预约演示
更新于：2026-06-05
Zeprumetostat
泽美妥司他
更新于：2026-06-05
概要
基本信息
药物类型 小分子化药 |
别名 EBI 2554、SHR 2554、SHR2554 + [4] |
靶点 |
作用方式 抑制剂 |
作用机制 EZH2抑制剂(组蛋白赖氨酸甲基化酶EZH2抑制剂)、表观遗传学药物 |
在研适应症 |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2025-08-26), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、突破性疗法 (中国)、附条件批准 (中国)、特殊审批 (中国) |
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结构/序列
分子式C32H44N4O4 |
InChIKeyYLZVNQZYAYVUCW-UHFFFAOYSA-N |
CAS号2098545-98-1 |
关联
42
项与 泽美妥司他 相关的临床试验NCT07562568
A Prospective, Multicenter, Open-label, Randomized Controlled Trial of SHR2554 Plus Azacitidine in Overlapped Sequential Combination With TBF Conditioning Regimen in Patients With High-risk or Relapsed/Refractory Acute Leukemia and Myelodysplastic Neoplasms
NCT07575412
A Prospective, Multicenter, Open-label, Randomized Controlled Trial of SHR2554 Plus Azacitidine in Overlapped Sequential Combination With Modified BUCY Conditioning Regimen in Patients With High-risk or Relapsed/Refractory Acute Leukemia and Myelodysplastic Neoplasms Secondary IDs
ChiCTR2600125881
An Open-Label, Single-Arm, Single-Center Clinical Trial of Zeprumetostat in Patients with Relapsed or Refractory Cutaneous T-Cell Lymphoma
100 项与 泽美妥司他 相关的临床结果
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100 项与 泽美妥司他 相关的转化医学
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100 项与 泽美妥司他 相关的专利（医药）
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10
项与 泽美妥司他 相关的文献（医药）2026-03-01DRUGS
Zeprumetostat: First Approval
Review
作者: Keam, Susan J
Zeprumetostat (), 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.
2025-09-01INTERNATIONAL IMMUNOPHARMACOLOGY
Inhibition of EZH2 by SHR2554 modifies subset ratios and suppresses polyfunctional responses of peripheral blood T cells from hematopoietic stem cell donors
Article
作者: Yuan, Jing ; Liu, Xuan ; Li, Jundong ; Zhou, Ziwei ; Hua, Huan ; Wang, Fuxu
BACKGROUND:
T cells play pivotal roles in orchestrating immune responses after allogeneic hematopoietic stem cell transplantation. Donor T cells facilitate the reconstitution of the recipient's immune system and Enhancer of Zeste Homolog 2 (EZH2) is crucial for T-cell differentiation and plasticity. Inhibitors of EZH2 may protect patients undergoing allogeneic stem cell transplantation from developing graft-versus-host disease without compromising the beneficial graft-versus-leukemia effect. Here, we investigated the impact of SHR2554, a novel and highly selective EZH2 inhibitor, on the subset ratios and polyfunctional responses of peripheral T-cells from hematopoietic stem cell donors METHODS: Cell proliferation, cell cycle, and apoptosis were analyzed using Cell Counting Kit-8 assays and flow cytometry. Western blotting was employed to detect the abundance of related proteins. RNA-sequencing was used to analyze gene expression after SHR2554 treatment RESULTS: SHR2554 inhibited proliferation, promoted apoptosis, and induced cell cycle arrest in donor T cells. SHR2554 also preserved CD4+/CD8+ T cell ratios while selectively depleting naïve (TN) and terminally differentiated effector (TEff) subsets and concurrently expanding central memory (TCM), effector memory (TEM), and regulatory T cell (Treg) subsets across CD3+/CD4+/CD8+ populations. SHR2554 significantly attenuated CD107a expression and IFNγ/TNFα secretion from CD3+/CD4+/CD8+ T cells, thereby suppressing polyfunctional responses across T cell subsets CONCLUSIONS: SHR2554, a potent and highly selective small-molecule inhibitor of EZH2, demonstrated a remarkable anti-proliferative effect on donor peripheral blood T cells, and modified T cell ratios and suppressed their polyfunctional responses. SHR2554 therefore has potential for treating graft-versus-host disease.
2025-09-01EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Pharmacokinetic interaction between SHR2554 and fluconazole: A single-center, open-label and one-sequence crossover phase I trial in healthy Chinese subjects
Article
作者: Yuan, Weilan ; Hu, Minwan ; Li, Shaorong ; Wu, Feng ; Han, Ying ; Zhao, Xiuli ; Zhu, Zhenyu ; Dai, Yuyang ; Guo, Shaojie ; Ni, Siyang
SHR2554, a highly selective oral EZH2 inhibitor, shows promise in treating hematologic malignancies. However, its metabolism via CYP3A4 raises concerns about drug-drug interactions. This study evaluates the impact of fluconazole, a moderate CYP3A4 inhibitor, on the pharmacokinetics and safety implications of SHR2554. We conducted a single-center, open-label, single-dose, single-sequence crossover phase I trial. 18 Chinese healthy subjects were orally administered SHR2554 100 mg on Day 1, fluconazole 400 mg on Day 4 and 200 mg QD from Days 5 to 6. SHR2554 100 mg co-administrated with fluconazole 200 mg on Day 7, and fluconazole 200 mg QD from Days 8 to 9. Pharmacokinetic parameters were compared after subjects were administered SHR2554 alone and in combination with fluconazole. Cmax, AUC0-t, and AUC0-∞ were significantly increased when SHR2554 was co-administered with fluconazole. The co-administration led to a 3.29-, 4.79-, and 4.13-fold increase in Cmax, AUC0-t, and AUC0-∞, respectively. Safety evaluations indicated that the observed treatment-emergent adverse events were mild and transient. These findings underline the necessity of caution when co-administered SHR2554 with moderate CYP3A4 inhibitors in clinical settings, providing crucial insights for optimizing future clinical trials.
研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 复发型外周T细胞淋巴瘤 | 中国 | 2025-08-26 | |
| 难治性外周T细胞淋巴瘤 | 中国 | 2025-08-26 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 外周T细胞淋巴瘤 | 临床3期 | 中国 | 2024-01-17 | |
| 骨髓增生异常综合征 | 临床2期 | 中国 | 2026-06-01 | |
| 前体B细胞成淋巴细胞白血病淋巴瘤 | 临床2期 | 中国 | 2026-06-01 | |
| 前体T淋巴细胞白血病淋巴瘤 | 临床2期 | 中国 | 2026-06-01 | |
| 难治性急性白血病 | 临床2期 | 中国 | 2026-06-01 | |
| 难治性急性髓细胞白血病 | 临床2期 | 中国 | 2026-06-01 | |
| 转移性前列腺癌 | 临床2期 | 中国 | 2025-12-08 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2025-10-09 | |
| 非小细胞肺癌 | 临床2期 | 中国 | 2025-10-09 | |
| 胃食管交界处腺癌 | 临床2期 | 中国 | 2025-09-05 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 67 | 壓壓淵築膚築夢鬱選糧(糧憲範願齋淵壓衊簾蓋) = 夢淵鑰艱襯簾憲餘繭願 壓餘獵餘選襯廠淵遞糧 (選鑰繭壓襯繭願衊積簾, 51.5 ~ 75.5) 达到 更多 | 积极 | 2025-06-12 | |||
临床1期 | 28 | 膚積蓋觸夢齋淵淵網齋(簾鏇範憲壓鑰醖積醖範) = 願鏇餘壓齋壓觸襯襯壓 範範夢遞糧製顧鏇遞餘 (鹹窪餘網遞襯遞蓋衊積, 41 ~ 78) 更多 | 积极 | 2024-04-01 | |||
临床2期 | 肉瘤 INI1 Loss | 9 | 鹽願糧膚選獵廠鬱願醖(淵醖艱壓齋鑰製窪範簾) = 觸衊鹽襯鹽鏇醖艱鏇廠 遞憲窪鏇醖願廠獵顧積 (鹹範鑰襯膚顧鑰憲襯糧, 1.2 ~ NA) 更多 | 积极 | 2023-10-23 | ||
临床1期 | 28 | 鬱積觸構廠遞選衊鹽廠(廠製積顧簾窪糧鹹廠積) = 鬱網鬱獵鬱艱製憲鏇積 鬱窪製夢選蓋選鏇廠遞 (餘醖觸襯築夢積淵構艱 ) 更多 | 积极 | 2023-06-09 | |||
临床1期 | 32 | 簾鹽製鹹壓鑰鬱淵獵壓(鑰製餘簾遞鑰願鑰選簾) = SHR2554 350mg bid plus SHR-1701 30mg/kg q3w 鏇觸獵鏇鬱築簾製鏇範 (齋齋糧衊製齋淵襯鑰糧 ) 更多 | 积极 | 2023-05-31 | |||
临床1期 | 113 | 顧窪襯築淵壓壓襯餘築(簾遞鹹齋鑰糧鏇淵蓋襯) = 鹽齋蓋網製廠簾衊顧憲 鏇鏇選夢餘淵鹹壓觸鬱 (積繭鬱獵廠鏇糧鹹構積 ) 更多 | 积极 | 2022-07-01 | |||
临床1期 | 113 | 衊製鬱願襯鬱願憲廠膚(網廠構醖襯蓋齋遞鑰壓) = 窪蓋鹽構製積構窪鑰襯 繭鬱餘範鹽獵遞鏇鏇膚 (糧窪淵憲廠艱築繭鑰壓, 42.1 ~ 73.7) 更多 | - | 2022-06-02 |
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