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LESTAURTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • LESTAURTINIB chembl:CHEMBL603469 Antineoplastic

    Alternate Names:

    LESTAURTINIB
    SPM-924
    SP924
    KT-5555
    KT-555
    A-1544750
    CEP-701
    SP-924
    A-154475

    Drug Info:

    Drug Class Kinase Inhibitors
    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    (5 More Sources)

    Publications:

    Vaishnavi et al., 2013, Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer., Nat. Med.
    Jin et al., 2005, The ETV6-NTRK3 chimeric tyrosine kinase suppresses TGF-beta signaling by inactivating the TGF-beta type II receptor., Proc. Natl. Acad. Sci. U.S.A.
    Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.
    Wang et al., 2012, MicroRNAs in liver disease., Gastroenterology
    Piloto et al., 2007, Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways., Blood
    Mathews et al., 2007, Impact of FLT3 mutations and secondary cytogenetic changes on the outcome of patients with newly diagnosed acute promyelocytic leukemia treated with a single agent arsenic trioxide regimen., Haematologica
    Zimmerman et al., 2013, Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia., Blood
    Bagrintseva et al., 2004, Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells., Blood
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Yamamoto et al., 2001, Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies., Blood
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.
    Martelli et al., 2013, Mutational landscape of AML with normal cytogenetics: biological and clinical implications., Blood Rev.
    Allen et al., 2013, The importance of relative mutant level for evaluating impact on outcome of KIT, FLT3 and CBL mutations in core-binding factor acute myeloid leukemia., Leukemia
    Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood
    Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
    Brown et al., 2005, FLT3 inhibition selectively kills childhood acute lymphoblastic leukemia cells with high levels of FLT3 expression., Blood
    Eisenhoffer et al., 2012, Crowding induces live cell extrusion to maintain homeostatic cell numbers in epithelia., Nature
    Clark et al., 2004, Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518., Blood
    Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
    Jourdan et al., 2013, Prospective evaluation of gene mutations and minimal residual disease in patients with core binding factor acute myeloid leukemia., Blood
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Fischer et al., 2010, Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3., J. Clin. Oncol.
    Smith et al., 2004, Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia., Blood
    Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
    Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
  • LESTAURTINIB   FLT3

    Interaction Score: 2.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name lestaurtinib , CEP-701
    Clinical Status case report

    PMIDs:
    17889720 22504185 17047150 17606455 24046014 14604974 23430109 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 22504184 20733134 14726387 22858906


    Sources:
    MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM CIViC TTD

  • LESTAURTINIB   ETV6

    Interaction Score: 1.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    16258068


    Sources:
    JAX-CKB

  • LESTAURTINIB   NTRK1

    Interaction Score: 0.48

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name lestaurtinib , CEP-701
    Mechanism of Interaction Nerve growth factor receptor Trk-A inhibitor

    PMIDs:
    24162815


    Sources:
    TdgClinicalTrial ChemblInteractions CIViC

  • LESTAURTINIB   JAK2

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name lestaurtinib, CEP-701
    Novel drug target Novel Target
    Indication/Tumor Type hematologic cancer

    PMIDs:
    21926964


    Sources:
    TdgClinicalTrial JAX-CKB ChemblInteractions

  • LESTAURTINIB   NTRK3

    Interaction Score: 0.39

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction NT-3 growth factor receptor inhibitor
    Direct Interaction yes
    Novel drug target Novel Target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • LESTAURTINIB   NTRK2

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Neurotrophic tyrosine kinase receptor type 2 inhibitor
    Direct Interaction yes
    Trial Name lestaurtinib , CEP-701

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • LESTAURTINIB   RET

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LESTAURTINIB   MTOR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LESTAURTINIB   HTT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LESTAURTINIB   AR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: LESTAURTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    CEP-701 Development Name
    LESTAURTINIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • TdgClinicalTrial: LESTAURTINIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • JAX-CKB: Lestaurtinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Jin et al., 2005, The ETV6-NTRK3 chimeric tyrosine kinase suppresses TGF-beta signaling by inactivating the TGF-beta type II receptor., Proc. Natl. Acad. Sci. U.S.A.
    Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

  • DoCM: LESTAURTINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.
    Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.
    Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood

  • CIViC: LESTAURTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Smith et al., 2004, Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia., Blood
    Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
    Vaishnavi et al., 2013, Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer., Nat. Med.

  • DTC: LESTAURTINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL603469 ChEMBL Drug ID

    Drug Info:

    Publications:

  • TTD: Lestaurtinib

    • Version: 2020.06.01

    Alternate Names:
    D0V9WF TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL603469

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL603469

    • 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