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zeprumetostat + golidocitinib
- Development stage
- Unknown
- Lead developer
- Ruijin Hospital
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
zeprumetostat + golidocitinib 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 catalyzes the trimethylation of histone H3 at lysine 27 (H3K27me3), leading to epigenetic silencing of tumor suppressor genes. Golidocitinib (DZD4205) is a highly selective Janus Kinase 1 (JAK1) inhibitor that blocks the phosphorylation of STAT proteins, thereby inhibiting the JAK/STAT signaling pathway which is frequently hyperactivated in T-cell malignancies. This combination is part of a genotype-guided clinical study led by Ruijin Hospital, where patients are assigned to specific targeted combinations based on their tumor's genetic profile to overcome resistance and improve therapeutic outcomes in refractory lymphoma.
- Other names
- zeprumetostat and golidocitinib
02
Targets
JAK1 (Janus kinase 1)EZH2 (Histone-lysine N-methyltransferase EZH2)
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