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QUIZARTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • QUIZARTINIB chembl:CHEMBL576982 Antineoplastic

    Alternate Names:

    AC010220
    QUIZARTINIB
    AC220
    ASP-2689
    AC-010220
    AC-220
    AC 220
    N-(5-(1,1-DIMETHYLETHYL)ISOXAZOL-3-YL)-N'-(4-(7-(2-(MORPHOLIN-4-YL)ETHOXY)IMIDAZO(2,1-B)BENZOTHIAZOL-2-YL)PHENYL)UREA
    AC 010220
    chemidplus:950769-58-1
    drugbank:12874
    pubchem.compound:24889392
    chembl:CHEMBL576982

    Drug Info:

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

    Publications:

    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood
    Cortes et al., 2013, Phase I study of quizartinib administered daily to patients with relapsed or refractory acute myeloid leukemia irrespective of FMS-like tyrosine kinase 3-internal tandem duplication status., J. Clin. Oncol.
    Cooper et al., 2016, A Phase I Study of Quizartinib Combined with Chemotherapy in Relapsed Childhood Leukemia: A Therapeutic Advances in Childhood Leukemia & Lymphoma (TACL) Study., Clin. Cancer Res.
    Uras et al., 2016, Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6., Blood
    Albers et al., 2013, The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib., Leukemia
    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
    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
    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.
    Zhang et al., 2014, Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies., Clin. Cancer Res.
    Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
    Tornillo et al., 2006, An update on molecular genetics of gastrointestinal stromal tumours., J. Clin. Pathol.
    Cairoli et al., 2006, Prognostic impact of c-KIT mutations in core binding factor leukemias: an Italian retrospective study., Blood
    Nakagomi et al., 2007, Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation., Lab. Invest.
    Gleixner et al., 2007, Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT., Haematologica
    Pan et al., 2007, EXEL-0862, a novel tyrosine kinase inhibitor, induces apoptosis in vitro and ex vivo in human mast cells expressing the KIT D816V mutation., Blood
    Todd et al., 2013, Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells., Pigment Cell Melanoma Res
    Gotlib et al., 2005, Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation., Blood
    Ustun et al., 2009, Chemotherapy and dasatinib induce long-term hematologic and molecular remission in systemic mastocytosis with acute myeloid leukemia with KIT D816V., Leuk. Res.
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
    Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.
    Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
    Kampa-Schittenhelm et al., 2013, Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms., Mol. Cancer
    Taylor et al., 2012, Flt3 inhibitor AC220 is a potent therapy in a mouse model of myeloproliferative disease driven by enhanced wild-type Flt3 signaling., Blood
    Traer et al., 2016, FGF2 from Marrow Microenvironment Promotes Resistance to FLT3 Inhibitors in Acute Myeloid Leukemia., Cancer Res.
  • QUIZARTINIB   FLT3

    Interaction Score: 2.99

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name AC-220
    Novel drug target Established target
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    22504184 23430109 23878140 24002496 26920889 27099147 23392356 17889720 22504185 17047150 17606455 24046014 14604974 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 20733134 24619500 22858906


    Sources:
    MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions DoCM COSMIC CIViC TTD OncoKB

  • QUIZARTINIB   CBL

    Interaction Score: 2.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type bone marrow cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    22990016


    Sources:
    JAX-CKB

  • QUIZARTINIB   KIT

    Interaction Score: 2.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    16731599 16384925 17259998 18024392 16912224 23582185 15972446 23714533 18986703 21689725 19164557 22504184 25157968 24045550 23497317


    Sources:
    JAX-CKB ChemblInteractions DoCM

  • QUIZARTINIB   IDH2

    Interaction Score: 1.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Enasidenib + Quizartinib
    Indication/Tumor Type acute myeloid leukemia
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • QUIZARTINIB   FGF2

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27671675


    Sources:
    CIViC

  • QUIZARTINIB   CSF1R

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Macrophage colony stimulating factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • QUIZARTINIB   RET

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • QUIZARTINIB   PDGFRA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • QUIZARTINIB   PDGFRB

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MyCancerGenome: QUIZARTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    AC220 Development Name
    QUIZARTINIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • TdgClinicalTrial: QUIZARTINIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • JAX-CKB: Quizartinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Cortes et al., 2013, Phase I study of quizartinib administered daily to patients with relapsed or refractory acute myeloid leukemia irrespective of FMS-like tyrosine kinase 3-internal tandem duplication status., J. Clin. Oncol.
    Uras et al., 2016, Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6., Blood
    Cooper et al., 2016, A Phase I Study of Quizartinib Combined with Chemotherapy in Relapsed Childhood Leukemia: A Therapeutic Advances in Childhood Leukemia & Lymphoma (TACL) Study., Clin. Cancer Res.

  • DoCM: QUIZARTINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
    Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
    Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.

  • CIViC: QUIZARTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    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
    Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood

  • TTD: AC220

    • Version: 2020.06.01

    Alternate Names:
    D07KYT TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL576982

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Quizartinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL576982

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Quizartinib

    • Version: 4-Sep-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