Protein heparin conjugates
AssigneeHalzyme Ltd.
InventorAlbert P. Halluin
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Abstract
A pharmaceutical composition is prepared wherein a biologically active conjugated protein is selectively conjugated to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue which has an aldehyde not involved in intramolecular hemiacetal formation. The resulting conjugate has a prolonged half-life as compared to native protein and is able to deliver heparin to the site of clots or to prevent reocclusion within the blood stream. Typical proteins include enzymes such as plasminogen activators, and in particular tissue plasminogen activators, and erythropoietin, hormones, antibodies and the like.
Claims14
A pharmaceutical composition comprising a non-toxic, inert, pharmaceutically acceptable carrier medium in which is dissolved a biologically active selectively conjugated fibrin-specific plasminogen activator wherein the fibrin-specific plasmogen activator is covalently conjugated via at least one of its lysine residues or amino-terminal amines to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue through the aldehyde group of such residue, wherein the half-life of the plasminogen activator is prolonged.
A pharmaceutical composition comprising a non-toxic, inert, pharmaceutically acceptable carrier medium in which is dissolved a biologically active selectively conjugated fibrin-specific plasminogen activator protein, wherein said protein is covalently conjugated via at least one of its lysine residues or amino-terminal amines to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue through the aldehyde group of such residue, wherein the conjugate has a greater half-life than the unconjugated form of the protein.
Dependencies are inferred from the claim text.