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ASTEMIZOLE Drug Record

  • Summary
  • Interactions
  • Claims
  • ASTEMIZOLE chembl:CHEMBL296419

    Alternate Names:

    ASTEMIZOLE
    GNF-PF-2461
    R-43512
    POLLON-EZE
    HISMANAL
    1-(P-FLUOROBENZYL)-2-{[1-(P-METHOXYPHENETHYL)-4-PIPERIDYL]AMINO}BENZIMIDAZOLE
    1-(P-FLUOROBENZYL)-2-({1-[2-(P-METHOXYPHENYL)ETHYL]PIPERID-4-YL}AMINO)BENZIMIDAZOLE
    rxcui:42328
    pubchem.compound:2247
    chemidplus:68844-77-9
    drugbank:00637
    chembl:CHEMBL296419

    Drug Info:

    Year of Approval 1988
    Drug Class anti-allergic agents
    FDA Approval 1988
    Drug Class small molecule
    Drug Indications Anti-Allergic Agents
    (2 More Sources)

    Publications:

    Zhou et al., 1999, Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole., J. Cardiovasc. Electrophysiol.
    Taglialatela et al., 1999, Cardiac ion channels and antihistamines: possible mechanisms of cardiotoxicity., Clin. Exp. Allergy
    Grzelewska-Rzymowska et al., 2001, [The effect of second generation histamine antagonists on the heart]., Pneumonol Alergol Pol
    Chachin et al., 1999, Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel., Eur. J. Pharmacol.
    Chiu et al., 2004, Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels., J. Pharmacol. Sci.
    Perrin MJ et al., 2008, Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels., Mol Pharmacol
    Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
    Aronov AM, 2005, Predictive in silico modeling for hERG channel blockers., Drug Discov Today
    Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
    Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem
    Howarth et al., 1984, Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels., Br J Clin Pharmacol
    Krstenansky et al., 1987, Astemizole: a long-acting, nonsedating antihistamine., Drug Intell Clin Pharm
    Llenas et al., 1999, Cardiotoxicity of histamine and the possible role of histamine in the arrhythmogenesis produced by certain antihistamines., Drug Saf
    Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.
    Kaliner et al., Non-sedating antihistamines., Allergy Proc
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Richards et al., 1984, Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy., Drugs
    Cavero et al., 1999, Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans?, Drug Saf
    Kong X et al., 2014, Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2., J Med Chem
    Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
  • ASTEMIZOLE   EED

    Interaction Score: 9.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25369470


    Sources:
    DTC

  • ASTEMIZOLE   CYP2J2

    Interaction Score: 0.95

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15861034


    Sources:
    PharmGKB

  • ASTEMIZOLE   HPSE

    Interaction Score: 0.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23415087


    Sources:
    DTC

  • ASTEMIZOLE   HRH1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -
    Direct Interaction yes

    PMIDs:
    6146346 2892659 10597866 8001268 3147222 11752352 6204835 10597865


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • ASTEMIZOLE   KCNH2

    Interaction Score: 0.14

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10376921 10444235 11575008 10422790 15272206 18701618 16253929 15718164 14999113


    Sources:
    PharmGKB

  • ASTEMIZOLE   PPARD

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ASTEMIZOLE   ABCB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ASTEMIZOLE   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ASTEMIZOLE   IDH1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ASTEMIZOLE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9187528


    Sources:
    PharmGKB

  • ASTEMIZOLE   GMNN

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ASTEMIZOLE   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ASTEMIZOLE   AR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: ASTEMIZOLE

    • Version: 01-August-2011

    Alternate Names:
    ASTEMIZOLE Primary Drug Name

    Drug Info:
    Drug Class anti-allergic agents
    Year of Approval 1988

    Publications:

  • TdgClinicalTrial: ASTEMIZOLE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Anti-Allergic Agents
    Drug Class small molecule
    FDA Approval 1988

    Publications:

  • DTC: ASTEMIZOLE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL296419 ChEMBL Drug ID

    Drug Info:

    Publications:
    Kong X et al., 2014, Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2., J Med Chem
    Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem

  • PharmGKB: astemizole

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
    Zhou et al., 1999, Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole., J. Cardiovasc. Electrophysiol.
    Perrin MJ et al., 2008, Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels., Mol Pharmacol

  • ChemblDrugs: chembl:CHEMBL296419

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL296419

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21