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phenacemide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2114 | 63-98-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Phenacemide (Phenurone) is an older antiepileptic agent. It is capable of relieving patients resistant to other antiepileptics, although its therapeutic effectiveness must be balanced against its toxic effects.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 280.60 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 | 0.745 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.263 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 107.152 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.112 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 70.580 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 80.940 | % | High | 1 |
| herg | hERG pIC50 | 3.511 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.660 | 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) | 79.590 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,MAP3K21,MAPK7,MARK4,NTRK2,PDK1,PDK2,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ULK1 | 33 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,MAP3K21,PDK4,TTK | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.158 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.704 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 83.490 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.722 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 80.330 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 3.750 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 97.350 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 75.080 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 620.869 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 28, 1951 | FDA | ABBVIE |
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 | N03AX07 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
Related Drugs by ATC class:
N03AX Other antiepileptics 18 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Epilepsy | indication | 84757009 | DOID:1826 |
| Epilepsy characterized by intractable complex partial seizures | indication | 442481002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 1 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4018717 | VUID |
| N0000147023 | NUI |
| D00504 | KEGG_DRUG |
| 4018717 | VANDF |
| C0070525 | UMLSCUI |
| CHEBI:8049 | CHEBI |
| CHEMBL918 | ChEMBL_ID |
| DB01121 | DRUGBANK_ID |
| 4753 | PUBCHEM_CID |
| 92 | INN_ID |
| C005396 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7265 | IUPHAR_LIGAND_ID |
| PAI7J52V09 | UNII |
| 204310 | RXNORM |
| 1302 | MMSL |
| 5265 | MMSL |
| d00947 | MMSL |
| 001632 | NDDF |
| 18712002 | SNOMEDCT_US |
| 400358006 | SNOMEDCT_US |
Pharmaceutical products:
None