D01899 | KEGG_DRUG |
| 2017 | RXNORM |
| C0006979 | UMLSCUI |
| CHEBI:41462 | CHEBI |
| CBO | PDB_CHEM_ID |
| CHEMBL499915 | ChEMBL_ID |
| CHEMBL1697717 | ChEMBL_ID |
| D002229 | MESH_DESCRIPTOR_UI |
| DB02329 | DRUGBANK_ID |
| 4151 | IUPHAR_LIGAND_ID |
| 1789 | INN_ID |
| 7421-40-1 | SECONDARY_CAS_RN |
| MM6384NG73 | UNII |
| 636403 | PUBCHEM_CID |
| 387273006 | SNOMEDCT_US |
| 395820002 | SNOMEDCT_US |
| 49617001 | SNOMEDCT_US |
| 003685 | NDDF |
| 003686 | NDDF |
Pharmaceutical products:
None