生物活性 | |||
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描述 | The activated serine protease Factor Xa (FXa), activated by both the intrinsic and the extrinsic pathways, plays a central role in the blood coagulation cascade. FXa catalyzes the conversion of prothrombin tothrombin through the prothrombinase complex[3]. Fondaparinux Sodium is a pentasaccharide inhibitor of antithrombin-dependent factor Xa with IC50 of 40 nM. Subcutaneous doses of 2.5 mg of fondaparinux once daily for at least five days reduced venous thromboembolism risk in patients undergoing surgery for fracture by 56.4 percent[4]. Fondaparinux inhibited endogenous FXa activity in platelet-poor human plasma with IC50 of 11 nM and 19 nM in rat plasma, whereas fondaparinux showed no significant inhibition of platelet-associated thrombin generation at the highest concentration tested (IC50 >300 nM) in rat model of balloon injury[5]. | ||
作用机制 | Fondaparinux Sodium binds to antithrombin and induces a conformational change in the antithrombin molecule, creating an increased affinity for factor Xa and causing a several thousand-fold increase in the inhibition of factor Xa by antithrombin. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01178333 | - | Completed | - | United States, Iowa ... 展开 >> University of Iowa Iowa City, Iowa, United States, 52242 United States, Louisiana Tulane University New Orleans, Louisiana, United States, 70112 United States, Maryland University of Maryland Greenebaum Cancer Center Baltimore, Maryland, United States, 21201 Johns Hopkins Baltimore, Maryland, United States, 21205 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Children's Hospital, Boston Boston, Massachusetts, United States, 02115 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, New York Cornell University New York, New York, United States, 10065 United States, North Carolina University of North Carolina, Chapel Hill Chapel Hill, North Carolina, United States, 27599 Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Case Western Reserve University School of Medicine Cleveland, Ohio, United States, 44106 Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Washington Fred Hutchinson Cancer Research Center Seattle, Washington, United States, 98104 United States, Wisconsin Gunderson Clinic LaCrosse, Wisconsin, United States, 54601 University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Froedtert Milwaukee, Wisconsin, United States, 53201 St. Luke's Medical Center Milwaukee, Wisconsin, United States, 53215 收起 << | |
NCT01178333 | - | Completed | - | - | |
NCT00127855 | Haemophilus Influenzae Type b ... 展开 >> Neisseria Meningitidis 收起 << | Phase 2 | Completed | - | Australia, South Australia ... 展开 >> GSK Investigational Site North Adelaide, South Australia, Australia, 5006 Australia, Victoria GSK Investigational Site Carlton, Victoria, Australia, 3053 Australia, Western Australia GSK Investigational Site Subiaco, Western Australia, Australia, 6018 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.58mL 0.12mL 0.06mL |
2.89mL 0.58mL 0.29mL |
5.79mL 1.16mL 0.58mL |
参考文献 |
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