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US 12,005,144 B2Granted
Lyophilized formulations for factor XA antidote
AssigneeAlexion Pharmaceuticals, Inc.
InventorPhuong M. Nguyen
Life of this patent
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Abstract
The present disclosure relates to solutions and methods of preparing lyophilized formulations of factor Xa (fXa) antidotes. A suitable aqueous formulation suitable for lyophilization can include a fXa antidote, a solubilizing agent, and a stabilizer, wherein the formulation does not collapse during lyophilization.
Claims18
A lyophilized composition prepared by lyophilizing an aqueous formulation, wherein:
- the aqueous formulation comprises a stabilizer, from 25 mM to 110 mM arginine, and a two-chain polypeptide comprising a first chain comprising the amino acid sequence of SEQ ID NO. 4, and a second chain comprising the amino acid sequence of SEQ ID NO. 5, wherein the polypeptide cannot assemble into a prothrombinase complex;
- the aqueous formulation has a pH from 7.7 to 7.9;
- the stabilizer comprises from 5.5% to 7.5% sucrose (w/v);
- and the molar ratio of the stabilizer to the polypeptide is at least 100, and wherein the aqueous formulation does not include mannitol.
1 more element
A lyophilized composition prepared by lyophilizing an aqueous formulation, wherein:
- the aqueous formulation comprises about 45 mM arginine, about 6% sucrose (w/v), 0% mannitol, and a two-chain polypeptide comprising a first chain comprising the amino acid sequence of SEQ ID NO. 4, and a second chain comprising the amino acid sequence of SEQ ID NO. 5, wherein the polypeptide cannot assemble into a prothrombinase complex;
- and the aqueous formulation has a pH of about 7.8.
A lyophilized composition prepared by lyophilizing an aqueous formulation, wherein:
- the aqueous formulation comprises about 100 mM arginine, about 6% sucrose (w/v), 0% mannitol, and a two-chain polypeptide comprising a first chain comprising the amino acid sequence of SEQ ID NO. 4, and a second chain comprising the amino acid sequence of SEQ ID NO. 5, wherein the polypeptide cannot assemble into a prothrombinase complex;
- and the aqueous formulation has a pH of about 7.8.
Dependencies are inferred from the claim text.