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gefapixant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| purinoreceptor (P2X) antagonists | 5519 | 1015787-98-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Gefapixant is a selective, non-narcotic P2X3 receptor antagonist being approved for the treatment of refractory chronic cough or unexplained chronic cough.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 90 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.842 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 5.346 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 5.035 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.242 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 56.070 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 67.730 | % | High | 1 |
| herg | hERG pIC50 | 4.479 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.393 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.119 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 47.300 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK9,ERBB2,GRK2,ITK,MAP3K21,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC | 17 | |||
| kinase-selectivity-class | MAP3K21,PIK3CD | 2 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.138 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.155 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.624 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 55.790 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.337 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 68.630 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.017 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.168 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 91.100 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 51.900 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 393.550 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 20, 2022 | PMDA | MSD K.K. | |
| Sept. 15, 2023 | EMA | Merck Sharp & Dohme B.V. |
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 | R05DB29 | RESPIRATORY SYSTEM COUGH AND COLD PREPARATIONS COUGH SUPPRESSANTS, EXCL. COMBINATIONS WITH EXPECTORANTS Other cough suppressants |
| CHEBI has role | CHEBI:51177 | antitussive |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:233423 | antifibrotic agent |
Related Drugs by ATC class:
R05DB Other cough suppressants 25 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Refractory chronic cough | indication | 2561000112106 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|
| P2X purinoceptor 3 | Ion channel | ANTAGONIST | IC50 | 7.37 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| CHEBI:755863 | CHEBI |
| AF9 | PDB_CHEM_ID |
| CHEMBL3716057 | ChEMBL_ID |
| C000597312 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9540 | IUPHAR_LIGAND_ID |
| DB15097 | DRUGBANK_ID |
| 1351858009 | SNOMEDCT_US |
| 467511000202104 | SNOMEDCT_US |
| C5139827 | UMLSCUI |
| CHEMBL4594278 | ChEMBL_ID |
| D11349 | KEGG_DRUG |
| 10642 | INN_ID |
| 2310299-91-1 | SECONDARY_CAS_RN |
| 24764487 | PUBCHEM_CID |
| 6K6L7E3F1L | UNII |
Pharmaceutical products:
None