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CABOZANTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • CABOZANTINIB chembl:CHEMBL2105717 ApprovedAntineoplastic

    Alternate Names:

    CABOMETYX
    XL-184 FREE BASE
    XL-184
    CABOZANTINIB
    BMS-907351
    COMETRIQ
    CABOMETYX®
    BMS 907351
    XL 184
    BMS907351
    COMETRIQ®
    XL184
    pubchem.compound:25102847
    chembl:CHEMBL2105717
    rxcui:1363268
    drugbank:08875
    chemidplus:849217-68-1

    Drug Info:

    Drug Categories cytochrome p-450 cyp2c9 substrates
    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    FDA Approval Medullary thyroid cancer, Renal cell carcinoma
    Drug Class Kinase Inhibitors
    Drug Categories amines
    Drug Categories aniline compounds
    Drug Categories cytochrome p-450 cyp2c8 inhibitors
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories kinase inhibitor
    Drug Categories tyrosine kinase inhibitors
    (13 More Sources)

    Publications:

    Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.
    Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.
    Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov
    Renaud et al., 1975, Effects of 5,6-dihydroxytryptamine on tyrosine-hydroxylase activity in central catecholaminergic neurons of the rat., Biochem. Pharmacol.
    Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
    Gautschi et al., 2013, A patient with lung adenocarcinoma and RET fusion treated with vandetanib., J Thorac Oncol
    Bentzien et al., 2013, In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer., Thyroid
    Gautschi et al., 2017, Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry., J. Clin. Oncol.
    Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer
    Drilon et al., 2016, Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial., Lancet Oncol.
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
    Drilon et al., 2016, A Novel Crizotinib-Resistant Solvent-Front Mutation Responsive to Cabozantinib Therapy in a Patient with ROS1-Rearranged Lung Cancer., Clin. Cancer Res.
    Katayama et al., 2015, Cabozantinib overcomes crizotinib resistance in ROS1 fusion-positive cancer., Clin. Cancer Res.
    Chong et al., 2017, Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer., Clin. Cancer Res.
    Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.
    Zhao et al., 2014, Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants., Cancer Sci.
    Cohen et al., 2015, Pharmacological Inhibition of KIT Activates MET Signaling in Gastrointestinal Stromal Tumors., Cancer Res.
    Gebreyohannes et al., 2016, Cabozantinib Is Active against Human Gastrointestinal Stromal Tumor Xenografts Carrying Different KIT Mutations., Mol. Cancer Ther.
    Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
    Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.
    Sameni et al., 2016, Cabozantinib (XL184) Inhibits Growth and Invasion of Preclinical TNBC Models., Clin. Cancer Res.
    Paik et al., 2015, Response to MET inhibitors in patients with stage IV lung adenocarcinomas harboring MET mutations causing exon 14 skipping., Cancer Discov
    Goyal et al., 2017, A phase 2 and biomarker study of cabozantinib in patients with advanced cholangiocarcinoma., Cancer
    Nakatani M et al., 2017, The Anti-tumor Effect of Cabozantinib on Ovarian Clear Cell Carcinoma <i>In Vitro</i> and <i>In Vivo</i>., Anticancer Res
    Li et al., 2017, Acquired MET Y1248H and D1246N Mutations Mediate Resistance to MET Inhibitors in Non-Small Cell Lung Cancer., Clin. Cancer Res.
    Song et al., 2015, Potent antitumor activity of cabozantinib, a c-MET and VEGFR2 inhibitor, in a colorectal cancer patient-derived tumor explant model., Int. J. Cancer
    Daud et al., 2017, Phase II randomised discontinuation trial of the MET/VEGF receptor inhibitor cabozantinib in metastatic melanoma., Br. J. Cancer
  • CABOZANTINIB   RET

    Interaction Score: 1.1

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

    Interaction Info:
    Details of the Assay for Interaction In a biochemical assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    25366691 8007 23533264 17 21606412 23584301 23705946 28447912 27525386 27825636 2015


    Sources:
    MyCancerGenomeClinicalTrial OncoKB FDA PharmGKB JAX-CKB CIViC DrugBank TALC MyCancerGenome GuideToPharmacology CGI

  • CABOZANTINIB   ROS1

    Interaction Score: 0.83

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Clinical Study
    Response Type predicted – sensitive

    PMIDs:
    26673800 25351743 27370605 26372962


    Sources:
    JAX-CKB CIViC CGI

  • CABOZANTINIB   GNA11

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28103611


    Sources:
    CIViC

  • CABOZANTINIB   MET

    Interaction Score: 0.6

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

    Interaction Info:
    Notes
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    27694386 26432786 21606412 25971939 28192597 29061793 21926191 28396313


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial OncoKB JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology CGI

  • CABOZANTINIB   CFLAR

    Interaction Score: 0.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial

  • CABOZANTINIB   KIT

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    24205792 25836719 27777285


    Sources:
    JAX-CKB MyCancerGenome

  • CABOZANTINIB   KDR

    Interaction Score: 0.21

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

    Interaction Info:
    Notes
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    21606412 21926191


    Sources:
    ClearityFoundationClinicalTrial TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology

  • CABOZANTINIB   HGF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Drug family Pan-kinase inhibitor
    Alteration HGF:over

    PMIDs:
    None found


    Sources:
    CGI

  • CABOZANTINIB   HRAS

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type thyroid medullary carcinoma
    Response Type sensitive
    Approval Status Phase III

    PMIDs:
    27525386


    Sources:
    JAX-CKB

  • CABOZANTINIB   TEK

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial

  • CABOZANTINIB   FLT3

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type predicted – sensitive
    Approval Status Preclinical

    PMIDs:
    21926191


    Sources:
    JAX-CKB MyCancerGenome

  • CABOZANTINIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase II
    Response Type unknown

    PMIDs:
    27694386 27825638


    Sources:
    JAX-CKB

  • CABOZANTINIB   KRAS

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type thyroid medullary carcinoma
    Response Type sensitive
    Approval Status Phase III

    PMIDs:
    27525386


    Sources:
    JAX-CKB

  • CABOZANTINIB   ABL1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Drug family Pan-kinase inhibitor
    Alteration ABL1:V299L

    PMIDs:
    None found


    Sources:
    CGI

  • CABOZANTINIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25242168


    Sources:
    CIViC

  • CABOZANTINIB   YES1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB08875

    • Version: 5.1.7

    Alternate Names:
    CABOZANTINIB DrugBank Drug Name
    849217-68-1 CAS Number
    Cabometyx Drug Brand

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

    Publications:
    Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
    Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.

  • MyCancerGenome: CABOZANTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    CABOZANTINIB Generic Name
    COMETRIQ Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Medullary thyroid cancer, Renal cell carcinoma

    Publications:

  • TdgClinicalTrial: CABOZANTINIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • CGI: Cabozantinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.
    Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.
    Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov

  • JAX-CKB: cabozantinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.
    Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
    Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer

  • JAX-CKB: Cabozantinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
    Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.

  • CIViC: CABOZANTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer
    Drilon et al., 2016, Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial., Lancet Oncol.
    Daud et al., 2017, Phase II randomised discontinuation trial of the MET/VEGF receptor inhibitor cabozantinib in metastatic melanoma., Br. J. Cancer

  • TALC: CABOZANTINIB

    • Version: 12-May-2016

    Alternate Names:
    CABOZANTINIB Primary Drug Name
    CABOZANTINIB Drug Generic Name
    COMETRIQ Drug Trade Name

    Drug Info:

    Publications:

  • GuideToPharmacology: 178102511

    • Version: 29-September-2020

    Alternate Names:
    CABOZANTINIB GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • DTC: CABOZANTINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL2105717 ChEMBL Drug ID

    Drug Info:

    Publications:

  • TTD: Cabozantinib

    • Version: 2020.06.01

    Alternate Names:
    D0IQ6P TTD Drug ID

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: CABOZANTINIB

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2105717

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: cabozantinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: CABOZANTINIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Cabozantinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Cabozantinib

    • 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