<p>Zeprumetostat (艾瑞璟), an oral, selective, small molecule inhibitor of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, is being developed by Jiangsu Hengrui Pharmaceutical Co., Ltd for the treatment of solid and haematological malignancies. In August 2025, zeprumetostat received conditional approval in China for use in adult patients with relapsed or refractory peripheral T-cell lymphoma (r/r PTCL) who have received ≥ 1 line of systemic therapy. This article summarizes the milestones in the development of zeprumetostat leading to this first approval for the treatment of r/r PTCL.</p>

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Zeprumetostat: First Approval

  • Susan J. Keam

摘要

Zeprumetostat (艾瑞璟), an oral, selective, small molecule inhibitor of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, is being developed by Jiangsu Hengrui Pharmaceutical Co., Ltd for the treatment of solid and haematological malignancies. In August 2025, zeprumetostat received conditional approval in China for use in adult patients with relapsed or refractory peripheral T-cell lymphoma (r/r PTCL) who have received ≥ 1 line of systemic therapy. This article summarizes the milestones in the development of zeprumetostat leading to this first approval for the treatment of r/r PTCL.