预约演示
更新于：2026-02-27
Uproleselan
更新于：2026-02-27
概要
基本信息
药物类型 化学药 |
别名 Uproleselan (USAN/INN)、Uproleselan injection、Uproleselan sodium + [2] |
靶点 |
作用方式 抑制剂 |
作用机制 E-sel抑制剂(选择素-E抑制剂) |
在研适应症 |
最高研发阶段临床2/3期 |
首次获批日期- |
最高研发阶段(中国)临床1期 |
特殊审评快速通道 (美国)、突破性疗法 (中国)、突破性疗法 (美国) |
登录后查看时间轴
结构/序列
分子式C60H109N3NaO27 |
InChIKeyHHTBXHJWLLMOLI-CVDXTIKBSA-N |
CAS号1914993-95-5 |
关联
17
项与 Uproleselan 相关的临床试验NCT05146739
A Phase 1 and Pharmacokinetic Study of Uproleselan (GMI-1271, NSC #801708) in Combination With Fludarabine and Cytarabine for Patients With Acute Myeloid Leukemia, Myelodysplastic Syndrome or Mixed Phenotype Acute Leukemia That Expresses E-selectin Ligand on the Cell Membrane and is in Second or Greater Relapse or That is Refractory to Relapse Therapy
NCT05569512
A Phase 1/2 Trial of Uproleselan Combined With High Dose Busulfan Pre-Transplant Conditioning in Hematopoietic Stem Cell Transplantation for Patients With Chemotherapy Resistant Acute Myeloid Leukemia
NCT05054543
A Phase 3 Randomized, Double-Blinded Bridging Trial to Evaluate the Efficacy of Uproleselan Administered With Chemotherapy Versus Chemotherapy Alone in Chinese Patients With Relapsed/Refractory Acute Myeloid Leukemia
100 项与 Uproleselan 相关的临床结果
登录后查看更多信息
100 项与 Uproleselan 相关的转化医学
登录后查看更多信息
100 项与 Uproleselan 相关的专利（医药）
登录后查看更多信息
11
项与 Uproleselan 相关的文献（医药）2025-11-01Transplantation and Cellular Therapy
A Phase II Randomized, Double-Blind, Placebo-Controlled Trial to Evaluate E-Selectin Inhibition with Uproleselan to Reduce Gastrointestinal Toxicity During Autologous Hematopoietic Cell Transplantation for Multiple Myeloma
Article
作者: DiPersio, John F ; Vij, Ravi ; Stockerl-Goldstein, Keith ; Gao, Feng ; Uy, Geoffrey L ; Ryan, Meaghan ; Christen, Brandon ; Slade, Michael J ; Mayeski, Chris ; Crees, Zachary D ; Schroeder, Mark A
2024-06-01British journal of haematology
Combining 5‐azacitidine with the E‐selectin antagonist uproleselan is an effective strategy to augment responses in myelodysplasia and acute myeloid leukaemia
Article
作者: Magnani, John L. ; Lincz, Lisa F. ; Enjeti, Anoop K. ; Bond, Danielle R. ; Smith, Theodore A. G. ; Fogler, William E.
Summary:
The interaction of acute myeloid leukaemic (AML) blasts with the bone marrow (BM) microenvironment is a major determinant governing disease progression and resistance to treatment. The constitutive expression of E‐selectin in the vascular compartment of BM, a key endothelial cell factor, directly mediates chemoresistance via E‐selectin ligand/receptors. Despite the success of hypomethylating agent (HMA)‐containing regimens to induce remissions in older AML patients, the development of primary or secondary resistance is common. We report that following treatment with 5‐azacitidine, promoter regions regulating the biosynthesis of the E‐selectin ligands, sialyl Lewis X, become further hypomethylated. The resultant upregulation of these gene products, in particular α(1,3)‐fucosyltransferase VII (FUT7) and α(2,3)‐sialyltransferase IV (ST3GAL4), likely causes functional E‐selectin binding. When combined with the E‐selectin antagonist uproleselan, the adhesion to E‐selectin is reversed and the survival of mice transplanted with AML cells is prolonged. Finally, we present clinical evidence showing that BM myeloid cells from higher risk MDS and AML patients have the potential to bind E‐selectin, and these cells are more abundant in 5‐azacitidine‐non‐responsive patients. The collective data provide a strong rationale to evaluate 5‐azacitidine in combination with the E‐selectin antagonist, uproleselan, in this patient population.
2024-05-01Blood reviews
Targeting hematologic malignancies by inhibiting E-selectin: A sweet spot for AML therapy?
Review
作者: Magnani, John L ; Lazarus, Hillard M ; Uy, Geoffrey L ; Lozier, Jay N ; Becker, Pamela S ; Jonas, Brian A ; DeAngelo, Daniel J ; Winkler, Ingrid G ; Fisher, Dennis M
E-selectin, a cytoadhesive glycoprotein, is expressed on venular endothelial cells and mediates leukocyte localization to inflamed endothelium, the first step in inflammatory cell extravasation into tissue. Constitutive marrow endothelial E-selectin expression also supports bone marrow hematopoiesis via NF-κB-mediated signaling. Correspondingly, E-selectin interaction with E-selectin ligand (sialyl Lewisx) on acute myeloid leukemia (AML) cells leads to chemotherapy resistance in vivo. Uproleselan (GMI-1271) is a carbohydrate analog of sialyl Lewisx that blocks E-selectin binding. A Phase 2 trial of MEC chemotherapy combined with uproleselan for relapsed/refractory AML showed a median overall survival of 8.8 months and low (2%) rates of severe oral mucositis. Clinical trials seek to confirm activity in AML and mitigation of neutrophil-mediated adverse events (mucositis and diarrhea) after intensive chemotherapy. In this review we summarize E-selectin biology and the rationale for uproleselan in combination with other therapies for hematologic malignancies. We also describe uproleselan pharmacology and ongoing clinical trials.
100 项与 Uproleselan 相关的药物交易
登录后查看更多信息
研发状态
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 |
|---|---|---|---|---|
| 复发性急性髓细胞白血病 | 临床3期 | 中国 | 2021-11-17 | |
| 成人急性髓性白血病 | 临床3期 | 中国 | 2021-10-27 | |
| 成人急性髓性白血病 | 临床3期 | 中国 | 2021-10-27 | |
| 急性早幼粒细胞白血病 | 临床3期 | 美国 | 2019-03-28 | |
| 难治性急性髓细胞白血病 | 临床3期 | 美国 | 2018-10-15 | |
| 难治性急性髓细胞白血病 | 临床3期 | 澳大利亚 | 2018-10-15 | |
| 难治性急性髓细胞白血病 | 临床3期 | 加拿大 | 2018-10-15 | |
| 难治性急性髓细胞白血病 | 临床3期 | 法国 | 2018-10-15 | |
| 难治性急性髓细胞白血病 | 临床3期 | 爱尔兰 | 2018-10-15 | |
| 难治性急性髓细胞白血病 | 临床3期 | 意大利 | 2018-10-15 |
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2/3期 | 267 | (Arm I (Daunorubicin, Cytarabine)) | 繭鑰艱廠鏇鏇壓鹽鏇醖(糧齋壓築醖鬱醖憲淵繭) = 觸鹹廠餘選衊觸顧選鬱 醖觸膚製網艱糧築餘鬱 (遞淵齋艱齋鑰蓋憲鹹築, 築齋觸醖鹽襯選選糧壓 ~ 壓餘顧窪積選觸繭顧築) 更多 | - | 2026-01-21 | ||
(Arm II (Uproleselan, Daunorubicin, Cytarabine)) | 繭鑰艱廠鏇鏇壓鹽鏇醖(糧齋壓築醖鬱醖憲淵繭) = 鬱顧醖壓衊遞遞蓋襯範 醖觸膚製網艱糧築餘鬱 (遞淵齋艱齋鑰蓋憲鹹築, 獵簾廠製醖蓋遞鏇醖廠 ~ 壓鑰蓋製範構顧積鬱觸) 更多 | ||||||
临床2/3期 | 急性髓性白血病 FLT3unmutated | ASXL1 mutated | 267 | Uproleselan + conventional chemotherapy | 窪構窪鬱餘繭餘鹹衊築(繭衊顧鏇簾齋鹽壓願鑰): HR = 0.71 (95.0% CI, 0.34 ~ 1.47), P-Value = 0.35 更多 | 不佳 | 2025-12-06 | |
Conventional chemotherapy | |||||||
临床1/2期 | 37 | (Ph 1 Treatment Dose Level -1 Cladaribine 3.75mg/m^2) | 蓋鏇襯淵積築遞醖選鏇 = 蓋範鹹餘糧齋簾遞願衊 製齋衊窪壓壓鑰糧壓齋 (鹹網獵衊鹹醖觸鑰觸憲, 鑰膚齋壓鹽願蓋蓋選蓋 ~ 淵壓獵壓積蓋構壓夢製) 更多 | - | 2025-10-20 | ||
(Ph 1 Treatment Dose Level 1 Cladaribine 5 mg/m^2) | 蓋鏇襯淵積築遞醖選鏇 = 鬱憲鹹範鹹鹹築窪獵簾 製齋衊窪壓壓鑰糧壓齋 (鹹網獵衊鹹醖觸鑰觸憲, 壓鬱網構獵艱遞齋製窪 ~ 糧範築遞網積觸蓋觸廠) 更多 | ||||||
临床3期 | 140 | 醖蓋顧鏇壓繭製築膚膚(鏇範繭餘鏇網廠夢繭鬱) = 膚鬱憲憲顧醖淵艱鏇築 餘鬱襯繭醖鏇壓積顧餘 (願衊壓糧醖鏇鹹鹽獵艱, 6.1 ~ 16.0) 未达到 更多 | 不佳 | 2024-12-20 | |||
Chemotherapy alone | 醖蓋顧鏇壓繭製築膚膚(鏇範繭餘鏇網廠夢繭鬱) = 構夢齋觸遞夢積鬱鬱鑰 餘鬱襯繭醖鏇壓積顧餘 (願衊壓糧醖鏇鹹鹽獵艱, 6.2 ~ NA) 未达到 更多 | ||||||
临床2期 | 急性髓性白血病 巩固 | 37 | 鏇鑰鹹鏇鏇襯選淵願築(憲廠鑰獵窪鏇廠網齋夢) = 醖鏇糧艱鏇艱襯繭獵壓 願鬱鑰艱壓鬱艱鏇衊簾 (願窪築夢醖壓淵齋遞積 ) 更多 | 积极 | 2024-12-09 | ||
临床2/3期 | - | 齋範遞鑰壓構獵鑰齋範(觸窪蓋願選夢膚衊製壓) = not reached the endpoint 構夢鏇願壓網積襯鑰襯 (顧膚餘繭膚積築餘鹽鑰 ) | 不佳 | 2024-10-29 | |||
临床3期 | 388 | 製糧醖簾窪鑰鬱壓鑰艱(蓋廠網鹽鑰鑰鏇憲衊壓) = 糧積觸齋艱淵襯憲鬱鹽 鬱糧鏇襯衊餘壓簾網廠 (選積廠願顧簾築憲襯衊 ) 更多 | 积极 | 2024-06-04 | |||
Placebo | 製糧醖簾窪鑰鬱壓鑰艱(蓋廠網鹽鑰鑰鏇憲衊壓) = 觸淵淵艱鏇獵憲窪鏇廠 鬱糧鏇襯衊餘壓簾網廠 (選積廠願顧簾築憲襯衊 ) 更多 | ||||||
临床3期 | 388 | 淵醖範鏇鬱鬱壓膚廠獵(鑰鬱鬱窪鹽製鬱簾膚壓) = 願範製遞鹹憲齋糧夢衊 膚齋鏇齋積廠夢齋夢廠 (艱夢鹹齋壓鬱鬱淵觸蓋 ) 未达到 | 不佳 | 2024-05-06 | |||
placebo | 淵醖範鏇鬱鬱壓膚廠獵(鑰鬱鬱窪鹽製鬱簾膚壓) = 醖夢鹽蓋夢淵夢簾糧窪 膚齋鏇齋積廠夢齋夢廠 (艱夢鹹齋壓鬱鬱淵觸蓋 ) 未达到 | ||||||
临床2期 | 51 | (Uproleselan + Standard of Care Melphalan) | 夢鏇艱糧遞築鹹鹹積鹹(遞製觸窪壓衊選窪壓襯) = 壓網構蓋繭襯窪製窪願 鏇範獵淵壓膚繭鑰膚鹽 (顧齋鹽構築顧範壓廠積, 0.00) 更多 | - | 2023-12-15 | ||
Placebo+Melphalan (Placebo + Standard of Care Melphalan) | 夢鏇艱糧遞築鹹鹹積鹹(遞製觸窪壓衊選窪壓襯) = 簾襯窪鹽選鏇鑰遞窪鹽 鏇範獵淵壓膚繭鑰膚鹽 (顧齋鹽構築顧範壓廠積, 0.34) 更多 | ||||||
临床1/2期 | 20 | 淵範齋壓襯獵憲齋糧獵(醖網願糧鹹鏇膚廠選膚) = 醖糧網遞範艱衊夢窪鏇 夢觸築鑰鬱淵廠夢繭齋 (淵築願遞鏇蓋醖鑰憲製 ) 更多 | - | 2023-12-10 |
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