• Postgraduate medicine · Nov 2014

    Review

    Reversal agents in development for the new oral anticoagulants.

    • James Costin, Jack Ansell, Bryan Laulicht, Sasha Bakhru, and Solomon Steiner.
    • Perosphere Inc., Danbury, CT. j.costin@perosphere.com.
    • Postgrad Med. 2014 Nov 1; 126 (7): 19-24.

    AbstractThe new oral anticoagulants have many advantages over vitamin K antagonists, but they are still associated with a troublesome incidence of major bleeding. Additionally, the absence of a reversal agent for the new oral anticoagulants is a barrier to their more widespread use. Currently, there are 3 potential reversal agents in development: idarucizumab is a humanized murine monoclonal antibody fragment directed specifically at dabigatran; andexanet alfa is a recombinant modified decoy factor Xa that binds to factor Xa inhibitors; and PER977 is a small molecule that binds to factor Xa and IIa inhibitors and to heparin-based anticoagulants through charge interaction. These agents have undergone phase I clinical testing, appear to be well tolerated in healthy volunteers, and are effective in neutralizing their respective targets. All 3 are currently undergoing or entering into a phase II or III clinical study. This article reviews the available data for idarucizumab, andexanet alfa, and PER977.

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