andexanet alfa   

GtoPdb Ligand ID: 7576

Synonyms: Andexxa® | coagulation factor Xa (recombinant), inactivated-zhzo | Ondexxya® | PRT064445 | PRT4445 | r-antidote
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
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
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.