gefapixant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
purinoreceptor (P2X) antagonists 5519 1015787-98-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gefapixant
  • gefapixant citrate
  • lyfnua
  • AF-219
  • RO4926219
  • MK-7264
Gefapixant is a selective, non-narcotic P2X3 receptor antagonist being approved for the treatment of refractory chronic cough or unexplained chronic cough.
  • Molecular weight: 353.40
  • Formula: C14H19N5O4S
  • CLOGP: 0.60
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 3
  • TPSA: 156.44
  • ALOGS: -2.85
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 20, 2022 PMDA MSD K.K.

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:

SourceCodeDescription
ATC R05DB29 RESPIRATORY SYSTEM
COUGH AND COLD PREPARATIONS
COUGH SUPPRESSANTS, EXCL. COMBINATIONS WITH EXPECTORANTS
Other cough suppressants

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
P2X purinoceptor 3 Ion channel ANTAGONIST IC50 7.37 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
AF9 PDB_CHEM_ID
CHEMBL3716057 ChEMBL_ID
C000597312 MESH_SUPPLEMENTAL_RECORD_UI
9540 IUPHAR_LIGAND_ID
2310299-91-1 SECONDARY_CAS_RN
DB15097 DRUGBANK_ID
C5139827 UMLSCUI
CHEMBL4594278 ChEMBL_ID
D11349 KEGG_DRUG
10642 INN_ID
24764487 PUBCHEM_CID
6K6L7E3F1L UNII

Pharmaceutical products:

None