Drug intelligence / Profile preview

zeprumetostat + chidamide

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of zeprumetostat and chidamide is an investigational epigenetic therapy being evaluated for the treatment of hematological malignancies, particularly peripheral T-cell lymphoma (PTCL). Zeprumetostat (SHR2554) is an oral, selective, small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a histone methyltransferase that often promotes tumor growth through gene silencing. Chidamide is a benzamide-type, subtype-selective histone deacetylase (HDAC) inhibitor that targets HDAC 1, 2, 3, and 10. Preclinical research has demonstrated synergistic anti-tumor activity between these two agents, as they simultaneously modulate different epigenetic pathways to reverse transcriptional repression and induce apoptosis in lymphoma cells. This combination is currently being studied in a genotype-guided Phase 1/2 clinical trial sponsored by Ruijin Hospital for patients with primary refractory PTCL.

Other names
SHR2554 + chidamidezeprumetostat + chidamide-Ruijin Hospital-peripheral T-cell lymphoma
02

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)HDAC (HDAC family)

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