amlexanox indications/contra

Stem definitionDrug idCAS RN
antiallergics, tixanox group 182 68302-57-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aphthasol
  • amlexanox
  • amoxanox
  • aphtheal
  • amlenanox
The mechanism of action by which amlexanox accelerates healing of aphthous ulcers is unknown. In vitro studies have demonstrated amlexanox to be a potent inhibitor of the formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils and mononuclear cells.
  • Molecular weight: 298.30
  • Formula: C16H14N2O4
  • CLOGP: 3.07
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 102.51
  • ALOGS: -3.31
  • ROTB: 2

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 17, 1996 FDA ULURU

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC A01AD07 ALIMENTARY TRACT AND METABOLISM
STOMATOLOGICAL PREPARATIONS
STOMATOLOGICAL PREPARATIONS
Other agents for local oral treatment
ATC R03DX01 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
Other systemic drugs for obstructive airway diseases
FDA PE N0000175628 Decreased Histamine Release
MeSH PA D018926 Anti-Allergic Agents
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Aphthous ulcer of mouth indication 426965005 DOID:9663
Stomatitis contraindication 61170000 DOID:9637

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.47 acidic
pKa2 7.04 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Phosphodiesterase 4 Enzyme INHIBITOR CHEMBL CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase INHIBITOR IC50 6 IUPHAR
Serine/threonine-protein kinase TBK1 Kinase INHIBITOR IC50 6 IUPHAR

External reference:

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IDSource
4021055 VUID
N0000148519 NUI
C0103049 UMLSCUI
7113 IUPHAR_LIGAND_ID
D01828 KEGG_DRUG
DB01025 DRUGBANK_ID
2161 PUBCHEM_CID
413507000 SNOMEDCT_US
4021055 VANDF
N0000007450 NDFRT
N0000148519 NDFRT
4179 MMSL
46307 RXNORM
108897008 SNOMEDCT_US
006853 NDDF
CHEMBL1096 ChEMBL_ID
CHEBI:31205 CHEBI
BRL1C2459K UNII
5950 INN_ID
C045742 MESH_SUPPLEMENTAL_RECORD_UI
ANW PDB_CHEM_ID

Pharmaceutical products:

None