Antidotes for factor xa inhibitors and methods of using the...

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 9/64 (2006.01) A61K 31/4545 (2006.01) A61K 31/5377 (2006.01) A61K 31/715 (2006.01) A61K 31/727 (2006.01) A61K 38/36 (2006.01) A61K 38/48 (2006.01) A61K 39/395 (2006.01) A61K 47/48 (2006.01) A61P 7/02 (2006.01) A61P 7/04 (2006.01) C07H 21/00 (2006.01) C07K 14/00 (2006.01) C07K 16/00 (2006.01) C12N 5/10 (2006.01) C12P 21/00 (2006.01)

Patent

CA 2697583

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.

La présente invention concerne des antidotes dirigés contre les anticoagulants ciblant le facteur Xa. Les antidotes sont des dérivés protéiques du facteur Xa qui se lient aux inhibiteurs du facteur Xa les neutralisant ainsi sensiblement mais qui ne s'intègrent pas dans le complexe prothrombinase. L'activité coagulante intrinsèque des dérivés décrits ici est inexistante ou réduite. L'invention décrit des procédés permettant d'interrompre ou de prévenir des saignements chez un patient en cours de traitement anticoagulant avec un inhibiteur du facteur Xa.

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