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REGORAFENIB Drug Record

  • Summary
  • Interactions
  • Claims
  • REGORAFENIB chembl:CHEMBL1946170 ApprovedAntineoplastic

    Alternate Names:

    REGORAFENIB
    BAY-734506 MONOHYDRATE
    STIVARGA
    BAY-73-4506
    BAY-734506
    RÉGORAFÉNIB
    STIVARGA®
    REGORAFENIBUM
    BAY 73-4506
    chemidplus:755037-03-7
    drugbank:08896
    chembl:CHEMBL1946170
    rxcui:1312397
    pubchem.compound:11167602

    Drug Info:

    FDA Approval not approved
    Drug Class small molecule
    Drug Indications antineoplastic agent
    FDA Approval Colorectal cancer, Gastrointestinal stromal tumors
    Drug Class Kinase Inhibitors
    (9 More Sources)

    Publications:

    Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
    Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
    Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
    Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.
    Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus
    Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res
    Tong J et al., 2017 Feb 9, FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation., Oncogene
  • REGORAFENIB   DDR2

    Interaction Score: 0.88

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Discoidin domain-containing receptor 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   FBXW7

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    27399335


    Sources:
    JAX-CKB

  • REGORAFENIB   TEK

    Interaction Score: 0.52

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name regorafenib, BAY 73-4506
    Novel drug target Novel Target
    Notes

    PMIDs:
    None found


    Sources:
    TALC TdgClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   KIT

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type decreased response
    Approval Status Preclinical - Cell culture
    Approval Status Phase II

    PMIDs:
    21170960 27371698 25239608


    Sources:
    TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC MyCancerGenomeClinicalTrial TTD OncoKB

  • REGORAFENIB   RAF1

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serine/threonine-protein kinase RAF inhibitor

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   VHL

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type renal cell carcinoma
    Response Type predicted – sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    21170960


    Sources:
    JAX-CKB

  • REGORAFENIB   ARAF

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • REGORAFENIB   RET

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor
    Direct Interaction yes

    PMIDs:
    21170960


    Sources:
    TALC MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • REGORAFENIB   APC

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27004155


    Sources:
    JAX-CKB

  • REGORAFENIB   MAPK11

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction MAP kinase p38 beta inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   BRAF

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Indication/Tumor Type colorectal cancer

    PMIDs:
    21170960 23629727 25838391


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   FRK

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase FRK inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   NRAS

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    23629727 25838391


    Sources:
    JAX-CKB

  • REGORAFENIB   KDR

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name regorafenib, BAY 73-4506
    Novel drug target Established target
    Indication/Tumor Type colorectal cancer

    PMIDs:
    27004155


    Sources:
    TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • REGORAFENIB   PDGFRA

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Platelet-derived growth factor receptor inhibitor
    Indication/Tumor Type gastrointestinal stromal tumor

    PMIDs:
    25905001


    Sources:
    JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   KRAS

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type breast cancer
    Approval Status Preclinical - Cell line xenograft
    Approval Status Preclinical - Cell culture

    PMIDs:
    21170960 23629727 27004155 25838391


    Sources:
    JAX-CKB MyCancerGenomeClinicalTrial PharmGKB OncoKB

  • REGORAFENIB   EPHA2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • REGORAFENIB   PDGFRB

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Platelet-derived growth factor receptor inhibitor
    Direct Interaction yes
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   FLT1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   FLT4

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   FGFR2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   VEGFA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • REGORAFENIB   FGFR1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • REGORAFENIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    23629727 25838391


    Sources:
    JAX-CKB

  • REGORAFENIB   NTRK1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • REGORAFENIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Regorafenib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    JAX-CKB PharmGKB

  • REGORAFENIB   ABL1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • REGORAFENIB   YES1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: REGORAFENIB

    • Version: 20-Jun-2017

    Alternate Names:
    REGORAFENIB Generic Name
    STIVARGA Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Colorectal cancer, Gastrointestinal stromal tumors

    Publications:

  • TdgClinicalTrial: REGORAFENIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • JAX-CKB: Regorafenib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
    Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

  • CIViC: REGORAFENIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

  • TALC: REGORAFENIB

    • Version: 12-May-2016

    Alternate Names:
    REGORAFENIB Primary Drug Name
    REGORAFENIB Drug Generic Name
    STIVARGA Drug Trade Name

    Drug Info:

    Publications:

  • DTC: REGORAFENIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1946170 ChEMBL Drug ID

    Drug Info:

    Publications:

  • TTD: Regorafenib

    • Version: 2020.06.01

    Alternate Names:
    D09GDD TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1946170

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: REGORAFENIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1946170

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Regorafenib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Regorafenib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: regorafenib

    • Version: 18-August-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