![]() ![]() ![]() Additionally, 4F-PCC is frequently used off-label to urgently reverse the anticoagulant effects of oral fXa inhibitors. It contains the clotting factors II, VII, IX, and X, and antithrombotic proteins C and S. Ĥ-factor prothrombin complex concentrate (4F-PCC), with trade name Kcentra®, was FDA approved in 2013 for the urgent reversal of oral vitamin-K antagonist associated coagulopathy. ![]() Ciraparantag is an investigational small molecule that binds and inactivates several anticoagulants and is currently undergoing clinical trials for reversal of bleeding associated with fXa Inhibitors. The Phase 3b/4 trial evaluating the safety and efficacy of andexanet alfa, ANNEXA-4, was completed in February 2019. Andexanet alfa, now labeled as inactivated coagulation fXa (recombinant) with trade name Andexxa®, was FDA approved in May of 2018 to reverse apixaban and rivaroxaban. To a greater extent than vitamin K antagonists, controversy exists regarding reversal strategies for oral fXa inhibitors. There may be a reduced risk of intracranial hemorrhage when compared to warfarin, a vitamin K antagonist. The use of fXa inhibitors may increase a patient's risk for bleeding due to their inhibition of the coagulation cascade. Commercially available oral fXa inhibitors in the United States include rivaroxaban, apixaban, edoxaban, and betrixaban. ![]() Conveniently, fXa inhibitors have consistent pharmacokinetic and pharmacodynamic properties that allow for a fixed dosing strategy without obligatory routine laboratory monitoring of anticoagulation effect. FXa inhibitors prevent fibrin clot formation by binding to the active site of coagulation fXa leading to the inhibition of the coagulation cascade. Oral factor Xa (fXa) inhibitors are anticoagulants with demonstrated utility in the treatment and prevention of thromboembolic disease including venous thromboembolism and reduction in the risk of stroke or systemic embolism in patients with nonvalvular atrial fibrillation. ![]()
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