alcaftadine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
histamine-H1 receptor antagonists, tricyclic compounds 4165 147084-10-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • R 89674
  • alcaftadine
  • lastacaft
Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
  • Molecular weight: 307.40
  • Formula: C19H21N3O
  • CLOGP: 2.45
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 38.13
  • ALOGS: -2.97
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 28, 2010 FDA ALLERGAN

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
Ocular hyperaemia 575.79 122.89 82 75 3974 2353954
Eye irritation 303.27 122.89 47 110 3465 2354463
Eye pruritus 173.32 122.89 28 129 2503 2355425
Scleral hyperaemia 137.92 122.89 16 141 106 2357822
Eye swelling 124.79 122.89 23 134 4367 2353561

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
Ocular hyperaemia 130.16 122.22 19 29 1991 1744742

Pharmacologic Action:

SourceCodeDescription
ATC S01GX11 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:37955 H1-receptor antagonist
CHEBI has role CHEBI:50857 anti-allergic agent
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175587 Histamine-1 Receptor Antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.27 Basic
pKa2 2.99 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.25% LASTACAFT ALLERGAN N022134 July 28, 2010 RX SOLUTION/DROPS OPHTHALMIC 8664215 Dec. 23, 2027 METHOD FOR PREVENTING ITCHING ASSOCIATED WITH ALLERGIC CONJUNCTIVITIS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST CHEMBL CHEMBL

External reference:

IDSource
4030132 VUID
N0000181719 NUI
C2348241 UMLSCUI
D06552 KEGG_DRUG
447209009 SNOMEDCT_US
27322 MMSL
4030132 VANDF
447208001 SNOMEDCT_US
013612 NDDF
1000082 RXNORM
7Z8O94ECSX UNII
8707 INN_ID
C557708 MESH_SUPPLEMENTAL_RECORD_UI
DB06766 DRUGBANK_ID
CHEBI:71023 CHEBI
7587 IUPHAR_LIGAND_ID
CHEMBL1201747 ChEMBL_ID
19371515 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LASTACAFT HUMAN PRESCRIPTION DRUG LABEL 1 0023-4290 SOLUTION/ DROPS 2.50 mg OPHTHALMIC NDA 15 sections
LASTACAFT HUMAN PRESCRIPTION DRUG LABEL 1 42254-288 SOLUTION/ DROPS 2.50 mg OPHTHALMIC NDA 14 sections
LASTACAFT HUMAN PRESCRIPTION DRUG LABEL 1 54868-6294 SOLUTION/ DROPS 2.50 mg OPHTHALMIC NDA 14 sections