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DOFETILIDE Drug Record

  • Summary
  • Interactions
  • Claims
  • DOFETILIDE chembl:CHEMBL473 Approved

    Alternate Names:

    DOFETILIDE
    TIKOSYN
    UK-68798
    TIKOSYN®
    DOFETILIDA
    BETA-((P-METHANESULFONAMIDOPHENETHYL)METHYLAMINO)METHANESULFONO-P-PHENETIDIDE
    DOFETILIDUM
    rxcui:49247
    pubchem.compound:71329
    chembl:CHEMBL473
    chemidplus:115256-11-6
    drugbank:00204

    Drug Info:

    Drug Class anti-arrhythmia agents
    Year of Approval 1999
    FDA Approval 1999
    Drug Class small molecule
    Drug Indications Anti-Arrhythmia Agents
    (3 More Sources)

    Publications:

    Ficker et al., 1998, Molecular determinants of dofetilide block of HERG K+ channels., Circ. Res.
    Lees-Miller et al., 2000, Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites., Mol. Pharmacol.
    Overholt et al., 2000, HERG-Like potassium current regulates the resting membrane potential in glomus cells of the rabbit carotid body., J. Neurophysiol.
    Kang et al., 2005, Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel., Mol. Pharmacol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Finlayson et al., 2001, [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel?, Eur. J. Pharmacol.
    Finlayson et al., 2001, [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen., Eur. J. Pharmacol.
    Ficker et al., 2001, Molecular determinants of inactivation and dofetilide block in ether a-go-go (EAG) channels and EAG-related K(+) channels., Mol. Pharmacol.
    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
    Sun Z et al., 2004, Role of a KCNH2 polymorphism (R1047 L) in dofetilide-induced Torsades de Pointes., J Mol Cell Cardiol
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Kiehn et al., 1996, Mapping the block of a cloned human inward rectifier potassium channel by dofetilide., Mol. Pharmacol.
    Roukoz et al., 2007, Dofetilide: a new class III antiarrhythmic agent., Expert Rev Cardiovasc Ther
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
  • DOFETILIDE   KCNJ12

    Interaction Score: 16.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    8700146


    Sources:
    TdgClinicalTrial TEND

  • DOFETILIDE   KCNK2

    Interaction Score: 4.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17187453 17016423 17139284


    Sources:
    TdgClinicalTrial TEND

  • DOFETILIDE   CALCA

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DOFETILIDE   ERG

    Interaction Score: 0.27

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction HERG blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DOFETILIDE   KCNH2

    Interaction Score: 0.23

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

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9486667 10648647 10712445 15548764 11752352 11166283 11698075 11723241 14999113 18701618 15522280


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • DOFETILIDE   CYP2C9

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DOFETILIDE   CYP2C19

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DOFETILIDE   CYP1A2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DOFETILIDE   CYP2D6

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DOFETILIDE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DOFETILIDE   AR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: DOFETILIDE

    • Version: 01-August-2011

    Alternate Names:
    DOFETILIDE Primary Drug Name

    Drug Info:
    Year of Approval 1999
    Drug Class anti-arrhythmia agents

    Publications:

  • TdgClinicalTrial: DOFETILIDE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Anti-Arrhythmia Agents
    Drug Class small molecule
    FDA Approval 1999

    Publications:

  • DTC: DOFETILIDE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL473 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

  • PharmGKB: dofetilide

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    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
    Sun Z et al., 2004, Role of a KCNH2 polymorphism (R1047 L) in dofetilide-induced Torsades de Pointes., J Mol Cell Cardiol
    Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med

  • TTD: Dofetilide

    • Version: 2020.06.01

    Alternate Names:
    D0NW3X TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL473

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL473

    • 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