Antidotes for factor Xa inhibitors and methods of using the same
AssigneePortola Pharmaceuticals, Inc.
InventorsUma Sinha, Genmin Lu, Pamela B. Conley
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Abstract
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor X and factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of reversing anticoagulation, stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
Claims25
An isolated polypeptide comprising the amino acid sequence of SEQ ID NO. 21 or an amino acid sequence having at least 95% sequence identity to SEQ ID NO. 21, wherein the polypeptide has (a) reduced procoagulant activity compared to wild-type factor Xa, (b) is capable of binding to a factor Xa inhibitor, (c) does not assemble into a prothrombinase complex and (d) prevents cleavage of amino acid residues 347-365 from the polypeptide.
An isolated polypeptide comprising the amino acid sequence of SEQ ID NO. 21.
An isolated polypeptide consisting essentially of the amino acid sequence of SEQ ID NO. 21.
Dependencies are inferred from the claim text.