Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
AssigneePortola Pharmaceuticals, Inc.
InventorsGenmin Lu, Uma Sinha
Life of this patent
Estimating the term…
Abstract
The present invention relates to antidotes of anticoagulants targeting factor Xa which antidotes are used in combination with blood coagulating agents or other heparin antidotes to prevent or reduce bleeding in a subject. The antidotes described herein have reduced or no intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is or will be undergoing anticoagulant therapy with a factor Xa inhibitor.
Claims13
A pharmaceutical composition comprising (i) an isolated polypeptide comprising (a) the amino acid sequence of SEQ ID NO. 12, 13, or 15 or (b) an amino acid sequence having at least 95% sequence identity to SEQ ID NO. 12, 13, or 15, wherein the polypeptide has reduced procoagulant activity compared to wild-type factor Xa and does not assemble into a prothrombinase complex and (ii) a blood coagulating agent or a heparin antidote.
A pharmaceutical composition comprising (i) an isolated two-chain polypeptide comprising the amino acid sequence of SEQ ID NO. 13 or an amino acid sequence having at least 95% sequence identity to SEQ ID NO. 13, wherein the amino acid sequence having at least 95% sequence identity to SEQ ID NO. 13 has reduced procoagulant activity compared to wild-type factor Xa and does not assemble into a prothrombinase complex, and (ii) a blood coagulating agent that has procoagulant, anti-thrombolytic, or anti-fibrinolytic activity or a heparin antidote.
A kit of parts comprising a) an isolated polypeptide comprising (i) the amino acid sequence of SEQ ID NO. 12, 13, or 15 or (ii) an amino acid sequence having at least 95% sequence identity to SEQ ID NO. 12, 13, or 15, wherein the polypeptide has reduced procoagulant activity compared to wild-type factor Xa and does not assemble into a prothrombinase complex;
- and b) a blood coagulating agent or a heparin antidote.
A kit of parts comprising a) an isolated two-chain polypeptide comprising the amino acid sequence of SEQ ID NO. 13 or an amino acid sequence having at least 95% sequence identity to SEQ ID NO. 13, wherein the amino acid sequence having at least 95% sequence identity to SEQ ID NO. 13 has reduced procoagulant activity compared to wild-type factor Xa and does not assemble into a prothrombinase complex, and b) a blood coagulating agent that has procoagulant, anti-thrombolytic, or anti-fibrinolytic activity or a heparin antidote.
Dependencies are inferred from the claim text.