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Description: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. [PubChem]
Drug Type: Small Molecule; Approved
Pharmacology: Ketotifen is a fast acting non-competitive histamine antagonist. It inhibits the release of mediators from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally).
Mechanism of Action: Ketotifen is a relatively selective, non-competitive histamine antagonist (H1-receptor) and mast cell stabilizer. Ketotifen inhibits the release of mediators from mast cells involved in hypersensitivity reactions. Decreased chemotaxis and activation of eosinophils has also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properties of ketotifen which may contribute to its antiallergic activity and its ability to affect the underlying pathology of asthma include inhibition of the development of airway hyper-reactivity associated with activation of platelets by PAF (Platelet Activating Factor), inhibition of PAF-induced accumulation of eosinophils and platelets in the airways, suppression of the priming of eosinophils by human recombinant cytokines and antagonism of bronchoconstriction due to leukotrienes. Ketotifen inhibits of the release of allergic mediators such as histamine, leukotrienes C4 and D4(SRS-A) and PAF.
Indication: Indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also for the temporary prevention of itching of the eye due to allergic conjunctivitis (ophthalmic).
Half Life: 21 hours (for elimination)
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Data Correlations | 2 studies

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Genes category icon Genes
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PDE7B 100 100
PDE7A 100 100
HRH1 100 100
SEC24D 100 100
SEC24A 90 90
FAS 88 88
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Biogroups category icon Biogroups
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Unknown proteases 100 100
RNA-directed DNA polymerase (revers… 97 97
Protein Export 91 91
Ubiquitin-associated/translation el… 91 91
Parkin Pathway 89 89
Peptidase M12B, propeptide 89 89
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Individual Studies

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    Organization: Department of Computing Science, Univers…

  • Broad Connectivity Map (CMAP 2.0) compound database

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    A reference collection of genome-wide transcriptional expression data from cultured human cells treated with bioactive small molecules that enable the discovery of functional connections between drugs, genes and diseases through the transitory feature of common gene-expression changes.

    Authors: Lamb J

    Organization: Broad Institute Seven Cambridge Center C…
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Associated Researchers

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Thought leaders and organizations working on research involving Ketotifen.

View All Author iconAuthors
  • Takeo Tsujii
  • Takayuki Ohira
  • Shigeru Watanabe
  • Mark B Abelson
  • Eriko Yamamoto
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Vistakon Pharmaceuticals
  • UCB
  • GlaxoSmithKline
  • Bausch & Lomb, Inc.
  • Campus Bio-Medico University
View All Affiliations icon Organizations
  • University of Alexandria
  • Keio University
  • Jordan University of Science and Technology
  • Kyushu Institute of Technology
  • Schepens Eye Research Institute

Clinical Trials | 27 trials

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