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BINIMETINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • BINIMETINIB chembl:CHEMBL3187723 ApprovedAntineoplastic

    Alternate Names:

    BINIMETINIB
    MEKTOVI
    ARRY-438162
    ARRY 438162
    NVP-MEK162
    MEK-162
    ARRY-162
    MEK162
    ARRY 162
    chembl:CHEMBL3187723
    pubchem.compound:10288191
    drugbank:11967
    chemidplus:606143-89-9

    Drug Info:

    Notes allosteric inhibitor
    Drug Class Kinase Inhibitors
    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antiinflammatory agent,DMARD,antineoplastic agent
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational
    Drug Categories antineoplastic agents
    Drug Categories antineoplastic and immunomodulating agents
    Drug Categories cytochrome p-450 cyp1a2 substrates
    Drug Categories cytochrome p-450 cyp2c19 substrates
    Drug Categories cytochrome p-450 substrates
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories map kinase kinase 1, antagonists & inhibitors
    Drug Categories map kinase kinase 2, antagonists & inhibitors
    Drug Categories p-glycoprotein substrates with narrow therapeutic index
    Drug Categories protein kinase inhibitors
    Drug Categories ugt1a1 substrates
    Drug Categories ugt1a1 substrates with narrow therapeutic index
    (13 More Sources)

    Publications:

    Woodfield et al., 2016, Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression., BMC Cancer
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    Ascierto et al., 2013, MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study., Lancet Oncol.
    Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
    Bendell et al., 2017, A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor., Br. J. Cancer
    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
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    Gao Y et al., 2019, V211D Mutation in MEK1 Causes Resistance to MEK Inhibitors in Colon Cancer., Cancer Discov
    Koelblinger P et al., 2017, A review of binimetinib for the treatment of mutant cutaneous melanoma., Future Oncol
    Raja et al., 2015, Assessment of the In Vivo Activity of PI3K and MEK Inhibitors in Genetically Defined Models of Colorectal Cancer., Mol. Cancer Ther.
    Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
    Thumar et al., 2014, MEK targeting in N-RAS mutated metastatic melanoma., Mol. Cancer
    Dummer et al., 2017, Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial., Lancet Oncol.
    Yan J et al., 2018, Analysis of NRAS gain in 657 patients with melanoma and evaluation of its sensitivity to a MEK inhibitor., Eur J Cancer
    Morgan et al., 2001, Cell-cycle-dependent activation of mitogen-activated protein kinase kinase (MEK-1/2) in myeloid leukemia cell lines and induction of growth inhibition and apoptosis by inhibitors of RAS signaling., Blood
    Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
    Vu et al., 2016, Targeting mutant NRAS signaling pathways in melanoma., Pharmacol. Res.
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Kiessling et al., 2016, Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma., PLoS ONE
    Monk BJ et al., 2020, MILO/ENGOT-ov11: Binimetinib Versus Physician's Choice Chemotherapy in Recurrent or Persistent Low-Grade Serous Carcinomas of the Ovary, Fallopian Tube, or Primary Peritoneum., J Clin Oncol
    Hamidi et al., 2014, KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition., Br. J. Cancer
    Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
    Kim et al., 2016, Phosphoproteomics Reveals MAPK Inhibitors Enhance MET- and EGFR-Driven AKT Signaling in KRAS-Mutant Lung Cancer., Mol. Cancer Res.
    Lee et al., 2016, Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models., Oncotarget
    Carita et al., 2016, Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma., Oncotarget
    Chen et al., 2014, Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations., Oncogene
  • BINIMETINIB   MAP2K7

    Interaction Score: 0.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial TTD

  • BINIMETINIB   GNA11

    Interaction Score: 0.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy MEK162 + AEB071
    Indication/Tumor Type uveal melanoma
    Response Type sensitive

    PMIDs:
    24141786 27507190


    Sources:
    JAX-CKB

  • BINIMETINIB   NRAS

    Interaction Score: 0.75

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BYL719 + MEK162
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive

    PMIDs:
    24588908 28284557 27307593 23414587 29245078 28152546 11238126 24569456 26987942 28514312 26821351


    Sources:
    OncoKB JAX-CKB CIViC

  • BINIMETINIB   MAP2K2

    Interaction Score: 0.48

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Novel Target
    Trial Name ARRY-162
    Specific Action of the Ligand Negative

    PMIDs:
    28587477


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial TdgClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • BINIMETINIB   MAP3K1

    Interaction Score: 0.47

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    28587477


    Sources:
    DrugBank

  • BINIMETINIB   MAP2K5

    Interaction Score: 0.43

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • BINIMETINIB   GNAQ

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy MEK162 + AEB071
    Indication/Tumor Type uveal melanoma
    Response Type predicted – sensitive

    PMIDs:
    27507190


    Sources:
    JAX-CKB

  • BINIMETINIB   MAP2K1

    Interaction Score: 0.38

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Negative

    PMIDs:
    31227518


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial TdgClinicalTrial CIViC MyCancerGenome GuideToPharmacology ChemblInteractions

  • BINIMETINIB   MAP2K4

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • BINIMETINIB   MAP2K3

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • BINIMETINIB   NF1

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26925841


    Sources:
    ClearityFoundationBiomarkers CIViC

  • BINIMETINIB   MAP2K6

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • BINIMETINIB   BRAF

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Encorafenib + Binimetinib
    combination therapy Encorafenib + Binimetinib + Cetuximab
    Evidence Type Actionable

    PMIDs:
    27307593 23414587 31566309 28152546 29573941 26577700


    Sources:
    ClearityFoundationBiomarkers OncoKB FDA PharmGKB JAX-CKB CIViC

  • BINIMETINIB   APC

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    Evidence Type Actionable
    Approval Status Preclinical

    PMIDs:
    26206338


    Sources:
    JAX-CKB

  • BINIMETINIB   KRAS

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung adenocarcinoma
    Response Type decreased response
    Approval Status Preclinical - Cell culture

    PMIDs:
    32822286 26206338 28152546 25167228 27556948 27422710 27167191


    Sources:
    ClearityFoundationBiomarkers OncoKB JAX-CKB CIViC

  • BINIMETINIB   HRAS

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type predicted – sensitive
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    26544513


    Sources:
    JAX-CKB CIViC

  • BINIMETINIB   UGT1A1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • BINIMETINIB   ATM

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Clinical Study

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • BINIMETINIB   IL6

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • BINIMETINIB   PTEN

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BYL719 + MEK162
    Indication/Tumor Type melanoma
    Response Type no benefit

    PMIDs:
    26206338 26577700


    Sources:
    JAX-CKB

  • BINIMETINIB   IL1B

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • BINIMETINIB   TNF

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • DrugBank: DB11967

    • Version: 5.1.7

    Alternate Names:
    BINIMETINIB DrugBank Drug Name
    606143-89-9 CAS Number
    Mektovi Drug Brand

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

    Publications:
    Koelblinger P et al., 2017, A review of binimetinib for the treatment of mutant cutaneous melanoma., Future Oncol

  • MyCancerGenome: MEK162

    • Version: 20-Jun-2017

    Alternate Names:
    MEK162 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes allosteric inhibitor

    Publications:

  • TdgClinicalTrial: ARRY-162

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • TTD: ARRY-162

    • Version: 2020.06.01

    Alternate Names:
    D0C4LF TTD Drug ID

    Drug Info:

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

  • JAX-CKB: Binimetinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Raja et al., 2015, Assessment of the In Vivo Activity of PI3K and MEK Inhibitors in Genetically Defined Models of Colorectal Cancer., Mol. Cancer Ther.
    Bendell et al., 2017, A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor., Br. J. Cancer
    Hamidi et al., 2014, KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition., Br. J. Cancer

  • JAX-CKB: MEK162

    • 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.
    Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
    Carita et al., 2016, Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma., Oncotarget

  • CIViC: BINIMETINIB

    • 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
    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
    Thumar et al., 2014, MEK targeting in N-RAS mutated metastatic melanoma., Mol. Cancer

  • TALC: MEK162

    • Version: 12-May-2016

    Alternate Names:
    MEK162 Primary Drug Name
    MEK162 Drug Synonym

    Drug Info:

    Publications:

  • GuideToPharmacology: 249565604

    • Version: 29-September-2020

    Alternate Names:
    BINIMETINIB GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • FDA: Binimetinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3187723

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: MEK162

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3187723

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Binimetinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: MEK162

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: binimetinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: MEK162

    • Version: 30-February-2014

    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 2021-04-13