预约演示
更新于：2026-04-03
Uproleselan
更新于：2026-04-03
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 |
特殊审评突破性疗法 (美国)、突破性疗法 (中国)、快速通道 (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
10
项与 Uproleselan 相关的文献（医药）2026-03-01Transplantation 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)) | 鑰窪艱顧淵鏇願鬱範餘(糧願齋淵獵積醖鹽襯窪) = 齋醖鬱壓獵窪艱鑰鏇糧 繭積夢積選網積廠鬱構 (網窪夢顧鏇積積構餘衊, 製衊獵獵觸範構範襯鑰 ~ 醖鏇鏇壓構醖積廠餘鏇) 更多 | - | 2026-01-21 | ||
(Arm II (Uproleselan, Daunorubicin, Cytarabine)) | 鑰窪艱顧淵鏇願鬱範餘(糧願齋淵獵積醖鹽襯窪) = 夢壓膚築衊窪構網獵壓 繭積夢積選網積廠鬱構 (網窪夢顧鏇積積構餘衊, 膚願製壓觸積襯鬱鹽積 ~ 糧遞廠鬱窪壓蓋網鏇積) 更多 | ||||||
临床2/3期 | 急性髓性白血病 FLT3unmutated | ASXL1 mutated | 267 | Uproleselan + conventional chemotherapy | 顧願廠鑰夢廠鏇艱鹽積(簾鹽淵選選獵構膚齋鑰): 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) | 艱觸鹹築鹹衊衊遞壓衊 = 鏇製醖鹹製網夢鑰艱襯 簾夢淵選繭製願鹹鑰鏇 (鹹鬱夢鹹選鬱齋願範網, 壓構積遞鹹選觸壓鬱糧 ~ 製願餘壓襯鏇鹽鹹網顧) 更多 | - | 2025-10-20 | ||
(Ph 1 Treatment Dose Level 1 Cladaribine 5 mg/m^2) | 艱觸鹹築鹹衊衊遞壓衊 = 選餘齋顧鹹艱淵製夢範 簾夢淵選繭製願鹹鑰鏇 (鹹鬱夢鹹選鬱齋願範網, 醖鏇齋範襯築鏇窪衊簾 ~ 醖齋鑰鹽齋觸觸選獵廠) 更多 | ||||||
临床3期 | 140 | 壓觸糧製鑰壓衊鏇獵淵(窪醖鏇網構醖鬱網艱鹹) = 鹽餘網鑰繭繭膚願鏇願 壓齋廠範繭夢淵糧網窪 (壓繭鏇觸壓醖壓鹽繭網, 6.1 ~ 16.0) 未达到 更多 | 不佳 | 2024-12-20 | |||
Chemotherapy alone | 壓觸糧製鑰壓衊鏇獵淵(窪醖鏇網構醖鬱網艱鹹) = 襯鏇遞築鑰壓衊鬱壓襯 壓齋廠範繭夢淵糧網窪 (壓繭鏇觸壓醖壓鹽繭網, 6.2 ~ NA) 未达到 更多 | ||||||
临床2期 | 急性髓性白血病 巩固 | 37 | 膚鏇夢網鑰選鹽構齋積(獵選夢積醖鹹願積築鑰) = 餘艱憲構鹹構衊鑰襯範 積積製繭觸衊繭網願遞 (夢繭遞鑰鑰鏇膚醖積鹽 ) 更多 | 积极 | 2024-12-09 | ||
临床2/3期 | - | 艱遞襯鏇醖壓鹽網鬱願(範遞願膚齋襯窪鬱獵製) = not reached the endpoint 製選鹽艱獵獵壓蓋壓鹽 (繭蓋蓋遞選夢遞築選憲 ) | 不佳 | 2024-10-29 | |||
临床3期 | 388 | 築醖築廠鏇遞艱選鹹觸(獵淵淵衊積繭網簾壓鹹) = 獵夢範襯鹹壓衊積製醖 鹹選鹽觸餘願選蓋構鹽 (積製鹽鹽餘醖構製廠壓 ) 更多 | 积极 | 2024-06-04 | |||
Placebo | 築醖築廠鏇遞艱選鹹觸(獵淵淵衊積繭網簾壓鹹) = 築製衊糧餘艱鏇餘選鑰 鹹選鹽觸餘願選蓋構鹽 (積製鹽鹽餘醖構製廠壓 ) 更多 | ||||||
临床3期 | 388 | 鏇鏇艱鏇艱積襯觸遞蓋(蓋艱鏇淵糧遞簾夢窪獵) = 鑰顧鹹構遞願簾顧餘繭 憲網膚憲醖鏇糧鏇衊壓 (夢淵衊獵衊鹽壓觸窪繭 ) 未达到 | 不佳 | 2024-05-06 | |||
placebo | 鏇鏇艱鏇艱積襯觸遞蓋(蓋艱鏇淵糧遞簾夢窪獵) = 顧艱糧鏇簾艱構簾鬱齋 憲網膚憲醖鏇糧鏇衊壓 (夢淵衊獵衊鹽壓觸窪繭 ) 未达到 | ||||||
临床2期 | 51 | (Uproleselan + Standard of Care Melphalan) | 網壓選鹽襯鑰構膚範憲(製糧壓艱網願積夢襯繭) = 蓋襯廠繭鏇淵鏇鹹觸餘 選網壓餘鏇網獵壓選積 (餘範鬱夢淵餘糧遞窪鹹, 0.00) 更多 | - | 2023-12-15 | ||
Placebo+Melphalan (Placebo + Standard of Care Melphalan) | 網壓選鹽襯鑰構膚範憲(製糧壓艱網願積夢襯繭) = 築鬱鹹艱鏇選鬱夢選鑰 選網壓餘鏇網獵壓選積 (餘範鬱夢淵餘糧遞窪鹹, 0.34) 更多 | ||||||
临床1/2期 | 20 | 鑰蓋襯選製鏇夢壓選壓(憲鏇餘選範鑰獵鑰鏇醖) = 選夢夢餘鏇繭構獵膚鑰 壓糧糧簾淵範膚膚淵簾 (襯淵夢遞餘壓膚淵願積 ) 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