Zeprumetostat is a tablet that blocks EZH2, an enzyme that switches genes off; China approved it in 2025 for peripheral T-cell lymphoma that came back after treatment, and Treeline Biosciences is testing it in phase 1 elsewhere.
Zeprumetostat (TLN-254, SHR2554, Airuijing) is a small molecule EZH2 inhibitor from Treeline Biosciences, with Jiangsu Hengrui Pharmaceuticals as partner. Inhibits EZH2, a protein that helps cells control which genes are switched on and that is overexpressed or mutated in many cancers. Its furthest stage is approval, for peripheral T-cell lymphoma and cutaneous T-cell lymphoma. ClinicalTrials.gov registers it in 6 studies linked below. China granted conditional approval in August 2025 for relapsed or refractory peripheral T-cell lymphoma after at least one line of systemic therapy, where Jiangsu Hengrui markets it as Airuijing. Treeline in-licensed it for territories outside Greater China, where its own programme is in phase 1.
Inhibits EZH2, a protein that helps cells control which genes are switched on and that is overexpressed or mutated in many cancers. Connects to EZH2.
1.Zeprumetostat slips into a pocket on EZH2.
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| Region | Year | Indication |
|---|---|---|
| China | 2025 | Relapsed or refractory peripheral T-cell lymphoma after at least one line of systemic therapy (conditional approval) · Marketed by Jiangsu Hengrui as Airuijing; Drugs, 'Zeprumetostat: First Approval', doi:10.1007/s40265-025-02271-0 |
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Query for this drug: (TITLE:"Zeprumetostat" OR ABSTRACT:"Zeprumetostat" OR TITLE:"TLN-254" OR ABSTRACT:"TLN-254" OR TITLE:"SHR2554" OR ABSTRACT:"SHR2554" OR TITLE:"Airuijing" OR ABSTRACT:"Airuijing") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Zeprumetostat, not a curated reading list.
Shares TLN-121 in Relapsed or Refractory Non-Hodgkin Lymphomas, Treeline Biosciences and the tag pipeline.
Shares Phase II Clinical Study of SHR2554 Tablets Combined With Other Anti-tumor Treatments in Non-small Cell Lung Cancer Subjects, SHR-1701 Combined with SHR2554 and BP102 for MCRC, Safety and Efficacy of SHR2554 Combined With Other Antitumor Therapies in Gastric or Gastro-oesophageal Junction Adenocarcinoma, Jiangsu Hengrui Pharmaceuticals and the tag pipeline.
Shares A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer, Jiangsu Hengrui Pharmaceuticals and the tag pipeline.
Shares Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome), Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma) and the tag pipeline.
Shares Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome), Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma) and the tag pipeline.
Shares Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome), Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma) and the tag pipeline.
Shares Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome), Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma) and the tag pipeline.
Shares Treeline Biosciences and the tag pipeline.
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