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RANOLAZINE Drug Record

  • Summary
  • Interactions
  • Claims
  • RANOLAZINE chembl:CHEMBL1404 Approved

    Alternate Names:

    CVT-303
    RANEXA
    RS-43285-003
    RANOLAZINE
    RANEXA®
    N-(2,6-DIMETHYLPHENYL)-2-[4-[2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL]PIPERAZIN-1-YL]ACETAMIDE
    RS-43285
    drugbank:00243
    pubchem.compound:56959
    chembl:CHEMBL1404
    rxcui:35829
    chemidplus:95635-55-5

    Drug Info:

    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antiallergy agent
    Year of Approval 2006
    Drug Class antianginal agents
    Drug Categories acetamides
    Drug Categories antianginal agents
    Drug Categories bsep/abcb11 substrates
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp2d6 substrates
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (weak)
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs that are mainly renally excreted
    Drug Categories mate 1 inhibitors
    Drug Categories mate 2 inhibitors
    Drug Categories mate inhibitors
    Drug Categories moderate risk qtc-prolonging agents
    Drug Categories oct2 inhibitors
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories qtc prolonging agents
    Drug Categories vasodilating agents
    (3 More Sources)

    Publications:

    Rajamani et al., Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine., Channels (Austin)
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Hale et al., 2006, Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit., J. Cardiovasc. Pharmacol. Ther.
    Neshatian L et al., 2015, Ranolazine inhibits voltage-gated mechanosensitive sodium channels in human colon circular smooth muscle cells., Am J Physiol Gastrointest Liver Physiol
    Saad M et al., 2016, Ranolazine in Cardiac Arrhythmia., Clin Cardiol
    Fredj S et al., 2006, Molecular basis of ranolazine block of LQT-3 mutant sodium channels: evidence for site of action., Br J Pharmacol
    Peters CH et al., 2013, Effects of the antianginal drug, ranolazine, on the brain sodium channel Na(V)1.2 and its modulation by extracellular protons., Br J Pharmacol
    Jerling M, 2006, Clinical pharmacokinetics of ranolazine., Clin Pharmacokinet
    Rayner-Hartley E et al., 2016, Ranolazine: A Contemporary Review., J Am Heart Assoc
    Virsolvy A et al., 2015, Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine., Sci Rep
    Zhao G et al., 2011, Antiadrenergic and hemodynamic effects of ranolazine in conscious dogs., J Cardiovasc Pharmacol
    Létienne R et al., 2001, Evidence that ranolazine behaves as a weak beta1- and beta2-adrenoceptor antagonist in the rat [correction of cat] cardiovascular system., Naunyn Schmiedebergs Arch Pharmacol
  • RANOLAZINE   KCNJ12

    Interaction Score: 3.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26459200 26979079


    Sources:
    DrugBank

  • RANOLAZINE   CACNA1C

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26185330 26459200 16520744 23472826


    Sources:
    DrugBank

  • RANOLAZINE   SCN5A

    Interaction Score: 0.25

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

    Interaction Info:
    Trial Name Ranexa
    Novel drug target Established target
    Mechanism of Interaction Sodium channel protein type V alpha subunit blocker

    PMIDs:
    17220471 19077543


    Sources:
    TEND TdgClinicalTrial ChemblInteractions

  • RANOLAZINE   SCN1A

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    16640453 26459200 26979079


    Sources:
    DrugBank

  • RANOLAZINE   SCN9A

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Ranexa
    Novel drug target Established target

    PMIDs:
    19077543 11752352


    Sources:
    TdgClinicalTrial

  • RANOLAZINE   PLG

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RANOLAZINE   ADRB1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    21633249 11330341 26979079


    Sources:
    DrugBank

  • RANOLAZINE   ADRA1A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    26655634 21633249 26979079


    Sources:
    DrugBank

  • RANOLAZINE   SCN4A

    Interaction Score: 0.07

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel protein type IV alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RANOLAZINE   ABCB1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24433361


    Sources:
    PharmGKB

  • RANOLAZINE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9187528


    Sources:
    PharmGKB

  • RANOLAZINE   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DrugBank: DB00243

    • Version: 5.1.7

    Alternate Names:
    95635-55-5 CAS Number
    Ranexa Drug Brand
    CHEMBL1404 ChEMBL ID

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

    Publications:
    Neshatian L et al., 2015, Ranolazine inhibits voltage-gated mechanosensitive sodium channels in human colon circular smooth muscle cells., Am J Physiol Gastrointest Liver Physiol
    Saad M et al., 2016, Ranolazine in Cardiac Arrhythmia., Clin Cardiol
    Fredj S et al., 2006, Molecular basis of ranolazine block of LQT-3 mutant sodium channels: evidence for site of action., Br J Pharmacol

  • TEND: RANOLAZINE

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Drug Class antianginal agents
    Year of Approval 2006

    Publications:

  • TdgClinicalTrial: RANOLAZINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antiallergy agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • PharmGKB: ranolazine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

  • TTD: Ranolazine

    • Version: 2020.06.01

    Alternate Names:
    D03HYQ TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1404

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1404

    • 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