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TOFACITINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • TOFACITINIB chembl:CHEMBL221959 ApprovedImmunotherapy

    Alternate Names:

    CP-690
    550
    CP-690,550 FREE BASE
    CP-690550 FREE BASE
    CP690550
    CP-690-550
    CP- 690 550
    CP 690550
    CP-690,550
    CP-690550
    TASOCITINIB
    CP690,550
    TOFACITINIB
    XELJANZ®
    rxcui:1357536
    chemidplus:477600-75-2
    drugbank:08895
    pubchem.compound:9926791
    chembl:CHEMBL221959

    Drug Info:

    (1 More Sources)

    Publications:

    Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem
    Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science
    Jang WD et al., 2015, Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design., Bioorg Med Chem Lett
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
    Hou S et al., 2014, Novel carbazole inhibits phospho-STAT3 through induction of protein-tyrosine phosphatase PTPN6., J Med Chem
    Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov
    Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood
    Yin et al., 2015, Identification of mutant alleles of JAK3 in pediatric patients with acute lymphoblastic leukemia., Leuk. Lymphoma
    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.
    Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood
  • TOFACITINIB   STAT5A

    Interaction Score: 13.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19053756 14593182


    Sources:
    DTC

  • TOFACITINIB   STAT5B

    Interaction Score: 5.89

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14593182


    Sources:
    DTC

  • TOFACITINIB   PTPN6

    Interaction Score: 4.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24978112


    Sources:
    DTC

  • TOFACITINIB   JAK3

    Interaction Score: 3.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235


    Sources:
    DTC JAX-CKB CIViC TTD

  • TOFACITINIB   TYK2

    Interaction Score: 1.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26231159 10592235


    Sources:
    DTC

  • TOFACITINIB   JAK2

    Interaction Score: 0.43

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26258521 10592235


    Sources:
    DTC

  • TOFACITINIB   YES1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DTC: TOFACITINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL221959 ChEMBL Drug ID

    Drug Info:

    Publications:
    Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science
    Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

  • JAX-CKB: Tofacitinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    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.
    Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov
    Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood

  • CIViC: TOFACITINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

  • TTD: Tofacitinib

    • Version: 2020.06.01

    Alternate Names:
    D0EG1I TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL221959

    • Version: ChEMBL_27

    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