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MIBEFRADIL Drug Record

  • Summary
  • Interactions
  • Claims
  • MIBEFRADIL chembl:CHEMBL45816

    Alternate Names:

    POSICOR
    MIBEFRADIL
    POSICOR 100
    POSICOR 50
    POSICOR®
    RO-405967-001
    chemidplus:116644-53-2
    drugbank:01388
    pubchem.compound:60663
    rxcui:83213
    chembl:CHEMBL45816

    Drug Info:

    Drug Groups investigational
    Drug Categories agents causing hyperkalemia
    Drug Categories antiarrhythmic agents
    Drug Categories bradycardia-causing agents
    Drug Categories calcium-regulating hormones and agents
    Drug Categories cytochrome p-450 cyp1a2 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a5 inhibitors
    Drug Categories cytochrome p-450 cyp3a5 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a7 inhibitors
    Drug Categories cytochrome p-450 cyp3a7 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 substrates
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories moderate risk qtc-prolonging agents
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories qtc prolonging agents
    Drug Categories vasodilating agents
    (2 More Sources)

    Publications:

    Jiménez et al., 2000, Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels., Neuropharmacology
    Mocanu et al., 1999, Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism., Cardiovasc Drugs Ther
    Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology
    Clozel et al., 1997, Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker., J Hypertens Suppl
    Massie, 1997, Mibefradil: a selective T-type calcium antagonist., Am. J. Cardiol.
    McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.
    Monteil et al., 2000, Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels., J. Biol. Chem.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Moosmang et al., 2006, Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2., Circ. Res.
    Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
    Coste et al., 2007, Pharmacological dissection and distribution of NaN/Nav1.9, T-type Ca2+ currents, and mechanically activated cation currents in different populations of DRG neurons., J. Gen. Physiol.
    Perez-Reyes, 2004, Paradoxical role of T-type calcium channels in coronary smooth muscle., Mol. Interv.
    Cribbs et al., 1998, Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family., Circ. Res.
    Brueggemann et al., 2005, Low voltage-activated calcium channels in vascular smooth muscle: T-type channels and AVP-stimulated calcium spiking., Am. J. Physiol. Heart Circ. Physiol.
    Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos
  • MIBEFRADIL   ANO1

    Interaction Score: 0.79

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MIBEFRADIL   CACNB3

    Interaction Score: 0.79

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CACNB4

    Interaction Score: 0.79

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CACNA1H

    Interaction Score: 0.72

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

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    17190903 14993472 9670923 9481612 15498818 9375939 16899990 15562257


    Sources:
    TTD DrugBank GuideToPharmacology

  • MIBEFRADIL   CACNA1G

    Interaction Score: 0.68

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

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    9481612 10692398 11752352 9375939 16899990 15562257


    Sources:
    DrugBank GuideToPharmacology

  • MIBEFRADIL   CACNB1

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CATSPER2

    Interaction Score: 0.59

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MIBEFRADIL   CATSPER1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MIBEFRADIL   CATSPER3

    Interaction Score: 0.59

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MIBEFRADIL   CATSPER4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MIBEFRADIL   CACNA1I

    Interaction Score: 0.53

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

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Antagonist

    PMIDs:
    9481612 9375939 16899990 15562257


    Sources:
    DrugBank GuideToPharmacology

  • MIBEFRADIL   CACNB2

    Interaction Score: 0.5

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CACNA1F

    Interaction Score: 0.34

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CACNA1D

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   CACNA1C

    Interaction Score: 0.24

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

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Antagonist

    PMIDs:
    10665814 10372226 16306443 16899990


    Sources:
    DrugBank GuideToPharmacology

  • MIBEFRADIL   CACNA1S

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    10665814 10372226 16899990


    Sources:
    DrugBank

  • MIBEFRADIL   THPO

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MIBEFRADIL   MTOR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MIBEFRADIL   MAPK1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MIBEFRADIL   KCNH2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16253929


    Sources:
    PharmGKB

  • MIBEFRADIL   ATXN2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MIBEFRADIL   ATAD5

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MIBEFRADIL   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21447734


    Sources:
    DTC

  • MIBEFRADIL   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB01388

    • Version: 5.1.7

    Alternate Names:
    MIBEFRADIL DrugBank Drug Name
    116644-53-2 CAS Number
    Batenac Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups investigational
    Drug Groups withdrawn

    Publications:
    Jiménez et al., 2000, Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels., Neuropharmacology
    Mocanu et al., 1999, Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism., Cardiovasc Drugs Ther
    Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology

  • DTC: MIBEFRADIL

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL45816 ChEMBL Drug ID

    Drug Info:

    Publications:
    Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

  • PharmGKB: mibefradil

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

  • TTD: Mibefradil

    • Version: 2020.06.01

    Alternate Names:
    D0W8XT TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 53801058

    • Version: 29-September-2020

    Alternate Names:
    MIBEFRADIL GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL45816

    • 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