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SHR-1701 + rivoceranib + SHR-2554

Development stage: Unknown
Lead developer: Hengrui Pharmaceutical
Modality: Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes, Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration: Intravenous, Oral

Overview

This combination therapy consists of SHR-1701, rivoceranib (also known as apatinib), and SHR-2554. SHR-1701 is a bifunctional fusion protein that simultaneously targets programmed cell death 1 ligand 1 (PD-L1) and transforming growth factor-beta (TGF-β), designed to overcome immune resistance in the tumor microenvironment. Rivoceranib is a highly selective small molecule tyrosine kinase inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), which acts as a potent anti-angiogenic agent. SHR-2554 is a selective small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), an epigenetic regulator that promotes tumor progression and immune evasion when overexpressed. This triplet regimen is being evaluated in Phase II clinical trials for the treatment of advanced gastric cancer and gastroesophageal junction adenocarcinoma, particularly in patients who have failed prior immunotherapy.

Other names: SHR-1701 + apatinib + SHR-2554

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)TGFB (GARP–latent transforming growth factor beta 1 complex)CD274 (Programmed cell death protein 1 ligand 1)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)EZH1

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