Biologic
UniProt P00742
Andexanet alfa
Andexxa
- Mechanism of action
- Recombinant factor Xa decoy protein (reverses apixaban/rivaroxaban anticoagulation)
- In plain language
- A modified, inactive copy of a natural clotting protein that acts as a decoy, soaking up apixaban or rivaroxaban so the body's own clotting system can work again.
- How it works
- Andexanet alfa is a recombinant, catalytically inactive variant of human coagulation factor Xa engineered to act as a decoy for direct factor Xa inhibitors. Two modifications distinguish it from native factor Xa: the active-site serine is substituted with alanine (Ser195Ala by chymotrypsin numbering), abolishing its ability to cleave and activate prothrombin, and its membrane-binding gamma-carboxyglutamic acid (Gla) domain is removed, preventing assembly into the prothrombinase complex on phospholipid surfaces. Despite lacking catalytic and procoagulant-complex activity, andexanet retains the active-site conformation that apixaban and rivaroxaban recognize, so it binds these factor Xa inhibitors with high affinity and sequesters them away from the patient's endogenous factor Xa, restoring normal thrombin generation and hemostasis.
- Therapeutic applications
- Per FDA-approved labeling, ANDEXXA is indicated for patients treated with rivaroxaban or apixaban, when reversal of anticoagulation is needed due to life-threatening or uncontrolled bleeding. It has not been shown to be effective for, and is not indicated for, the treatment of bleeding related to any factor Xa inhibitors other than apixaban or rivaroxaban.
- Class
- Recombinant decoy protein
- Therapeutic area
- Emergency / Hematology
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