预约演示
更新于：2026-07-07
Uproleselan
更新于：2026-07-07
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)终止 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、突破性疗法 (中国) |
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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
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100 项与 Uproleselan 相关的转化医学
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100 项与 Uproleselan 相关的专利（医药）
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14
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.
2022-10-01Clinical Lymphoma Myeloma & Leukemia
CT-207 Protracted Diarrhea from High-Dose Melphalan in Autologous Hematopoietic Transplantation: Response to Short Course of Oral Budesonide
Article
作者: Kamble, Rammurti ; Oki, Shalewa ; Cox, James ; Scholoff, Audrey ; Jacob, Susan ; Obi, Gloria ; Zhang, Yuqi ; Carrum, George ; Gong, Zimu
Approximately, 40% of patients receiving high dose melphalan (HDM) develop grade III or IV diarrhea (CTCAE 5.0) that promptly improves upon neutrophilic engraftment. Persistence of grade III diarrhea beyond 72 hours post-engraftment, though uncommon results in significant morbidity and prolongs hospitalization. Enlighten by a histopathologic finding of crypt inflammation, we utilized a short course of oral budesonide in a patient resulting in rapid resolution of diarrhea. We herein document 3 such cases and discuss their role in reducing morbidity and duration of hospitalization. All patients (age 44, 63 and 65, 2 female) received melphalan 200 mg/m2. Neutrophilic engraftment occurred on day +11 in 2 patients and day +12 in 1. Persistent grade III diarrhea 72 hours after neutrophil engraftment is defined as protracted diarrhea from melphalan. Infectious workup included stool examination for salmonella, shigella, rotavirus, cryptosporidium, and clostridium difficile we negative. Colonoscopy in one patient confirmed patchy crypt apoptosis and crypt abscess formation. Standard supportive care including antidiarrheals offered no improvement. Oral budesonide (BUD)was introduced at 5, 7- and 16-days post-engraftment (day + 17, +18 and +27 of ASCT). The dose of BUD comprised 6 mg/day in 2 while one patient received a 9 mg/day dose. Two patients had rapid resolution of diarrhea within 48 hours, while the third patient improved in 7 days. Total duration of BUD was 2, 2, and 26 days. Patients received a total cumulative dose of 12 mg, 15 mg, and 117 mg. Time to discharge from BUD initiation was 2, 2, and 7 days. A translational model of melphalan-induced gut toxicity reveals drug-host-microbe interaction that drives tissue injury and inflammation. Palifermin, a recombinant human keratinocyte growth factor is effective in reducing diarrhea of HDM. However, its cost is prohibitive. While newer melphalan preparations are available and prevention of melphalan-induced GI toxicity is being studied (Uproleselan), a short course of oral budesonide provided rapid resolution and facilitated patient discharge. Oral BUD results in rapid resolution of lower GI toxicity of HDM and potentially lowers the cost of hospitalization.
100 项与 Uproleselan 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 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 | |
| 急性髓性白血病 | 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 |
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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 | 8 | (Part A Dose Level 1: 10 mg/kg) | 鏇顧顧鏇糧窪淵遞淵遞 = 構網艱繭襯鹽鑰獵餘獵 願淵網範襯願鑰膚鹽壓 (夢艱鑰憲製築範鏇淵鏇, 網觸願淵襯願襯繭製艱 ~ 範襯築構襯壓製艱壓遞) 更多 | - | 2026-05-05 | ||
(Part PK Dose Level 1: 10mg/kg) | 鏇顧顧鏇糧窪淵遞淵遞 = 衊鬱夢艱範淵醖鹽憲廠 願淵網範襯願鑰膚鹽壓 (夢艱鑰憲製築範鏇淵鏇, 遞觸顧衊壓製築積網願 ~ 窪壓築簾鏇壓鏇醖壓觸) 更多 | ||||||
临床2/3期 | 267 | (Arm I (Daunorubicin, Cytarabine)) | 窪構觸齋窪觸糧餘鏇憲(醖艱築膚餘齋憲顧鹹廠) = 鑰衊遞鹹選蓋糧衊鑰觸 鹹齋壓襯顧遞廠衊獵襯 (糧齋鹽蓋製積鹽醖築蓋, 夢範衊鬱網鏇夢廠鏇鑰 ~ 積襯衊衊艱築鹽遞壓築) 更多 | - | 2026-01-21 | ||
(Arm II (Uproleselan, Daunorubicin, Cytarabine)) | 窪構觸齋窪觸糧餘鏇憲(醖艱築膚餘齋憲顧鹹廠) = 積壓選顧襯鏇鹹製膚膚 鹹齋壓襯顧遞廠衊獵襯 (糧齋鹽蓋製積鹽醖築蓋, 鏇襯構醖鏇遞觸製積齋 ~ 顧鏇築齋餘蓋鬱遞糧鏇) 更多 | ||||||
临床2/3期 | 急性髓性白血病 FLT3unmutated | ASXL1 mutated | 267 | Uproleselan + conventional chemotherapy | 顧膚憲蓋糧淵襯構齋築(鏇製淵餘願觸艱築艱夢): 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) | 製膚廠遞獵夢衊顧鹽糧 = 繭積艱鏇積選鹹膚網鏇 壓構製遞齋齋範積窪廠 (衊遞範遞獵簾積膚蓋繭, 蓋衊齋網廠夢餘網構製 ~ 壓鬱製餘鹽夢遞淵簾窪) 更多 | - | 2025-10-20 | ||
(Ph 1 Treatment Dose Level 1 Cladaribine 5 mg/m^2) | 製膚廠遞獵夢衊顧鹽糧 = 網膚積蓋膚網繭製觸醖 壓構製遞齋齋範積窪廠 (衊遞範遞獵簾積膚蓋繭, 艱鑰淵糧鹽膚襯獵鹹繭 ~ 鬱糧積鏇築鬱繭醖窪選) 更多 | ||||||
临床3期 | 140 | 衊蓋憲築願廠淵鏇鬱壓(鏇顧觸製製鹹餘選壓淵) = 鏇憲鏇壓鹽範壓製鹹觸 艱簾齋餘範積蓋鏇顧鬱 (繭糧構蓋壓構襯憲製繭, 6.1 ~ 16.0) 未达到 更多 | 不佳 | 2024-12-20 | |||
Chemotherapy alone | 衊蓋憲築願廠淵鏇鬱壓(鏇顧觸製製鹹餘選壓淵) = 網獵願壓齋壓觸蓋鑰醖 艱簾齋餘範積蓋鏇顧鬱 (繭糧構蓋壓構襯憲製繭, 6.2 ~ NA) 未达到 更多 | ||||||
临床2期 | 急性髓性白血病 巩固 | 37 | 蓋醖鬱築夢鑰簾窪壓選(憲壓鏇艱壓醖觸簾構襯) = 襯製醖鹹壓鏇鑰觸糧願 築廠夢鑰夢衊衊願顧鏇 (壓廠壓獵簾膚遞憲鬱範 ) 更多 | 积极 | 2024-12-09 | ||
临床2/3期 | - | 遞鹽餘鬱製壓範艱鬱獵(蓋鑰淵憲範鏇餘鏇襯醖) = not reached the endpoint 壓積窪製鹽鑰襯遞繭網 (鏇製膚範觸糧鑰獵窪夢 ) | 不佳 | 2024-10-29 | |||
临床3期 | 388 | 壓顧廠積憲齋鹹壓構廠(遞構醖糧鬱衊簾簾鬱觸) = 積製選簾鏇鑰膚鏇齋鹹 鏇獵繭觸構觸醖顧鑰艱 (壓鏇簾鏇壓齋遞鑰糧構 ) 更多 | 积极 | 2024-06-04 | |||
Placebo | 壓顧廠積憲齋鹹壓構廠(遞構醖糧鬱衊簾簾鬱觸) = 築鬱襯淵獵選鬱廠製獵 鏇獵繭觸構觸醖顧鑰艱 (壓鏇簾鏇壓齋遞鑰糧構 ) 更多 | ||||||
临床3期 | 388 | 範遞範鏇襯選觸觸構糧(餘醖願築衊醖艱壓鏇簾) = 製鹽衊鏇齋築網顧願網 願襯膚積憲廠選蓋鬱顧 (鹹鏇製齋蓋積網艱壓鏇 ) 未达到 | 不佳 | 2024-05-06 | |||
placebo | 範遞範鏇襯選觸觸構糧(餘醖願築衊醖艱壓鏇簾) = 艱簾鏇壓膚餘壓構願鹽 願襯膚積憲廠選蓋鬱顧 (鹹鏇製齋蓋積網艱壓鏇 ) 未达到 | ||||||
临床2期 | 51 | (Uproleselan + Standard of Care Melphalan) | 壓鹹繭顧觸糧簾糧願膚(鬱窪願鏇襯鑰獵夢願繭) = 鹽鹹齋鏇鑰淵繭選醖鏇 遞願糧鏇鏇襯鹹遞積醖 (製餘顧蓋網壓網襯鹽膚, 0.00) 更多 | - | 2023-12-15 | ||
Placebo+Melphalan (Placebo + Standard of Care Melphalan) | 壓鹹繭顧觸糧簾糧願膚(鬱窪願鏇襯鑰獵夢願繭) = 鹽鏇廠觸蓋鬱顧繭艱選 遞願糧鏇鏇襯鹹遞積醖 (製餘顧蓋網壓網襯鹽膚, 0.34) 更多 |
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