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mirogabalin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| gabamimetic agents | 5491 | 1138245-13-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Mirogabalin, a novel ligand for the alpha2delta subunit of voltage-gated calcium channels, has been approved for the treatment of peripheral neuropathic pain including painful diabetic peripheral neuropathy (DPNP) and postherpetic neuralgia (PHN) in Japan. Mirogabalin showed potent and selective binding affinities for the alpha2delta subunits, and slower dissociation rates for the alpha2delta-1 subunit than for the alpha2delta-2 subunit. It also showed potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for the central nervous system side effects. A pharmacological study using mutant mice demonstrated that the analgesic effects of mirogabalin were mediated by binding of the drug to the alpha2delta-1 subunit, not the alpha2delta-2 subunit.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 25 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 | 37 | |||
| kinase-selectivity-class | AXL,BRAF,CHUK,EIF2AK3,EPHB4,MAP2K6,TEK | 7 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 1, 2019 | PMDA | DAIICHI SANKYO COMPANY, LIMITED |
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 | N02BF03 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Gabapentinoids |
Related Drugs by ATC class:
N02BF Gabapentinoids 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postherpetic neuralgia | indication | 2177002 | |
| Peripheral neuropathic pain | indication | 279981003 | |
| Diabetic peripheral neuropathy | indication | 424736006 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-dependent calcium channel subunit alpha-2/delta-1 | Ion channel | MODULATOR | Kd | 7.87 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Voltage-dependent calcium channel subunit alpha-2/delta-2 | Ion channel | MODULATOR | Kd | 7.64 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| CHEBI:755472 | CHEBI |
| 8X9 | PDB_CHEM_ID |
| CHEMBL3545257 | ChEMBL_ID |
| CHEMBL3545125 | ChEMBL_ID |
| C000598618 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8303 | IUPHAR_LIGAND_ID |
| DB11825 | DRUGBANK_ID |
| C4043827 | UMLSCUI |
| D10790 | KEGG_DRUG |
| 9767 | INN_ID |
| 59509752 | PUBCHEM_CID |
| S7LK2KDM5U | UNII |
Pharmaceutical products:
None