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RUXOLITINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • RUXOLITINIB chembl:CHEMBL1789941 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    JAKAVI
    INCB018424
    INC-424
    INCB-18424
    INC424
    INCB-018424
    RUXOLITINIB
    INCB424
    JAKAFI®
    JAKAVI®
    INCB 18424
    (R)-RUXOLITINIB
    chembl:CHEMBL1789941
    drugbank:08877
    pubchem.compound:25126798
    chemidplus:941678-49-5
    rxcui:1193326

    Drug Info:

    FDA Approval Myelofibrosis
    Drug Class Kinase Inhibitors
    (7 More Sources)

    Publications:

    Mazzacurati et al., 2015, The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells., Oncotarget
    Hornakova et al., 2011, Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors., Haematologica
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
    Weigert et al., 2012, Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition., J. Exp. Med.
    Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood
    Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
    Dusa et al., 2010, JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors., PLoS ONE
    Bercovich et al., 2008, Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome., Lancet
    Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., 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
    Mullighan et al., 2009, JAK mutations in high-risk childhood acute lymphoblastic leukemia., Proc. Natl. Acad. Sci. U.S.A.
    Kilpivaara et al., 2009, A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms., Nat. Genet.
    Kiladjian et al., 2006, High molecular response rate of polycythemia vera patients treated with pegylated interferon alpha-2a., Blood
    Ismael et al., 2012, De novo childhood myelodysplastic/myeloproliferative disease with unique molecular characteristics., Br. J. Haematol.
    Paschka et al., 2013, Secondary genetic lesions in acute myeloid leukemia with inv(16) or t(16;16): a study of the German-Austrian AML Study Group (AMLSG)., Blood
    Wernig et al., 2008, Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera., Cancer Cell
    Nagao et al., 2014, Proliferation and survival signaling from both Jak2-V617F and Lyn involving GSK3 and mTOR/p70S6K/4EBP1 in PVTL-1 cell line newly established from acute myeloid leukemia transformed from polycythemia vera., PLoS ONE
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Rumi et al., 2014, Clinical effect of driver mutations of JAK2, CALR, or MPL in primary myelofibrosis., Blood
    Yoshiki et al., 2011, A case of myeloid sarcoma with correlation to JAK2V617F mutation, complicated by myelofibrosis and secondary acute myeloid leukemia., Intern. Med.
    Novotny-Diermayr et al., 2012, The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML., Blood Cancer J
    Wang et al., 2010, AML1 is overexpressed in patients with myeloproliferative neoplasms and mediates JAK2V617F-independent overexpression of NF-E2., Blood
    Levine et al., 2005, The JAK2V617F activating mutation occurs in chronic myelomonocytic leukemia and acute myeloid leukemia, but not in acute lymphoblastic leukemia or chronic lymphocytic leukemia., Blood
    Malak et al., Long term follow up of 93 families with myeloproliferative neoplasms: life expectancy and implications of JAK2V617F in the occurrence of complications., Blood Cells Mol. Dis.
    Jekarl et al., 2010, JAK2 V617F mutation in myelodysplastic syndrome, myelodysplastic syndrome/myeloproliferative neoplasm, unclassifiable, refractory anemia with ring sideroblasts with thrombocytosis, and acute myeloid leukemia., Korean J Hematol
    Campbell et al., 2006, V617F mutation in JAK2 is associated with poorer survival in idiopathic myelofibrosis., Blood
    Baxter et al., Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders., Lancet
    Eghtedar et al., 2012, Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia., Blood
    Roug et al., 2011, A patient with a 20-year lag phase between JAK2-V617F+ myeloproliferation and NPM1-mutated AML arguing against a common origin of disease., Eur. J. Haematol.
    Passamonti et al., 2010, A prospective study of 338 patients with polycythemia vera: the impact of JAK2 (V617F) allele burden and leukocytosis on fibrotic or leukemic disease transformation and vascular complications., Leukemia
    Yang et al., 2012, Ruxolitinib: in the treatment of myelofibrosis., Drugs
    Cervantes et al., 2013, Myelofibrosis: an update on current pharmacotherapy and future directions., Expert Opin Pharmacother
    Lierman et al., 2012, Ruxolitinib inhibits transforming JAK2 fusion proteins in vitro and induces complete cytogenetic remission in t(8;9)(p22;p24)/PCM1-JAK2-positive chronic eosinophilic leukemia., Blood
    Chase et al., 2013, Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements., Haematologica
    Ding YY et al., 2018, Clinical efficacy of ruxolitinib and chemotherapy in a child with Philadelphia chromosome-like acute lymphoblastic leukemia with <i>GOLGA5-JAK2</i> fusion and induction failure., Haematologica
    Yang et al., 2016, Activating JAK1 mutation may predict the sensitivity of JAK-STAT inhibition in hepatocellular carcinoma., Oncotarget
    Newton Y et al., 2018, Comparative RNA-Sequencing Analysis Benefits a Pediatric Patient With Relapsed Cancer., JCO Precis Oncol
    Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.
    Maxson et al., 2016, The Colony-Stimulating Factor 3 Receptor T640N Mutation Is Oncogenic, Sensitive to JAK Inhibition, and Mimics T618I., Clin. Cancer Res.
    Dao KH et al., 2014, Significant clinical response to JAK1/2 inhibition in a patient with CSF3R-T618I-positive atypical chronic myeloid leukemia., Leuk Res Rep
    Fleischman et al., 2013, The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition., Blood
    2013, Genomic and epigenomic landscapes of adult de novo acute myeloid leukemia., N. Engl. J. Med.
    Maxson et al., 2013, Oncogenic CSF3R mutations in chronic neutrophilic leukemia and atypical CML., N. Engl. J. Med.
    Zhou et al., 2016, Clinical Improvement with JAK2 Inhibition in Chuvash Polycythemia., N. Engl. J. Med.
  • RUXOLITINIB   CRLF2

    Interaction Score: 13.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22955920


    Sources:
    CIViC

  • RUXOLITINIB   CSF3R

    Interaction Score: 7.85

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26475333 25180155 24081659 23634996 23656643


    Sources:
    JAX-CKB DoCM CIViC

  • RUXOLITINIB   JAK2

    Interaction Score: 4.99

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type hematologic cancer
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    26472029 21393331 24251790 21926964 22271575 24398328 25207766 26258521 20585391 18805579 22955920 22368270 19470474 19287384 16709929 22571758 23115274 18394554 24404189 25157968 24986690 22041374 22829971 20339092 16081687 22818858 21120162 16293597 15781101 22422826 21689158 20631743 23061804 23514013 22899477 22875628 29773603


    Sources:
    DTC MyCancerGenome JAX-CKB DoCM CIViC MyCancerGenomeClinicalTrial TTD OncoKB

  • RUXOLITINIB   JAK1

    Interaction Score: 3.43

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    22955920 18805579 23061804 23514013 26701727 31372595


    Sources:
    MyCancerGenome DoCM CIViC TTD

  • RUXOLITINIB   PLAUR

    Interaction Score: 2.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RUXOLITINIB   MPL

    Interaction Score: 1.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ruxolitinib + TGX-221
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • RUXOLITINIB   VHL

    Interaction Score: 0.92

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27518686


    Sources:
    CIViC

  • RUXOLITINIB   JAK3

    Interaction Score: 0.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Indication/Tumor Type Advanced Solid Tumor
    Response Type decreased response

    PMIDs:
    26258521 26446793


    Sources:
    DTC JAX-CKB

  • RUXOLITINIB   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • MyCancerGenome: RUXOLITINIB

    • Version: 20-Jun-2017

    Alternate Names:
    INCB18424 Development Name
    RUXOLITINIB Generic Name
    JAKAFI Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Myelofibrosis

    Publications:

  • DTC: RUXOLITINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1789941 ChEMBL Drug ID

    Drug Info:

    Publications:
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

  • JAX-CKB: Ruxolitinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Maxson et al., 2016, The Colony-Stimulating Factor 3 Receptor T640N Mutation Is Oncogenic, Sensitive to JAK Inhibition, and Mimics T618I., Clin. Cancer Res.
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood

  • DoCM: RUXOLITINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood
    2013, Genomic and epigenomic landscapes of adult de novo acute myeloid leukemia., N. Engl. J. Med.
    Maxson et al., 2013, Oncogenic CSF3R mutations in chronic neutrophilic leukemia and atypical CML., N. Engl. J. Med.

  • CIViC: RUXOLITINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Zhou et al., 2016, Clinical Improvement with JAK2 Inhibition in Chuvash Polycythemia., N. Engl. J. Med.
    Dao KH et al., 2014, Significant clinical response to JAK1/2 inhibition in a patient with CSF3R-T618I-positive atypical chronic myeloid leukemia., Leuk Res Rep
    Fleischman et al., 2013, The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition., Blood

  • TTD: Ruxolitinib

    • Version: 2020.06.01

    Alternate Names:
    D04LKS TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1789941

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: INCB018424

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Ruxolitinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: RUXOLITINIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: ruxolitinib

    • Version: 18-August-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