rinzimetostat

Rinzimetostat (formerly ORIC-944) is an orally bioavailable, potent, and selective allosteric small molecule inhibitor of the Embryonic Ectoderm Development (EED) subunit of the Polycomb Repressive Complex 2 (PRC2). By binding to the H3K27me3-binding pocket of EED, rinzimetostat induces a conformational change that inhibits the methyltransferase activity of both EZH2 and EZH1 subunits. This epigenetic modulation aims to reverse PRC2-mediated gene silencing, which is a key driver in various malignancies. Developed by ORIC Pharmaceuticals, rinzimetostat is currently being evaluated for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in combination with androgen receptor pathway inhibitors, targeting the synergistic pathways of AR signaling and PRC2-mediated repression.