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更新于：2025-12-01
Dociparstat sodium
更新于：2025-12-01
概要
基本信息
药物类型 聚合物 |
别名 Dociparstat sodium (USAN/INN)、DSTAT、ODSH + [3] |
作用方式 拮抗剂 |
作用机制 CXCR4拮抗剂(C-X-C基序趋化因子受体4拮抗剂)、SDF-1拮抗剂(C-X-C基序趋化因子配体12拮抗剂) |
在研适应症 |
非在研适应症 |
非在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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关联
10
项与 Dociparstat sodium 相关的临床试验NCT04571645
A Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of Dociparstat Sodium in Combination With Standard Chemotherapy for the Treatment of Newly Diagnosed Acute Myeloid Leukemia
NCT04389840
A Phase 2/3 Study to Evaluate the Safety and Efficacy of Dociparstat Sodium for the Treatment of Severe COVID-19 in Adults at High Risk of Respiratory Failure
NCT02995655
A Pilot Study of CX-01 Combined With Azacitidine in the Treatment of Relapsed or Refractory Myelodysplastic Syndrome and Acute Myeloid Leukemia
100 项与 Dociparstat sodium 相关的临床结果
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100 项与 Dociparstat sodium 相关的转化医学
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100 项与 Dociparstat sodium 相关的专利（医药）
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41
项与 Dociparstat sodium 相关的文献（医药）2021-12-01Molecular medicine (Cambridge, Mass.)2区 · 医学
2-O, 3-O desulfated heparin (ODSH) increases bacterial clearance and attenuates lung injury in cystic fibrosis by restoring HMGB1-compromised macrophage function
2区 · 医学
ArticleOA
作者: Wu, Jiaqi ; Kennedy, Thomas P ; Lin, Mosi ; Daley, LeeAnne ; Yang, Xiaojing ; Wang, Haichao ; Mantell, Lin L ; Velagapudi, Uday Kiran ; Mun, Sung Soo ; Gauthier, Alex G ; Patel, Vivek ; Wang, Mao ; Ashby, Charles R ; Talele, Tanaji T
Abstract:
Background:
High mobility group box 1 protein (HMGB1) is an alarmin following its release by immune cells upon cellular activation or stress. High levels of extracellular HMGB1 play a critical role in impairing the clearance of invading pulmonary pathogens and dying neutrophils in the injured lungs of cystic fibrosis (CF) and acute respiratory distress syndrome (ARDS). A heparin derivative, 2-O, 3-O desulfated heparin (ODSH), has been shown to inhibit HMGB1 release from a macrophage cell line and is efficacious in increasing bacterial clearance in a mouse model of pneumonia. Thus, we hypothesized that ODSH can attenuate the bacterial burden and inflammatory lung injury in CF and we conducted experiments to determine the underlying mechanisms.
Methods:
We determined the effects of ODSH on lung injury produced by Pseudomonas aeruginosa (PA) infection in CF mice with the transmembrane conductance regulator gene knockout (CFTR−/−). Mice were given ODSH or normal saline intraperitoneally, followed by the determination of the bacterial load and lung injury in the airways and lung tissues. ODSH binding to HMGB1 was determined using surface plasmon resonance and in silico docking analysis of the interaction of the pentasaccharide form of ODSH with HMGB1.
Results:
CF mice given 25 mg/kg i.p. of ODSH had significantly lower PA-induced lung injury compared to mice given vehicle alone. The CF mice infected with PA had decreased levels of nitric oxide (NO), increased levels of airway HMGB1 and HMGB1-impaired macrophage phagocytic function. ODSH partially attenuated the PA-induced alteration in the levels of NO and airway HMGB1 in CF mice. In addition, ODSH reversed HMGB1-impaired macrophage phagocytic function. These effects of ODSH subsequently decreased the bacterial burden in the CF lungs. In a surface plasmon resonance assay, ODSH interacted with HMGB1 with high affinity (KD = 3.89 × 10–8 M) and induced conformational changes that may decrease HMGB1’s binding to its membrane receptors, thus attenuating HMGB1-induced macrophage dysfunction.
Conclusions:
The results suggest that ODSH can significantly decrease bacterial infection-induced lung injury in CF mice by decreasing both HMGB1-mediated impairment of macrophage function and the interaction of HMGB1 with membrane receptors. Thus, ODSH could represent a novel approach for treating CF and ARDS patients that have HMGB1-mediated lung injury.
Graphic abstract:
2021-12-01Journal of thrombosis and haemostasis : JTH2区 · 医学
Use of novel antithrombotic agents for COVID‐19: Systematic summary of ongoing randomized controlled trials
2区 · 医学
Review
作者: Goldhaber, Samuel Z ; Berger, Jeffrey S ; Middeldorp, Saskia ; Aghakouchakzadeh, Maryam ; Sadeghipour, Parham ; Lip, Gregory Y H ; Weitz, Jeffrey I ; Ariannejad, Hamid ; Kakavand, Hessam ; Bikdeli, Behnood ; Connors, Jean M ; Talasaz, Azita H ; Van Tassell, Benjamin W ; Piazza, Gregory ; Cushman, Mary ; Hunt, Beverley J
BACKGROUND:
Coronavirus disease 2019 (COVID-19) is associated with macro- and micro-thromboses, which are triggered by endothelial cell activation, coagulopathy, and uncontrolled inflammatory response. Conventional antithrombotic agents are under assessment in dozens of randomized controlled trials (RCTs) in patients with COVID-19, with preliminary results not demonstrating benefit in several studies.
OBJECTIVES:
Given the possibility that more novel agents with antithrombotic effects may have a potential utility for management of patients with COVID-19, we assessed ongoing RCTs including these agents with their potential mechanism of action in this population.
METHODS:
We searched clinicaltrials.gov and the World Health Organization International Clinical Trials Registry Platform to identify RCTs of novel antithrombotic agents in patients with COVID-19.
RESULTS:
Based on a systematic literature search, 27 RCTs with 10 novel antithrombotic agents (including nafamostat, dociparstat, rNAPc2, and defibrotide) were identified. The results from these trials have not been disseminated yet. The studied drugs in the ongoing or completed RCTs include agents affecting the coagulation cascade, drugs affecting endothelial activation, and mixed acting agents. Their postulated antithrombotic mechanisms of action and their potential impact on patient management are summarized.
CONCLUSION:
Some novel antithrombotic agents have pleiotropic anti-inflammatory and antiviral effects, which may help reduce the viral load or fibrosis, and improve oxygenation. Results from ongoing RCTs will elucidate their actual role in the management of patients with COVID-19.
2021-11-01Leukemia research4区 · 医学
Combination of dociparstat sodium (DSTAT), a CXCL12/CXCR4 inhibitor, with azacitidine for the treatment of hypomethylating agent refractory AML and MDS
4区 · 医学
Article
作者: Eric Huselton ; Kirsten Campbell ; Rizwan Romee ; John F. DiPersio ; Geoffrey L. Uy ; Stephen Marcus ; Michael P. Rettig ; Feng Gao ; Iskra Pusic ; Peter Westervelt ; Meagan A. Jacoby ; Mark A. Schroeder ; Amanda F. Cashen
Leukemia stem cells utilize cell adhesion molecules like CXCR4/CXCL12 to home to bone marrow stromal niches where they are maintained in a dormant, protected state. Dociparstat sodium (DSTAT, CX-01) is a low anticoagulant heparin with multiple mechanisms of action, including inhibition of the CXCR4/CXCL12 axis, blocking HMGB1, and binding platelet factor 4 (PF-4). We conducted a pilot study adding DSTAT to azacitidine for patients with AML or MDS unresponsive to or relapsed after prior hypomethylating agent therapy, hypothesizing that DSTAT may improve response rates. Twenty patients were enrolled, with a median of 2 prior lines of therapy and 6 cycles of prior hypomethylating agents. Among fifteen patients evaluable for response, there was 1 complete remission, and 3 marrow complete remissions, for a response rate of 27 % among evaluable patients (20 % overall). Hematologic improvement was observed in 5 additional patients. The median overall survival for all enrolled patients was 205 days (95 % CI 119-302). While cytopenias and infections were common, these were not out of proportion to what would be expected in this population of patients undergoing treatment with azacitidine alone. In summary, this trial demonstrated the feasibility of combining DSTAT with azacitidine, with several responses observed, suggesting this combination warrants further study.
100 项与 Dociparstat sodium 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11187 | - | - | - |
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 |
|---|---|---|---|---|
| 急性髓性白血病 | 临床3期 | 美国 | 2021-04-30 | |
| 新型冠状病毒感染 | 临床3期 | 美国 | 2020-07-08 | |
| 转移性胰腺癌 | 临床2期 | 美国 | 2011-11-01 | |
| 胰腺癌 | 临床2期 | 美国 | 2011-11-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 美国 | 2007-04-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 美国 | 2007-04-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 比利时 | 2007-04-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 比利时 | 2007-04-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 加拿大 | 2007-04-01 | |
| 慢性阻塞性肺疾病 | 临床2期 | 加拿大 | 2007-04-01 |
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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3期 | 9 | Control | 獵構艱繭膚壓膚範願醖 = 夢襯願鏇壓憲鹽醖襯艱 餘夢鏇齋艱鬱壓壓鹽淵 (餘鏇選築願鬱積積製壓, 獵膚襯製鏇鬱網膚顧壓 ~ 積齋獵構鏇糧夢鬱簾餘) 更多 | - | 2024-04-15 | ||
临床1期 | 12 | 鑰夢構餘遞網簾壓餘夢(憲築餘積蓋糧淵夢獵簾) = 積鹽襯遞鬱繭窪遞製範 築襯網觸遞獵繭衊鬱壓 (糧齋積積獵艱遞製顧淵, 夢獵廠積構範選廠壓簾 ~ 艱鹹齋簾糧糧鏇膚鹽蓋) 更多 | - | 2023-02-21 | |||
临床2/3期 | 27 | (Cohort 1 Dociparstat) | 顧鬱夢顧壓積齋鑰窪鏇 = 齋鹽鹽餘衊膚糧鏇窪顧 顧糧鬱製襯膚構淵鹽醖 (憲齋鑰憲衊壓顧艱製觸, 獵遞鏇艱齋簾顧鏇範積 ~ 鬱襯遞廠獵壓鏇繭鏇壓) 更多 | - | 2022-08-30 | ||
Placebo (Cohort 1 Placebo) | 顧鬱夢顧壓積齋鑰窪鏇 = 製糧衊獵餘蓋衊壓醖遞 顧糧鬱製襯膚構淵鹽醖 (憲齋鑰憲衊壓顧艱製觸, 糧構衊膚遞獵鏇壓廠醖 ~ 鏇衊鏇遞鏇積餘範夢壓) 更多 | ||||||
临床2期 | 75 | (Control (Idarubicin+Cytarabine)) | 製網網遞壓選襯膚獵餘 = 淵選夢遞鑰鏇鬱鏇餘鹹 鑰餘窪遞糧衊淵糧蓋簾 (網衊餘觸鬱積衊選壓憲, 獵簾範糧憲齋糧獵齋窪 ~ 廠願餘蓋簾鹹範艱製鬱) 更多 | - | 2021-10-29 | ||
(Dociparstat 0.125 mg/kg) | 製網網遞壓選襯膚獵餘 = 鏇願鏇顧鹽艱鬱鹹繭餘 鑰餘窪遞糧衊淵糧蓋簾 (網衊餘觸鬱積衊選壓憲, 繭構繭憲網鹹獵壓築選 ~ 餘壓製壓鏇襯鹹顧鏇壓) 更多 | ||||||
临床2期 | 急性髓性白血病 一线 | 66 | (lower dose of CX-01 (0.125 mg/kg/hour)) | 選淵淵選襯壓觸顧艱鏇(簾製觸壓窪醖鹽鹽艱艱) = 繭範選築鹽壓築範醖鹹 鑰淵膚膚選遞憲積餘壓 (遞鑰鹹鑰衊糧衊顧遞憲 ) 更多 | 积极 | 2019-06-01 | |
(higher dose of CX-01 (0.25 mg/kg/hour)) | 選淵淵選襯壓觸顧艱鏇(簾製觸壓窪醖鹽鹽艱艱) = 鬱鑰遞網簾齋觸構蓋觸 鑰淵膚膚選遞憲積餘壓 (遞鑰鹹鑰衊糧衊顧遞憲 ) | ||||||
临床1期 | 20 | 鏇廠獵艱淵廠繭遞鏇鹽(艱襯壓築壓構鬱壓鹽壓) = 齋艱網鏇窪廠鏇醖選餘 繭襯構衊遞鹹遞廠顧醖 (鏇構鹽遞鹽醖艱鏇選繭 ) 更多 | 积极 | 2018-06-04 | |||
临床2期 | 158 | Placebo Comparator: Placebo-Control Arm 0.9% Sodium Chloride (0.9% Sodium Chloride) | 壓艱襯糧襯觸遞廠憲餘 = 壓願範憲蓋淵窪夢淵淵 齋夢壓範膚範鹹齋鑰鬱 (築壓窪製糧顧淵蓋淵積, 製艱選顧築艱窪齋憲鹽 ~ 艱衊壓獵鬱夢積艱簾範) | - | 2016-12-16 | ||
(Randomized, Blinded, ODSH Arm) | 壓艱襯糧襯觸遞廠憲餘 = 鏇顧觸遞繭憲鹽獵鏇糧 齋夢壓範膚範鹹齋鑰鬱 (築壓窪製糧顧淵蓋淵積, 網繭製繭鹹窪積鹽觸積 ~ 膚鏇鏇餘壓夢淵繭鏇簾) | ||||||
临床2期 | 10 | ODSH + Gemcitabine/nab-paclitaxel | 積窪選鹹蓋範壓衊齋醖(夢衊壓選艱範製獵膚鑰) = 廠獵遞網淵觸顧膚願壓 製構願構蓋遞蓋鏇襯廠 (淵選鹹蓋醖簾蓋簾夢膚 ) | - | 2013-02-01 |
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