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Experimental cancer drugs
Quisinostat
Другие языки:

    Quisinostat

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    Quisinostat
    Quisinostat.svg
    Clinical data
    Other names JNJ-26481585
    ATC code
    • None
    Pharmacokinetic data
    Bioavailability oral
    Identifiers
    • N-Hydroxy-2-[4-({[(1-methyl-1H-indol-3-yl)methyl]amino}methyl)-1-piperidinyl]-5-pyrimidinecarboxamide
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C21H26N6O2
    Molar mass 394.479 g·mol−1
    3D model (JSmol)
    • O=C(NO)c1cnc(nc1)N2CCC(CC2)CNCc4c3ccccc3n(c4)C
    • InChI=1S/C21H26N6O2/c1-26-14-17(18-4-2-3-5-19(18)26)11-22-10-15-6-8-27(9-7-15)21-23-12-16(13-24-21)20(28)25-29/h2-5,12-15,22,29H,6-11H2,1H3,(H,25,28)
    • Key:PAWIYAYFNXQGAP-UHFFFAOYSA-N

    Quisinostat (USAN; development code JNJ-26481585) is an experimental drug candidate for the treatment of cancer. It is a "second generation" histone deacetylase inhibitor with antineoplastic activity. It is highly potent against class I and II HDACs.

    History

    It was developed by Janssen Pharmaceuticals and licensed to NewVac LLC.

    Preclinical studies show that quisinostat amplifies HDAC-repressed expression of E-cadherin, leading to a reversal of epithelial to mesenchymal transition in tumor cells.

    Clinical trials

    Results of a phase I trials in patients with multiple myeloma in combination with bortezomib and dexamethasone were published in 2016.


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