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LC53-0110 is an orally bioavailable, small-molecule proteasome inhibitor developed by LG Life Sciences for the treatment of multiple myeloma. It specifically and reversibly targets the chymotrypsin-like proteolytic (β5) subunit of the 20S proteasome. Compared to first- and second-generation proteasome inhibitors like bortezomib and ixazomib, LC53-0110 demonstrates higher specificity for the β5 site and has shown potent activity against multiple myeloma cells, including those resistant to existing FDA-approved therapies. Preclinical studies indicate superior and more sustained tumor proteasome inhibition in xenograft models compared to other inhibitors.
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