HH2853

HH2853 is an orally bioavailable, small molecule dual inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2), which are components of the polycomb repressive complex 2 (PRC2). By inhibiting both wild-type and mutated forms of EZH1/2, HH2853 reduces H3K27me3 levels in tumor cells, leading to antineoplastic effects. It has demonstrated potent preclinical and clinical activity against tumors with gain-of-function EZH2 mutations as well as those with wild-type EZH2. The drug is being developed primarily for relapsed/refractory non-Hodgkin lymphomas—including peripheral T-cell lymphoma, diffuse large B-cell lymphoma, follicular lymphoma—and advanced solid tumors such as soft tissue sarcoma and epithelioid sarcoma. Clinical trials have shown promising efficacy and a favorable safety profile compared to existing EZH2 inhibitors like tazemetostat[1][2][4][7].