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Ligand id: 7576
Name: andexanet alfa
View more information in the IUPHAR Pharmacology Education Project: andexanet alfa
|No information available.|
|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 . 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 .
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 .
|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 . In this way the recombinant peptide neutralizes the inhibitor drugs in the bloodstream and restores hemostasis.|