Drug intelligence / Profile preview

zeprumetostat + azacitidine + mitoxantrone hydrochloride liposome

Development stage
Phase 2
Lead developer
Hengrui Therapeutics
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral, Subcutaneous, Intravenous
01

Overview

zeprumetostat + azacitidine + mitoxantrone hydrochloride liposome is a combination therapy being investigated for the treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL). The regimen consists of zeprumetostat, an oral small-molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2) developed by Jiangsu Hengrui Pharmaceuticals; azacitidine, a DNA methyltransferase inhibitor; and mitoxantrone hydrochloride liposome, a liposomal formulation of the cytotoxic agent mitoxantrone. This triple-drug combination is the subject of a Phase II clinical trial led by The First Affiliated Hospital of Soochow University, which aims to evaluate its efficacy and safety in patients who have failed at least one prior line of systemic therapy. Zeprumetostat itself received conditional approval in China in August 2025 for r/r PTCL as a monotherapy.

Other names
SHR2554 combinationSHR-2554 combinationSHR 2554 combination
02

Targets

DNADNMT (DNA methyltransferase)EZH2 (Histone-lysine N-methyltransferase EZH2)TOP2A (DNA topoisomerase II)

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