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BR1733 is an orally bioavailable small molecule inhibitor targeting the embryonic ectoderm development (EED) protein, a core component of the polycomb repressive complex 2 (PRC2). By binding to EED, BR1733 disrupts PRC2 function and inhibits its histone methyltransferase activity, leading to reduced trimethylation of histone H3 at lysine 27 (H3K27me3), chromatin de-repression, and potential antitumor effects. The drug is being developed primarily for advanced cancers including diffuse large B-cell lymphoma (DLBCL), peripheral T-cell lymphoma (PTCL), refractory follicular lymphoma, and other solid tumors. It is currently in Phase 1/2 clinical trials. BR1733 was initially developed by Shanghai Blueray Biopharma.
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