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PEXIDARTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • PEXIDARTINIB chembl:CHEMBL3813873 ApprovedAntineoplastic

    Alternate Names:

    CML-261
    PEXIDARTINIB
    PLX-3397
    PLX3397

    Drug Info:

    Drug Class Kinase Inhibitors
    Pharmaceutical Developer Plexxicon
    Source Reported Drug Name(s) PLX3397
    Drug Class Kinase Inhibitor
    (3 More Sources)

    Publications:

    Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
    Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov
    Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer
    Kim et al., 2014, Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor., Clin. Cancer Res.
    Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.
    Yan D et al., 2017, Inhibition of colony stimulating factor-1 receptor abrogates microenvironment-mediated therapeutic resistance in gliomas., Oncogene
  • PEXIDARTINIB   CSF1

    Interaction Score: 10.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26222558


    Sources:
    CIViC

  • PEXIDARTINIB   CSF1R

    Interaction Score: 1.93

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Macrophage colony stimulating factor receptor inhibitor
    Direct Interaction yes
    Approval Status Phase I

    PMIDs:
    26222558 25939769 28759044 28716061


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons

  • PEXIDARTINIB   CSF3R

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PEXIDARTINIB   KIT

    Interaction Score: 1.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    24583793 28716061


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CancerCommons TTD

  • PEXIDARTINIB   FLT3

    Interaction Score: 0.97

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Prostate
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant

    PMIDs:
    25847190 28716061


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons TTD

  • PEXIDARTINIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PLX3397 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    25939769


    Sources:
    JAX-CKB

  • MyCancerGenome: PLX3397

    • Version: 20-Jun-2017

    Alternate Names:
    PLX3397 Development Name
    PLX108-01 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • CancerCommons: PLX3397

    • Version: 25-July-2013

    Alternate Names:
    PLX3397 Drug Trade Name
    PLX3397 Drug Development Name

    Drug Info:
    Drug Class Kinase Inhibitor
    Source Reported Drug Name(s) PLX3397
    Pharmaceutical Developer Plexxicon

    Publications:

  • JAX-CKB: PLX3397

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
    Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.
    Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov

  • CIViC: PEXIDARTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.
    Yan D et al., 2017, Inhibition of colony stimulating factor-1 receptor abrogates microenvironment-mediated therapeutic resistance in gliomas., Oncogene
    Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov

  • TTD: PLX-3397

    • Version: 2020.06.01

    Alternate Names:
    D09TAB TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3813873

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3545158

    • Version: chembl_23

    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