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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
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational
    Drug Categories amines
    Drug Categories antineoplastic agents
    Drug Categories cytochrome p-450 cyp2b6 inducers
    Drug Categories cytochrome p-450 cyp2b6 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp2b6 inhibitors
    Drug Categories cytochrome p-450 cyp2b6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c9 inhibitors
    Drug Categories cytochrome p-450 cyp2c9 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a inducers
    Drug Categories cytochrome p-450 cyp3a inhibitors
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (weak)
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a4 substrates
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories hepatotoxic agents
    Drug Categories mate 1 inhibitors
    Drug Categories mate 2 inhibitors
    Drug Categories mate inhibitors
    Drug Categories narrow therapeutic index drugs
    Drug Categories oatp1b1/slco1b1 inhibitors
    Drug Categories oatp1b3 inhibitors
    Drug Categories pyridines
    Drug Categories tyrosine kinase inhibitors
    Drug Categories ugt1a1 inhibitors
    Drug Categories ugt1a4 substrates
    (6 More Sources)

    Publications:

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

    Interaction Score: 4.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26222558


    Sources:
    CIViC

  • PEXIDARTINIB   CSF1R

    Interaction Score: 0.75

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    28716061 25939769 28759044 26222558


    Sources:
    CancerCommons JAX-CKB CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • PEXIDARTINIB   KIT

    Interaction Score: 0.52

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    28716061 24583793


    Sources:
    CancerCommons JAX-CKB TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • PEXIDARTINIB   FLT3

    Interaction Score: 0.45

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    28716061 25847190


    Sources:
    CancerCommons JAX-CKB CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • PEXIDARTINIB   CSF3R

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PEXIDARTINIB   CDK19

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXIDARTINIB   NF1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Drug family Pan-TK inhibitor
    Alteration NF1:del
    Alteration NF1:.

    PMIDs:
    None found


    Sources:
    CGI

  • PEXIDARTINIB   NTRK3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXIDARTINIB   PDGFRB

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    28716061


    Sources:
    DrugBank

  • PEXIDARTINIB   BRAF

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    25939769


    Sources:
    JAX-CKB

  • PEXIDARTINIB   LCK

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXIDARTINIB   FLT1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXIDARTINIB   KDR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • DrugBank: DB12978

    • Version: 5.1.7

    Alternate Names:
    PEXIDARTINIB DrugBank Drug Name
    1029044-16-3 CAS Number
    Turalio Drug Brand

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

    Publications:
    Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer

  • 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:

  • GuideToPharmacology: 252827368

    • Version: 29-September-2020

    Alternate Names:
    PEXIDARTINIB GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3813873

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3545158

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • CGI: PLX3397

    • Version: 27-September-2017

    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