Antidotes for factor Xa inhibitors and methods of using the same
AssigneeAlexion Pharmaceuticals, Inc.
InventorsGenmin Lu, David R. Phillips, Patrick Andre, Uma Sinha
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Abstract
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are 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 stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
Claims12
A polypeptide comprising SEQ ID NO:12 or an amino acid sequence having at least 90% sequence identity to SEQ ID NO:12, wherein the amino acid sequence, upon cleavage at the -RKRRKR- (SEQ ID NO:17) linker within the sequence in a cell, produces a two-chain polypeptide comprising a first chain and a second chain, and wherein the two-chain polypeptide (a) has reduced catalytic activity as compared to the wild-type factor Xa protein, (b) is capable of binding to a factor Xa inhibitor and (c) cannot assemble into a prothrombinase complex.
Dependencies are inferred from the claim text.