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zeprumetostat + fuzuloparib
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Zeprumetostat + fuzuloparib is a combination therapy comprising an EZH2 inhibitor and a PARP inhibitor, currently under investigation for the treatment of advanced or recurrent ovarian epithelial carcinoma. Zeprumetostat (SHR2554) is a small molecule that selectively inhibits the histone methyltransferase Enhancer of Zeste Homolog 2 (EZH2), thereby reversing epigenetic silencing of tumor suppressor genes. Fuzuloparib (SHR3162) is a potent inhibitor of Poly (ADP-ribose) polymerase (PARP) 1 and 2, which are critical for the repair of single-strand DNA breaks. By combining these two agents, the therapy aims to induce synthetic lethality and overcome resistance mechanisms in ovarian cancer cells. This specific clinical trial is being conducted by Peking University Third Hospital using agents developed by Jiangsu Hengrui Pharmaceuticals.
- Other names
- Zeprumetostat and Fuzuloparib combination
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)EZH2 (Histone-lysine N-methyltransferase EZH2)
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