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CRENOLANIB Drug Record

  • Summary
  • Interactions
  • Claims
  • CRENOLANIB chembl:CHEMBL2105728 Antineoplastic

    Alternate Names:

    ARO 002
    CP-868596
    CP-868,596
    CP 868596
    CRENOLANIB
    ARO-002
    chemidplus:670220-88-9
    chembl:CHEMBL2105728
    pubchem.compound:10366136

    Drug Info:

    Drug Class Kinase Inhibitors
    (5 More Sources)

    Publications:

    Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Zhang et al., 2014, Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies., Clin. Cancer Res.
    Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
    Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
    Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
    Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
    Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
    Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
    Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
    Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
    Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
    Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.
  • CRENOLANIB   PDGFRA

    Interaction Score: 3.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Clinical Status preclinical
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions DoCM CIViC TTD

  • CRENOLANIB   FLT3

    Interaction Score: 1.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive
    Approval Status Phase II

    PMIDs:
    24623852 23430109 22504184 24619500 23878140


    Sources:
    JAX-CKB ChemblInteractions DoCM MyCancerGenomeClinicalTrial OncoKB

  • CRENOLANIB   ALK

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • CRENOLANIB   SRC

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CRENOLANIB   PDGFRB

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CRENOLANIB   MET

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • MyCancerGenome: CRENOLANIB

    • Version: 20-Jun-2017

    Alternate Names:
    CP-868569 Development Name
    CRENOLANIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • JAX-CKB: Crenolanib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.
    Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.

  • DoCM: CRENOLANIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
    Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

  • CIViC: CRENOLANIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.
    Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.

  • TTD: CP-868596

    • Version: 2020.06.01

    Alternate Names:
    D0J1GR TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2105728

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: CRENOLANIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Crenolanib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2105728

    • 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