Fondaprinux is sulfated pentasaccharide , an ultra low molecular weight synthetic form of heparain with antithrombotic properties. It is analogous to the pentasaccharide sequence in heparin.
|Mechanism of Action||Fondaprinux Sodium binds antithrombin and induces a conformational change in antithrombin. It inhibits Factor Xa which is the activated form of the coagulation factor thrombokinase (Stuart-Prower factor). By binding to this site, it accelerates the rate at which antithrombin (ATIII) neutralizes Factor Xa. Neutralization of Factor Xa decreases conversion of prothrombin to thrombin. Disruption of the coagulation cascade prevents thrombin formation.|
|Eukaryotic Cell Culture Applications||In vitro, Fondaparinux Sodium was demonstrated to impair thrombin generation in human platelet-poor plasma in a dose-dependent manner. It also inhibited thrombin formation in platelet-rich plasma. Fondaparinux Sodium did not cross-react in vitro with antibodies present in plasma samples associated with heparain-associated thrombocytopenia (Herbert et al, 1997). Monocytes and monocyte-derived microparticles are cell models that play a procoagulant role in acute coronary syndrome by expressing high tissue factor levels, which then trigger thrombin generation. The in-vitro effect of Fondaparinux was compared to Enoxaparin and unfractionated heparin. IC50 values (anti-Xa IU/ml) were 0.59 for activated monocytes and 0.17 for monocyte-derived microparticles (Ben-Hadj-Khalifa et al, 2011).|
|Molecular Formula||C31H43N3O49S8 · 10Na|
|References||Ben-Hadj-Khalifa S (2011) Differential coagulation inhibitory effect of fondaparinux, enoxaparin and unfractionated heparin in cell models of thrombin generation. Blood Coagul.Fibrinolysis.22(5):369-373 PMID 21577096 |
Fu L, Suflita M, and Linhardt RJ (2016 Bioengineered heparins and heparan sulfates. Adv. Drug Deliv. Rev. 97:237-249 PMID 26555370
Frank RD (2005) The synthetic pentasaccharide Fondaparinux reduces coagulation, inflammation and neutrophil accumulation in kidney ischemia-reperfusion injury. J.Thromb. Haemost. 2005 3(3):531-540
Herbert M et al (1997) SR 90107A/Org 31540, a novel anti-factor Xa antithrombotic agent. Cardiovasc. Drug Rev. 15(1):1-26