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COBIMETINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • COBIMETINIB chembl:CHEMBL2146883 ApprovedAntineoplastic

    Alternate Names:

    RG-7420
    GDC-0973
    COTELLIC
    COBIMETINIB
    XL-518
    RG-7421
    XL 518
    GDC0973
    XL518
    RG7420
    GDC 0973
    RG 7420
    pubchem.compound:16222096
    chemidplus:934660-93-2
    rxcui:1722365
    chembl:CHEMBL2146883
    drugbank:05239

    Drug Info:

    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    FDA Approval Melanoma (with BRAF V600E or V600K mutation)
    Drug Class Kinase Inhibitor
    Pharmaceutical Developer Exelixis
    Source Reported Drug Name(s) GDC-0973/XL518
    Drug Class MEK Inhibitor
    Notes allosteric inhibitor
    Drug Class Kinase Inhibitors
    (13 More Sources)

    Publications:

    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
    Diamond et al., 2016, Diverse and Targetable Kinase Alterations Drive Histiocytic Neoplasms., Cancer Discov
    Singh et al., 2015, Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cells., J. Exp. Clin. Cancer Res.
    Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol
    Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
    Kirouac et al., 2017, Clinical responses to ERK inhibition in BRAF(V600E)-mutant colorectal cancer predicted using a computational model., NPJ Syst Biol Appl
    McEvoy CR et al., 2019, Profound MEK inhibitor response in a cutaneous melanoma harboring a GOLGA4-RAF1 fusion., J Clin Invest
  • COBIMETINIB   MAP2K7

    Interaction Score: 1.47

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • COBIMETINIB   NF1

    Interaction Score: 1.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers OncoKB

  • COBIMETINIB   MAP2K1

    Interaction Score: 0.97

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Novel drug target Novel Target

    PMIDs:
    26566875 26384788


    Sources:
    TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial OncoKB

  • COBIMETINIB   MAP2K5

    Interaction Score: 0.88

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • COBIMETINIB   MAP2K4

    Interaction Score: 0.74

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • COBIMETINIB   MAP2K3

    Interaction Score: 0.74

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • COBIMETINIB   MAP2K6

    Interaction Score: 0.74

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • COBIMETINIB   RAF1

    Interaction Score: 0.7

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30835257


    Sources:
    CIViC OncoKB

  • COBIMETINIB   ARAF

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    OncoKB

  • COBIMETINIB   MAP2K2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial OncoKB

  • COBIMETINIB   BRAF

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status FDA approved
    Approval Status Phase Ib/II
    combination therapy Atezolizumab + Vemurafenib + Cobimetinib

    PMIDs:
    25037139 27480103 25265494 23934108 22084396 28649441


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB

  • COBIMETINIB   KRAS

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Atezolizumab + Cobimetinib
    Indication/Tumor Type colorectal cancer
    Response Type predicted – sensitive

    PMIDs:
    23934108 22084396


    Sources:
    ClearityFoundationBiomarkers JAX-CKB OncoKB

  • COBIMETINIB   NRAS

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    OncoKB

  • COBIMETINIB   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + cobimetinib
    Indication/Tumor Type colorectal adenocarcinoma
    Response Type sensitive

    PMIDs:
    22084396


    Sources:
    JAX-CKB

  • MyCancerGenome: COBIMETINIB

    • Version: 20-Jun-2017

    Alternate Names:
    COTELLIC Trade Name

    Drug Info:
    Drug Class Kinase Inhibitor
    FDA Approval Melanoma (with BRAF V600E or V600K mutation)

    Publications:

  • CancerCommons: GDC-0973

    • Version: 25-July-2013

    Alternate Names:
    GDC-0973 PubChem Drug Name
    16222096 PubChem Drug ID
    XL518 Drug Trade Name

    Drug Info:
    Drug Class MEK Inhibitor
    Source Reported Drug Name(s) GDC-0973/XL518
    Pharmaceutical Developer Exelixis

    Publications:

  • MyCancerGenome: GDC-0973

    • Version: 20-Jun-2017

    Alternate Names:
    GDC-0973 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes allosteric inhibitor

    Publications:

  • TdgClinicalTrial: GDC-0973

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small molecule
    FDA Approval not approved

    Publications:

  • TTD: RG7420

    • Version: 2020.06.01

    Alternate Names:
    D0O2FN TTD Drug ID

    Drug Info:

    Publications:
    Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

  • JAX-CKB: Cobimetinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.

  • JAX-CKB: cobimetinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.

  • CIViC: COBIMETINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    McEvoy CR et al., 2019, Profound MEK inhibitor response in a cutaneous melanoma harboring a GOLGA4-RAF1 fusion., J Clin Invest
    Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol
    Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol

  • TALC: GDC-0973

    • Version: 12-May-2016

    Alternate Names:
    GDC-0973 Primary Drug Name
    GDC-0973 Drug Synonym
    XL518 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2146883

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2146883

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: cobimetinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Cobimetinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: GDC-0973

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: XL518

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: GDC-0973

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Cobimetinib

    • Version: 23-July-2020

    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