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acetohexamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperglycaemics | 57 | 968-81-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 3.43 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 77.06 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.257 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.198 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 47.973 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.184 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 6.260 | % | High | 1 |
| herg | hERG pIC50 | 4.480 | pIC50 | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 7.610 | % | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.089 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.483 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.690 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PIK3CB,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 34 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,MAPK7,PDK4,STK33,TEK,TTK | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 10.399 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 8.017 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 4.670 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.873 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 4.510 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 5.058 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.180 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.090 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 853.100 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 23, 1964 | FDA | LILLY |
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 | A10BB31 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sulfonylureas |
| MeSH PA | D007004 | Hypoglycemic Agents |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:90415 | insulin secretagogue |
Related Drugs by ATC class:
A10BB Sulfonylureas 12 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.63 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 | Ion channel | BLOCKER | Ki | 4.64 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 4017503 | VUID |
| N0000145888 | NUI |
| D00219 | KEGG_DRUG |
| 173 | RXNORM |
| C0000992 | UMLSCUI |
| CHEBI:28052 | CHEBI |
| TF9 | PDB_CHEM_ID |
| CHEMBL1589 | ChEMBL_ID |
| DB00414 | DRUGBANK_ID |
| D000092 | MESH_DESCRIPTOR_UI |
| 1989 | PUBCHEM_CID |
| 6793 | IUPHAR_LIGAND_ID |
| 1134 | INN_ID |
| QGC8W08I6I | UNII |
| 4123 | MMSL |
| 522 | MMSL |
| 873 | MMSL |
| d00162 | MMSL |
| 4017503 | VANDF |
| 000907 | NDDF |
| 387210001 | SNOMEDCT_US |
| 39064002 | SNOMEDCT_US |
Pharmaceutical products:
None