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zeprumetostat + glofitamab + gemcitabine + oxaliplatin
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This combination therapy is a multi-agent regimen being evaluated for the treatment of relapsed or refractory diffuse large B-cell lymphoma (DLBCL). It consists of **zeprumetostat** (SHR2554), a small molecule inhibitor of the histone methyltransferase **EZH2**; **glofitamab** (Columvi), a bispecific monoclonal antibody that targets both **CD20** on B-cells and **CD3** on T-cells; and the **GemOx** chemotherapy doublet, comprising **gemcitabine** and **oxaliplatin**. The rationale for the combination lies in the epigenetic priming effect of EZH2 inhibition, which can enhance the expression of surface antigens and sensitize tumor cells to T-cell mediated killing by glofitamab. GemOx provides additional cytotoxic activity by inhibiting DNA synthesis and inducing DNA damage. The regimen is currently in Phase Ib/II clinical development.
- Other names
- Zeprumetostat + Glofitamab + GemOx
02
Targets
CD20 (B-lymphocyte antigen CD20)EZH2 (Histone-lysine N-methyltransferase EZH2)RNR (Ribonucleotide reductase)CD3 (T-cell surface glycoprotein CD3)DNA
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