^
    almost2years
    The discovery and preclinical characterization of the SAM-competitive PRMT5 inhibitor UCT-000445 (AACR 2023)
    UCT-000445 was well tolerated in vivo and using a CD-1 nude mouse model we found that while reticulocyte proliferation (a surrogate marker for bone marrow cytopenias) is abrogated by continuous treatment with UCT-000445, the use of intermittent dosing schedules overcomes this effect, while yielding equivalent efficacy. Our data with UCT-000445 indicate that SAM-competitive PRMT5 inhibitors may represent a novel and compelling therapeutic strategy for the treatment of multiple solid tumors.
    Preclinical
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    MTAP (Methylthioadenosine Phosphorylase) • PRMT5 (Protein Arginine Methyltransferase 5) • FBXO11 (F-Box Protein 11)
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    UCT-000445