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LUMACAFTOR Drug Record

  • Summary
  • Interactions
  • Claims
  • LUMACAFTOR chembl:CHEMBL2103870 Approved

    Alternate Names:

    VRT-826809
    VX 809
    VX-809
    VRT 826809
    LUMACAFTOR
    3-(6-{[1-(2,2-DIFLUORO-2H-1,3-BENZODIOXOL-5-YL)CYCLOPROPANE-1-CARBONYL]AMINO}-3-METHYLPYRIDIN-2-YL)BENZOIC ACID
    chembl:CHEMBL2103870
    rxcui:1655922
    drugbank:09280
    pubchem.compound:16678941
    chemidplus:936727-05-8

    Drug Info:

    FDA Approval not approved
    Drug Class small molecule
    Drug Indications for treatment of cystic fibrosis
    (3 More Sources)

    Publications:

    Hubert D et al., 2017, Real-life initiation of lumacaftor/ivacaftor combination in adults with cystic fibrosis homozygous for the Phe508del CFTR mutation and severe lung disease., J Cyst Fibros
    Dekkers JF et al., 2016, Characterizing responses to CFTR-modulating drugs using rectal organoids derived from subjects with cystic fibrosis., Sci Transl Med
    Veit G et al., 2016, From CFTR biology toward combinatorial pharmacotherapy: expanded classification of cystic fibrosis mutations., Mol Biol Cell
    Awatade NT et al., 2014, Measurements of Functional Responses in Human Primary Lung Cells as a Basis for Personalized Therapy for Cystic Fibrosis., EBioMedicine
    Yu et al., 2012, Ivacaftor potentiation of multiple CFTR channels with gating mutations., J. Cyst. Fibros.
    Van Goor F et al., 2011, Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809., Proc Natl Acad Sci U S A
    Clancy JP et al., 2012, Results of a phase IIa study of VX-809, an investigational CFTR corrector compound, in subjects with cystic fibrosis homozygous for the F508del-CFTR mutation., Thorax
    Boyle MP et al., 2014, A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial., Lancet Respir Med
    Kopeikin Z et al., 2014, Combined effects of VX-770 and VX-809 on several functional abnormalities of F508del-CFTR channels., J Cyst Fibros
    Ikpa PT et al., 2014, Cystic fibrosis: toward personalized therapies., Int J Biochem Cell Biol
    Norman P, 2014, Novel picolinamide-based cystic fibrosis transmembrane regulator modulators: evaluation of WO2013038373, WO2013038376, WO2013038381, WO2013038386 and WO2013038390., Expert Opin Ther Pat
    Compain P et al., 2013, Rescue of functional CFTR channels in cystic fibrosis: a dramatic multivalent effect using iminosugar cluster-based correctors., Chembiochem
    Van Goor F et al., 2014, Effect of ivacaftor on CFTR forms with missense mutations associated with defects in protein processing or function., J Cyst Fibros
    Lubamba B et al., 2012, Cystic fibrosis: insight into CFTR pathophysiology and pharmacotherapy., Clin Biochem
    Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem
    Kuk et al., 2015, Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects., Ther Adv Respir Dis
  • LUMACAFTOR   CFTR

    Interaction Score: 85.02

    Interaction Types & Directionality:
    modulator

    Interaction Info:
    Trial Name VX-809
    Novel drug target Established target
    Trial Name VX-809 + VX-770

    PMIDs:
    28325531 27334259 26823392 26137539 22293084 21976485 21825083 24973281 24796242 24561283 24392786 24038832 23891399 22698459 26041577 26416827


    Sources:
    DTC TdgClinicalTrial ChemblInteractions PharmGKB TTD FDA

  • TdgClinicalTrial: VX-809

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications for treatment of cystic fibrosis
    Drug Class small molecule
    FDA Approval not approved

    Publications:

  • DTC: LUMACAFTOR

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL2103870 ChEMBL Drug ID

    Drug Info:

    Publications:
    Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem

  • PharmGKB: lumacaftor

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Lubamba B et al., 2012, Cystic fibrosis: insight into CFTR pathophysiology and pharmacotherapy., Clin Biochem
    Ikpa PT et al., 2014, Cystic fibrosis: toward personalized therapies., Int J Biochem Cell Biol
    Awatade NT et al., 2014, Measurements of Functional Responses in Human Primary Lung Cells as a Basis for Personalized Therapy for Cystic Fibrosis., EBioMedicine

  • TTD: Lumacaftor

    • Version: 2020.06.01

    Alternate Names:
    D0X0CB TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2103870

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2103870

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Lumacaftor

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

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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