![]() ![]() 6 The recombinant Factor Xa derivative binds to apixaban with high affinity, forming a complex that cannot act on the coagulation cascade it reverses the anticoagulant activity of apixaban, which may be necessitated during emergency surgery or during a major bleeding episode. Once andexanet alfa binds to Factor Xa, it will sequester the Factor Xa inhibitor (apixaban) and reduce its concentration and anticoagulant effects. 4 The GLA domain, which is the membrane bound domain of Factor Xa, is removed in andexanet alfa composition, eliminating prothrombin assembly. It is not catalytically active due to the mutation of a serine to an alanine in the protease catalytic triad. 3 However, apixaban carries a risk of bleeding, and thus development of an antidote is essential.Īndexanet alfa is a recombinant Factor Xa derivative that works by acting as a decoy for Factor Xa inhibitors. Due to its mechanism, apixaban alters the coagulation cascade by decreasing thrombin development and formation. Furthermore, apixaban inhibits prothrombinase activity, which converts prothrombin to thrombin via cleavage, and indirectly inhibits platelet aggregation. 2 Apixaban is a selective inhibitor of both free and bound Factor Xa, a clotting factor composed of serine proteases. ![]() 1Īpixaban received FDA approval in late 2012 to reduce the risk of blood clots in patients with non-valvular atrial fibrillation, leading to reduction in the risk of stroke. ![]() The study demonstrated the effects of andexanet alfa being the proposed antidote to the oral anticoagulant Factor Xa inhibitor: apixaban (Eliquis ©). By: Galina Perel, PharmD Candidate c/o 2016Īndexanet alfa’s has achieved great advancement in part one of the Phase 3 ANNEXA-A study conducted by Portola Pharmaceuticals. ![]()
0 Comments
Leave a Reply. |
AuthorWrite something about yourself. No need to be fancy, just an overview. ArchivesCategories |