epinastine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics 1027 80012-43-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alesion
  • epinastine
  • (+/-)-Epinastine
  • epinastine hydrochloride
  • epinastine HCl
direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell, indicated for the prevention of itching associated with allergic conjunctivitis
  • Molecular weight: 249.32
  • Formula: C16H15N3
  • CLOGP: 2.15
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 41.62
  • ALOGS: -3.18
  • ROTB: 0

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.15 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Oct. 16, 2003 FDA ALLERGAN
Sept. 20, 2019 PMDA Santen Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 170.03 26.77 80 1311 137557 50466176
Platelet count decreased 35.20 26.77 26 1365 100700 50503033
Hepatic function abnormal 33.98 26.77 17 1374 32664 50571069

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 99.03 30.63 43 1293 36896 29536295
Hepatic function abnormal 71.58 30.63 35 1301 39224 29533967

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hepatic function abnormal 92.12 23.12 47 2555 64266 64431864
Platelet count decreased 43.54 23.12 43 2559 167668 64328462
Drug eruption 36.55 23.12 21 2581 36115 64460015
Pyrexia 35.83 23.12 73 2529 558571 63937559
Interstitial lung disease 32.93 23.12 29 2573 97703 64398427
Decreased appetite 27.18 23.12 44 2558 281245 64214885
Neutrophil count decreased 26.18 23.12 23 2579 77173 64418957

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AX24 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
ATC S01GX10 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
FDA MoA N0000000122 Adrenergic Agonists
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175519 Histamine-1 Receptor Inhibitor
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
FDA PE N0000175628 Decreased Histamine Release
FDA EPC N0000175883 Adrenergic Receptor Agonist
CHEBI has role CHEBI:37955 H1 receptor antagonists
CHEBI has role CHEBI:37956 antihistamines
CHEBI has role CHEBI:50857 anti-allergic drugs
CHEBI has role CHEBI:66981 ophthalmology drugs

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

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204
Ocular Itching indication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.94 Basic

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
Histamine H1 receptor GPCR ANTAGONIST Ki 8.90 WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4 WOMBAT-PK
Multidrug resistance protein 1 Transporter WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR WOMBAT-PK
Alpha-1A adrenergic receptor GPCR WOMBAT-PK
Histamine H2 receptor GPCR WOMBAT-PK
Solute carrier family 22 member 2 Transporter IC50 5.37 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.96 CHEMBL
Alpha-2A adrenergic receptor GPCR WOMBAT-PK
Multidrug and toxin extrusion protein 2 Transporter IC50 4.53 CHEMBL
Histamine H1 receptor GPCR IC50 8.80 CHEMBL

External reference:

IDSource
4021466 VUID
N0000148850 NUI
D01713 KEGG_DRUG
108929-04-0 SECONDARY_CAS_RN
4021466 VANDF
C0078442 UMLSCUI
CHEBI:51032 CHEBI
CHEMBL1106 ChEMBL_ID
DB00751 DRUGBANK_ID
CHEMBL1200491 ChEMBL_ID
C053090 MESH_SUPPLEMENTAL_RECORD_UI
3241 PUBCHEM_CID
7176 IUPHAR_LIGAND_ID
5953 INN_ID
Q13WX941EF UNII
236961 RXNORM
17645 MMSL
181234 MMSL
007311 NDDF
007312 NDDF
407068009 SNOMEDCT_US
407069001 SNOMEDCT_US
427671005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Epinastine HUMAN PRESCRIPTION DRUG LABEL 1 17478-911 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 22 sections
Epinastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 51991-836 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 26 sections
EPINASTINE HYDROCHLORIDE Human Prescription Drug Label 1 62756-329 SOLUTION 0.50 mg OPHTHALMIC ANDA 22 sections
EPINASTINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 70069-008 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 20 sections