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ENCORAFENIB Drug Record

  • Summary
  • Interactions
  • Claims
  • ENCORAFENIB chembl:CHEMBL3301612 ApprovedAntineoplastic

    Alternate Names:

    NVP-LGX818
    ENCORAFENIB
    LGX-818
    NVP-LGX818-NXA
    NVP-LGX-818-NXA
    BRAFTOVI
    LGX818
    pubchem.compound:50922675
    drugbank:11718
    chemidplus:1269440-17-6
    chembl:CHEMBL3301612

    Drug Info:

    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) LGX818
    Drug Class RAF Inhibitor
    Drug Class Kinase Inhibitors
    (8 More Sources)

    Publications:

    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Tripathy et al., 2017, Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors., Clin. Cancer Res.
    Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol
    Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
    Koelblinger P et al., 2018, Development of encorafenib for BRAF-mutated advanced melanoma., Curr Opin Oncol
    Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am
    Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
  • ENCORAFENIB   BRAF

    Interaction Score: 1.59

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy Cetuximab + Encorafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345


    Sources:
    TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

  • ENCORAFENIB   ARAF

    Interaction Score: 0.97

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ENCORAFENIB   RAF1

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ENCORAFENIB   MAP2K1

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type resistant
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • ENCORAFENIB   KRAS

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Encorafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27312529 25673644


    Sources:
    JAX-CKB CIViC

  • ENCORAFENIB   PTEN

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GSK2636771 + LGX818
    Indication/Tumor Type melanoma
    Response Type no benefit

    PMIDs:
    26577700


    Sources:
    JAX-CKB

  • ENCORAFENIB   EGFR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Encorafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • ENCORAFENIB   TP53

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy CGM097 + LGX818
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • MyCancerGenome: LGX818

    • Version: 20-Jun-2017

    Alternate Names:
    LGX818 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • CancerCommons: LGX818

    • Version: 25-July-2013

    Alternate Names:
    LGX818 Drug Trade Name
    LGX818 Drug Development Name

    Drug Info:
    Drug Class RAF Inhibitor
    Source Reported Drug Name(s) LGX818
    Pharmaceutical Developer Novartis

    Publications:

  • JAX-CKB: Encorafenib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov

  • JAX-CKB: LGX818

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.

  • CIViC: ENCORAFENIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol

  • TALC: LGX818

    • Version: 12-May-2016

    Alternate Names:
    LGX818 Primary Drug Name
    LGX818 Drug Synonym

    Drug Info:

    Publications:

  • TTD: LGX818

    • Version: 2020.06.01

    Alternate Names:
    D0TK7R TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3301612

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Encorafenib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3301612

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Encorafenib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: encorafenib

    • Version: 18-August-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