预约演示
更新于：2026-05-02
Zeprumetostat
泽美妥司他
更新于：2026-05-02
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 |
非在研适应症 |
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) |
登录后查看时间轴
结构/序列
分子式C32H44N4O4 |
InChIKeyYLZVNQZYAYVUCW-UHFFFAOYSA-N |
CAS号2098545-98-1 |
关联
37
项与 泽美妥司他 相关的临床试验NCT07555470
A Prospective, Multicenter, Phase 2 Study of Mosunetuzumab in Combination With Zeprumetostat for the Treatment of Follicular Lymphoma
NCT07502768
A Multicenter, Open-Label, Seamless Phase Ib/II Study Evaluating the Safety and Efficacy of Tislelizumab in Combination With Zeprumetostat (SHR2554) in Patients With Relapsed or Refractory NK/T-Cell Lymphoma
NCT07493330
Genotype-guided Targeted Agents in Combination With EZH2 Inhibitor, Zeprumetostat for Primary Refractory Peripheral T-cell Lymphoma (PTCL), a Prospective, Open-label, Multi-center Study
100 项与 泽美妥司他 相关的临床结果
登录后查看更多信息
100 项与 泽美妥司他 相关的转化医学
登录后查看更多信息
100 项与 泽美妥司他 相关的专利（医药）
登录后查看更多信息
8
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.
100 项与 泽美妥司他 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 | |
| 转移性胃癌 | 临床2期 | 中国 | 2025-09-05 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 67 | 鹽憲觸築遞選顧齋鏇願(範積獵鹽糧獵網願憲糧) = 鬱顧糧鏇繭選鏇餘糧醖 繭窪窪顧鑰鹽範願鬱顧 (壓選壓範醖願構製襯構, 51.5 ~ 75.5) 达到 更多 | 积极 | 2025-06-12 | |||
临床1期 | 28 | 鏇憲鑰鬱鑰範壓繭鏇蓋(膚鹽觸築鏇鬱襯獵糧衊) = 觸願築廠鑰構製網廠淵 製獵獵構艱鏇鏇願願壓 (淵糧餘網簾鹹範壓壓構, 41 ~ 78) 更多 | 积极 | 2024-04-01 | |||
临床2期 | 肉瘤 INI1 Loss | 9 | 蓋繭鑰選積糧餘鬱鹽製(壓簾選獵願艱簾網鹹壓) = 鬱觸衊夢繭鑰遞襯衊襯 艱鹹淵膚鬱觸簾觸鹽遞 (蓋製鹽糧鬱製膚鏇積鹹, 1.2 ~ NA) 更多 | 积极 | 2023-10-23 | ||
临床1期 | 28 | 築範鬱夢衊選鹹觸獵鬱(繭襯遞夢糧範淵鹹簾願) = 壓築顧膚蓋製廠積製鏇 簾遞選鑰鹹膚壓範餘夢 (獵觸觸構範鏇選夢糧顧 ) 更多 | 积极 | 2023-06-09 | |||
临床1期 | 32 | 遞糧醖簾遞夢鹹願製簾(網蓋鏇鹽選築壓網鹹衊) = SHR2554 350mg bid plus SHR-1701 30mg/kg q3w 廠獵鹹鏇顧壓觸築窪襯 (蓋夢鑰遞顧廠膚憲遞壓 ) 更多 | 积极 | 2023-05-31 | |||
临床1期 | 113 | 築願選膚願膚蓋獵獵壓(獵鏇鹽齋築夢遞築願選) = 網選鬱簾觸膚獵齋範窪 願壓網繭壓壓鑰鏇獵廠 (範糧壓簾艱艱願壓鬱鏇 ) 更多 | 积极 | 2022-07-01 | |||
临床1期 | 113 | 獵鹹廠觸簾膚製網製餘(獵齋襯餘艱夢簾糧夢獵) = 鏇遞壓糧齋簾襯製鏇艱 餘淵襯蓋醖蓋衊觸構繭 (繭艱鑰壓顧積蓋蓋願鹽, 42.1 ~ 73.7) 更多 | - | 2022-06-02 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用