andexanet alfa   Click here for help

GtoPdb Ligand ID: 7576

Synonyms: Andexxa® | coagulation factor Xa (recombinant), inactivated-zhzo | Ondexxya® | PRT064445 | PRT4445 | r-antidote
Approved drug
andexanet alfa is an approved drug (FDA (2018), EMA (2019))
Comment: Andexanet alfa is a recombinant modified human Factor Xa (FXa) protein that acts as a mimetic of endogenous human factor Xa, and which was developed as a universal antidote to reverse thhe anticoagulant effects of direct or indirect FXa inhibitors. Information regarding the invention of andexanet alfa is available in patent WO2009042962 [2].
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Summary of Clinical Use Click here for help
Patients receiving direct factor Xa inhibitor drugs to reduce thrombotic events may have bleeding crises, or may need urgent surgical intervention where the presence of anti-clotting drugs would be problematic. Andexanet alfa was designed to address these issues by effectively and rapidly removing the inhibitor drugs from the blood [4]. In vitro experiments show that andexanet alfa dose-dependently reverses the inhibitory activity of tested small-molecule FXa inhibitors, and in vivo studies show that andexanet alfa is able to restore hemostasis in a rats treated with FXa inhibitors or in a mouse model of blood loss [1].
Preliminary results of a Phase 2 clinical trial (NCT01758432) indicated that andexanet alfa rapidly reversed the action of rivaroxaban in human subjects.
In May 2018, the FDA approved andexanet alfa (Andexxa®) to reverse the anticoagulation effects of rivaroxaban and apixaban, in patients that are experiencing life-threatening or uncontrolled bleeding [3].
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Andexanet alfa acts as a decoy and binds to FXa inhibitors. It binds FXa inhibitor drugs more strongly than it does FXa itself [1]. In this way the recombinant peptide neutralizes the inhibitor drugs in the bloodstream and restores hemostasis.