retigabine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| gabamimetic agents | 4181 | 150812-12-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
It is a first-in-class anticonvulsant that works by activating KCNQ2/3 channels. In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.90 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 2.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 8.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.20 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 28, 2011 | EMA | ||
| June 10, 2011 | FDA | GLAXOSMITHKLINE |
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 | N03AX21 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| FDA MoA | N0000182728 | Potassium Channel Openers |
| FDA EPC | N0000182729 | Potassium Channel Opener |
| CHEBI has role | CHEBI:35623 | anticonvulsants |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Partial Epilepsy Treatment Adjunct | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.53 | acidic |
| pKa2 | 4.74 | Basic |
| pKa3 | 3.12 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily KQT member 2 | Ion channel | ACTIVATOR | EC50 | 5.60 | IUPHAR | CHEMBL | |||
| Potassium voltage-gated channel subfamily KQT member 3 | Ion channel | ACTIVATOR | EC50 | 6.20 | IUPHAR | CHEMBL | |||
| Potassium voltage-gated channel subfamily KQT member 5 | Ion channel | ACTIVATOR | EC50 | 5 | IUPHAR | CHEMBL | |||
| Potassium voltage-gated channel subfamily KQT member 4 | Ion channel | ACTIVATOR | EC50 | 5.20 | IUPHAR | CHEMBL | |||
| Potassium voltage-gated channel subfamily KQT member 2 | Ion channel | EC50 | 5.89 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4030907 | VUID |
| N0000182972 | NUI |
| D09569 | KEGG_DRUG |
| 4030907 | VANDF |
| C0530684 | UMLSCUI |
| CHEBI:68584 | CHEBI |
| FBX | PDB_CHEM_ID |
| CHEMBL41355 | ChEMBL_ID |
| DB04953 | DRUGBANK_ID |
| C101866 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2601 | IUPHAR_LIGAND_ID |
| 121892 | PUBCHEM_CID |
| 1112990 | RXNORM |
| 184560 | MMSL |
| 27995 | MMSL |
| d07769 | MMSL |
| 013807 | NDDF |
| 699271005 | SNOMEDCT_US |
| 704476003 | SNOMEDCT_US |
| 7545 | INN_ID |
| 12G01I6BBU | UNII |
Pharmaceutical products:
None