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Experimental drugs
Resminostat
Другие языки:

    Resminostat

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    Resminostat
    Resminostat.svg
    Names
    Preferred IUPAC name
    (2E)-3-(1-{4-[(Dimethylamino)methyl]benzene-1-sulfonyl}-1H-pyrrol-3-yl)-N-hydroxyprop-2-enamide
    Other names
    RAS2410; Resminostat 4SC-201
    Identifiers
    3D model (JSmol)
    ChemSpider
    PubChem CID
    UNII
    • InChI=1S/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+
      Key: FECGNJPYVFEKOD-VMPITWQZSA-N
    • InChI=1/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+
      Key: FECGNJPYVFEKOD-VMPITWQZBF
    • CN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(=C2)/C=C/C(=O)NO
    Properties
    C16H19N3O4S
    Molar mass 349.41 g·mol−1
    Density 1.282 g/cm3
    Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

    Resminostat (4SC-201 or RAS2410) is an orally bioavailable inhibitor of histone deacetylases (HDACs), of which inhibitors are antineoplastic agents.

    In 2011, the German drug maker 4SC was granted orphan drug designation for resminostat by the US FDA for the treatment of hepatocellular carcinoma (HCC).

    In 2016 the FDA granted [another?] IND for clinical tests in combination with sorafenib for HCC. 4SC say "In several phase I and phase II trials, resminostat has already demonstrated very good safety and tolerability, alongside promising indications of efficacy."

    Clinical trials

    It has undergone a phase I/II clinical trial for K-ras mutated advanced colorectal carcinoma.

    It has undergone a phase II clinical trial for relapsed or refractory Hodgkin's Lymphoma.

    Mechanism

    Resminostat restrains the phosphorylation of 4E-BP1 and p70S6k, indicating a disturbance with Akt signalling pathway. The treatment of resminostat leads to a drop of Bim and Bax protein level and Bcl-xL level.

    As with other HDAC inhibitors such as pracinostat, the inhibition of HDACs by resminostat results in an accumulation of highly acetylated histones, followed by an abduction of chromatin remodeling, inhibition of tumor suppressor genes transcription and cell division, and finally tumor cell apoptosis.



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