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zeprumetostat + decitabine
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Zeprumetostat + decitabine is an investigational combination therapy being evaluated for the treatment of primary refractory peripheral T-cell lymphoma (PTCL). Zeprumetostat (SHR2554) is an oral, potent, and selective small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2) that mediates gene silencing through histone H3 lysine 27 (H3K27) methylation. Decitabine is a pyrimidine nucleoside analog that acts as a DNA methyltransferase (DNMT) inhibitor, functioning as a hypomethylating agent to reactivate silenced tumor suppressor genes. This combination is part of a genotype-guided treatment strategy developed at Ruijin Hospital, aiming to synergistically target epigenetic dysregulation in T-cell lymphomas.
- Other names
- SHR2554 + decitabinezeprumetostat and decitabine
02
Targets
EZH2 (Histone-lysine N-methyltransferase EZH2)DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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