# Zeprumetostat

Source: https://onco.cc/drugs/zeprumetostat/  
OnCo record `zeprumetostat` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Summary

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.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-11-03
- Also known as: TLN-254; SHR2554; Airuijing
- Tags: pipeline; ctgov-ingest
- Code: TLN-254
- Modality: Small molecule EZH2 inhibitor
- Mechanism: Inhibits EZH2, a protein that helps cells control which genes are switched on and that is overexpressed or mutated in many cancers.
- Approvals: China 2025: Relapsed or refractory peripheral T-cell lymphoma after at least one line of systemic therapy (conditional approval)

## Sources

- Treeline Biosciences: treeline.bio: https://treeline.bio/medicines
- Treeline Biosciences: treeline.bio: https://treeline.bio/medicines
- Zeprumetostat: First Approval (Drugs, 2026): https://doi.org/10.1007/s40265-025-02271-0
- ClinicalTrials.gov: trials of TLN-254: https://clinicaltrials.gov/search?intr=TLN-254

## Connected records

- cancers: [Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome)](https://onco.cc/cancers/cutaneous-t-cell-lymphoma/), [Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma)](https://onco.cc/cancers/peripheral-t-cell-lymphoma/)
- targets: [EZH2](https://onco.cc/targets/ezh2/)
- companies: [Jiangsu Hengrui Pharmaceuticals](https://onco.cc/companies/hengrui/), [Treeline Biosciences](https://onco.cc/companies/treeline-biosciences/)
- trials: [A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer](https://onco.cc/trials/nct07230106/), [A Study of TLN-254 in Participants With Relapsed or Refractory T-cell Lymphoma](https://onco.cc/trials/nct06733441/), [Phase II Clinical Study of SHR2554 Tablets Combined With Other Anti-tumor Treatments in Non-small Cell Lung Cancer Subjects](https://onco.cc/trials/nct07175220/), [Safety and Efficacy of SHR2554 Combined With Other Antitumor Therapies in Gastric or Gastro-oesophageal Junction Adenocarcinoma](https://onco.cc/trials/nct07102901/), [SHR-1701 Combined with SHR2554 and BP102 for MCRC](https://onco.cc/trials/nct06679673/), [TLN-121 in Relapsed or Refractory Non-Hodgkin Lymphomas](https://onco.cc/trials/nct07082803/)

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