zeprumetostat + azacitidine

Zeprumetostat + azacitidine is an investigational combination therapy being evaluated for the treatment of primary refractory peripheral T-cell lymphoma (PTCL). Zeprumetostat (SHR2554) is a potent, selective small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a histone methyltransferase that mediates gene silencing through H3K27 trimethylation. Azacitidine is a pyrimidine nucleoside analog that acts as a DNA methyltransferase (DNMT) inhibitor, promoting DNA hypomethylation and the reactivation of silenced tumor suppressor genes. This combination therapy aims to achieve synergistic anti-tumor effects by simultaneously targeting multiple epigenetic pathways that are frequently dysregulated in T-cell malignancies. The combination is currently being studied in a Phase 1/2 genotype-guided clinical trial sponsored by Ruijin Hospital.

Other names

SHR2554 + azacitidinezeprumetostat + azacitadine