Drug intelligence / Profile preview

zeprumetostat + adabelimumab

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

SHR2554 + adabelimumab is an investigational combination therapy developed by Jiangsu HengRui Medicine. It consists of zeprumetostat (SHR2554), a highly selective oral small-molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), and adabelimumab, a monoclonal antibody targeting Programmed Death-Ligand 1 (PD-L1). EZH2 is a histone methyltransferase that often contributes to tumor progression and immune evasion; its inhibition suppresses H3K27 trimethylation, leading to cell cycle arrest and apoptosis. Adabelimumab acts as a checkpoint inhibitor to restore anti-tumor immune responses. The combination is being evaluated in Phase II clinical trials for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC), aiming to leverage potential synergy between epigenetic modulation and immune checkpoint blockade.

Other names
zeprumetostat + adabelimumab
02

Targets

TNFA (Tumor necrosis factor alpha (soluble))EZH1EZH2 (Histone-lysine N-methyltransferase EZH2)

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