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Fondaparinux Sodium is the sodium salt of Fondaparinux, a synthetic sulfated pentasaccharide antithrombotic anticoagulant.   It has 5 monomeric sugar units that are identical to the those isolated after cleavage of the polymeric glycosaminoglycan heparin.  The sequence in heparin is thought to form the binding site for the natural anti-coagulant factor antithrombin III (ATIII) as binding to this site increases the anti-coagulant activity of ATIII by a factor of 1000-fold.  Fondaparinux Sodium is a Factor Xa inhibitor.   The compound is sparingly soluble in water.

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    Molecular Formula

    C31H43N3O49S8 · 10Na

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    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.

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    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).





    White to off-white powder





    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

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