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The first crystal structure of human factor Xa was deposited in May 1993. To date, 191 crystal structures of factor Xa with various inhibitors have been deposited in the protein data bank. The active site of factor Xa is divided into four subpockets as S1, S2, S3 and S4. The S1 subpocket determines the major component of selectivity and binding.
A specialist may request a quantitative factor Xa assay in a situation of overdose. [2] Andexanet alfa, a specific antidote to reverse the anticoagulant activity of direct Xa inhibitors in the event of major bleeding, was approved by the FDA in 2018. [9] It is also available in the UK. [10]
Factor Xa was identified as a promising target for the development of new anticoagulants in the early 1980s. In 1987 the first factor Xa inhibitor, the naturally occurring compound antistasin, was isolated from the salivary glands of the Mexican leech Haementeria officinalis. Antistasin is a polypeptide and a potent Xa inhibitor.
Inhibition of factor Xa prevents thrombin activation, thereby preventing clot formation. Thus, Factor Xa is used as both a direct and indirect target of several anticoagulant drugs. For example, the drug Fondaparinux is an indirect inhibitor of factor Xa. Fondaparinux binds to antithrombin III and activates the molecule for factor Xa inhibition.
The methodology of an anti-factor Xa assay is that patient plasma is added to a known amount of excess recombinant factor X and excess antithrombin. If heparin or LMWH is present in the patient's plasma, it will bind to antithrombin and form a complex with factor X, inhibiting it from becoming factor Xa. [ 17 ]
Fondaparinux is a synthetic pentasaccharide factor Xa inhibitor. Fondaparinux binds antithrombin and accelerates its inhibition of factor Xa.. Apart from the O-methyl group at the reducing end of the molecule, the identity and sequence of the five monomeric sugar units contained in fondaparinux is identical to a sequence of five monomeric sugar units that can be isolated after either chemical ...
Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [25] Apixaban has no direct effect on platelet aggregation, but by ...
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [8]Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [11]