SPECIFIC ANTIDOTES TO NEW ORAL ANTICOAGULANTS

Abstract

Safety profiles of the novel oral anticoagulants (NOAC) (rivaroxaban, apixaban, edoxaban, dabigatran) are better than that of warfarin. However, the risk (including lifethreatening) of bleeding is no less than 2.3–3.1% per year. Three specific antidotes to NOAC are currently in different phases of clinical trial and implementation. Idarucizumab is a monoclonal antibody which immediately and completely reverses the anticoagulation effect of dabigatran. Andexanet alfa is a recombinant, modified factor Xa molecule that binds and inhibits the effects of oral and parenteral factor Xa inhibitors (rivaroxaban, apixaban, edoxaban, fondaparinux, heparins). Andexanet is already in 3b Phase, and at the end of 2016 — beginning of 2017 it is expected to be approved for clinical use. Ciraparantag is a small molecule, non-covalently binding to factor Xa inhibitors, and dabigatran (i.e., a universal antidote). Recently, promising results of phase 1 trials involving aripazin were published. The article tells about the practical aspects of the use of antidotes, treatment approaches for life-threatening bleeding during treatment with NOAC.

Keywords

• antidote
• bleeding
• novel anticoagulants
• praxbind
• idarucizumab
• andexanet
• annexa
• ciraparantag
• aripazin
• dabigatran
• rivaroxaban
• apixaban
• edoxaban