{"entity":{"id":"zeprumetostat","kind":"drug","name":"Zeprumetostat","aka":["TLN-254","SHR2554","Airuijing"],"tldr":"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.","status":"approved","asOf":"2026-11-03","links":[{"label":"Treeline Biosciences: treeline.bio","url":"https://treeline.bio/medicines"},{"label":"Treeline Biosciences: treeline.bio","url":"https://treeline.bio/medicines"},{"label":"Zeprumetostat: First Approval (Drugs, 2026)","url":"https://doi.org/10.1007/s40265-025-02271-0"},{"label":"ClinicalTrials.gov: trials of TLN-254","url":"https://clinicaltrials.gov/search?intr=TLN-254"}],"tags":["pipeline","ctgov-ingest"],"related":[],"cancers":["peripheral-t-cell-lymphoma","cutaneous-t-cell-lymphoma"],"sections":[],"technologies":[],"targets":["ezh2"],"drugs":[],"companies":["treeline-biosciences","hengrui"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06733441","nct07082803","nct07230106","nct07175220","nct07102901","nct06679673"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"OnCo gap audit, class 5 (company pipeline pages and ClinicalTrials.gov v2)","editedOn":"2026-11-03"},"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":[{"region":"China","year":2025,"indication":"Relapsed or refractory peripheral T-cell lymphoma after at least one line of systemic therapy (conditional approval)","note":"Marketed by Jiangsu Hengrui as Airuijing; Drugs, 'Zeprumetostat: First Approval', doi:10.1007/s40265-025-02271-0"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/zeprumetostat/","neighbours":{"cancer":[{"id":"cutaneous-t-cell-lymphoma","kind":"cancer","name":"Cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome)","route":"/cancers/cutaneous-t-cell-lymphoma/"},{"id":"peripheral-t-cell-lymphoma","kind":"cancer","name":"Peripheral T-cell lymphomas (including cutaneous T-cell lymphoma)","route":"/cancers/peripheral-t-cell-lymphoma/"}],"target":[{"id":"ezh2","kind":"target","name":"EZH2","route":"/targets/ezh2/"}],"company":[{"id":"hengrui","kind":"company","name":"Jiangsu Hengrui Pharmaceuticals","route":"/companies/hengrui/"},{"id":"treeline-biosciences","kind":"company","name":"Treeline Biosciences","route":"/companies/treeline-biosciences/"}],"trial":[{"id":"nct07230106","kind":"trial","name":"A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer","route":"/trials/nct07230106/"},{"id":"nct06733441","kind":"trial","name":"A Study of TLN-254 in Participants With Relapsed or Refractory T-cell Lymphoma","route":"/trials/nct06733441/"},{"id":"nct07175220","kind":"trial","name":"Phase II Clinical Study of SHR2554 Tablets Combined With Other Anti-tumor Treatments in Non-small Cell Lung Cancer Subjects","route":"/trials/nct07175220/"},{"id":"nct07102901","kind":"trial","name":"Safety and Efficacy of SHR2554 Combined With Other Antitumor Therapies in Gastric or Gastro-oesophageal Junction Adenocarcinoma","route":"/trials/nct07102901/"},{"id":"nct06679673","kind":"trial","name":"SHR-1701 Combined with SHR2554 and BP102 for MCRC","route":"/trials/nct06679673/"},{"id":"nct07082803","kind":"trial","name":"TLN-121 in Relapsed or Refractory Non-Hodgkin Lymphomas","route":"/trials/nct07082803/"}]}}