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TERFENADINE Drug Record

  • Summary
  • Interactions
  • Claims
  • TERFENADINE chembl:CHEMBL17157

    Alternate Names:

    ANTIHISTAMINE
    TERFENOR FTE
    TERFINAX 120
    HISTAFEN 120
    RMI-9918
    TRILUDAN FTE
    TERFENADINE
    TERFINAX 60
    TRILUDAN
    SELDANE
    HISTAFEN
    TERFENOR
    TERFEX
    TRILUDAN®
    TERFENADIN
    TERFENADINA
    TERFENADINUM
    SELDANE®
    TERFÉNADINE
    (RS)-1-(4-TERT-BUTYLPHENYL)-4-{4-[HYDROXY(DIPHENYL)METHYL]PIPERIDIN-1-YL}-BUTAN-1-OL
    drugbank:00342
    chembl:CHEMBL17157
    pubchem.compound:5405
    chemidplus:50679-08-8
    rxcui:42330

    Drug Info:

    Drug Class anti-allergic agents
    Year of Approval 1985
    FDA Approval 1985
    Drug Class small molecule
    Drug Indications Anti-Allergic Agents
    (3 More Sources)

    Publications:

    Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
    Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
    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
    Gessner et al., 2004, Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents., Mol. Pharmacol.
    Testai et al., 2010, Effects of K openers on the QT prolongation induced by HERG-blocking drugs in guinea-pigs., J. Pharm. Pharmacol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Wood-Baker et al., 1995, A double-blind, placebo controlled study of the effect of the specific histamine H1-receptor antagonist, terfenadine, in chronic severe asthma., Br J Clin Pharmacol
    Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.
    Rafferty et al., 1987, Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways., Am. Rev. Respir. Dis.
    Kishimoto et al., 1997, Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine., Res. Commun. Mol. Pathol. Pharmacol.
    Phillips et al., 1989, The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma., Clin. Exp. Allergy
    Crampette et al., 1996, Inhibition of mediator and cytokine release from dispersed nasal polyp cells by terfenadine., Allergy
    Gervasini et al., 2006, The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study., Br J Clin Pharmacol
    Wang et al., 2001, Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein., Drug Metab. Dispos.
    Kim et al., 1999, Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein., Pharm. Res.
    Ohtani et al., 2003, Evaluation of the efficacy of antihistamines using human monocyte-derived dendritic cells stimulated with histamine., J. Am. Acad. Dermatol.
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Yang et al., 1995, Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers., Br. J. Pharmacol.
    Crimi et al., 1990, Influence of antihistamine (astemizole) and anticholinergic drugs (ipratropium bromide) on bronchoconstriction induced by substance P., Ann Allergy
    Amsellem et al., 1996, Antihistamines and production of granulocyte-macrophage colony-stimulating factor and interleukin-8 by human bronchial epithelial cells in vitro: evaluation of the effects of loratadine and cetirizine., Gen. Pharmacol.
  • TERFENADINE   CD86

    Interaction Score: 1.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12894071


    Sources:
    NCI

  • TERFENADINE   CYP2J2

    Interaction Score: 0.88

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    15861034


    Sources:
    PharmGKB

  • TERFENADINE   KCNA5

    Interaction Score: 0.8

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7670728


    Sources:
    NCI

  • TERFENADINE   TAC1

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1696438


    Sources:
    NCI

  • TERFENADINE   HRH1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    7654486 8001268 2879489 9485522 11752352 2569356


    Sources:
    TdgClinicalTrial TEND

  • TERFENADINE   CSF2

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8836342


    Sources:
    NCI

  • TERFENADINE   CXCL8

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8919641


    Sources:
    NCI

  • TERFENADINE   KCNH2

    Interaction Score: 0.12

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

    Interaction Info:

    PMIDs:
    14999113 18701618 16253929 15718164 15102940 20636881 11752352


    Sources:
    DTC PharmGKB

  • TERFENADINE   ABCB1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16842392 11454724 10213372


    Sources:
    NCI PharmGKB

  • TERFENADINE   THPO

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TERFENADINE   MTOR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TERFENADINE   HTT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TERFENADINE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9187528


    Sources:
    PharmGKB

  • TERFENADINE   GMNN

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: TERFENADINE

    • Version: 01-August-2011

    Alternate Names:
    TERFENADINE Primary Drug Name

    Drug Info:
    Year of Approval 1985
    Drug Class anti-allergic agents

    Publications:

  • TdgClinicalTrial: TERFENADINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Anti-Allergic Agents
    Drug Class small molecule
    FDA Approval 1985

    Publications:

  • NCI: ANTIHISTAMINE

    • Version: 14-September-2017

    Alternate Names:
    C29716 NCI drug code

    Drug Info:

    Publications:
    Wang et al., 2001, Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein., Drug Metab. Dispos.
    Gervasini et al., 2006, The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study., Br J Clin Pharmacol
    Amsellem et al., 1996, Antihistamines and production of granulocyte-macrophage colony-stimulating factor and interleukin-8 by human bronchial epithelial cells in vitro: evaluation of the effects of loratadine and cetirizine., Gen. Pharmacol.

  • NCI: TERFENADINE

    • Version: 14-September-2017

    Alternate Names:
    C29494 NCI drug code

    Drug Info:

    Publications:
    Crampette et al., 1996, Inhibition of mediator and cytokine release from dispersed nasal polyp cells by terfenadine., Allergy
    Kim et al., 1999, Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein., Pharm. Res.
    Yang et al., 1995, Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers., Br. J. Pharmacol.

  • PharmGKB: terfenadine

    • 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
    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
    Aronov AM, 2005, Predictive in silico modeling for hERG channel blockers., Drug Discov Today

  • DTC: TERFENADINE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL17157 ChEMBL Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL17157

    • Version: ChEMBL_27

    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