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zeprumetostat
- Development stage
- Phase 3
- Lead developer
- Hengrui Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Zeprumetostat (SHR2554) is an orally bioavailable, highly selective small-molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), developed by Jiangsu Hengrui Pharmaceuticals. EZH2 is a histone methyltransferase and the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2), which mediates the trimethylation of histone H3 at lysine 27 (H3K27me3), a modification associated with epigenetic gene silencing. In various cancers, including triple-negative breast cancer (TNBC) and certain lymphomas, EZH2 is often overexpressed or mutated, leading to the silencing of tumor suppressor genes and promoting oncogenesis. In the context of the FUTURE umbrella trial led by Fudan University Shanghai Cancer Center, zeprumetostat is being evaluated as a targeted therapy for patients with the Luminal Androgen Receptor (LAR) subtype of refractory metastatic TNBC, typically in combination with the androgen receptor inhibitor rezvilutamide (SHR3680).
- Brand names
- Airuijing
- Other names
- SHR2554SHR-2554SHR 2554EZH2 inhibitor SHR2554EZH-2 inhibitor SHR2554EZH 2 inhibitor SHR2554
02
Targets
EZH2 (Histone-lysine N-methyltransferase EZH2)
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