Method for increasing the serum half-life of a biologically active molecule
AssigneeChiron Corporation
InventorsRobert J. Drummond, Steve Rosenberg
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Abstract
A method is provided for preparing a biologically active molecule having an increased serum half-life. The method involves conjugating a polymer such as polyethylene glycol to the biologically active molecule. Also provided are polypeptide drugs having an increased serum half-life, e.g., human urokinase plasminogen activator (human “uPA” or “hUPA”) or a fragment or derivative thereof. Pharmaceutical compositions containing such molecules and methods of using them to treat uPA-mediated and uPA receptor-mediated disorders are also provided.
Claims16
A method for preparing a biologically active polypeptide having an increased serum half-life, comprising coupling the polypeptide to a polymer by reacting an aldehyde functionality on the polypeptide with a hydrazide or semicarbazide group on the polymer under reaction conditions effective to promote formation of a conjugated polypeptide, wherein the polypeptide is bound to the polymer through a hydrazone or semicarbazone linkage.
A modified polypeptide comprising a biologically active polypeptide conjugated to a polymer having a hydrazide or semicarbazide group, wherein said modified polypeptide exhibits a proportional increase in serum half-life compared to the unmodified polypeptide which is greater than any proportional decrease in its biological activity compared to the unmodified polypeptide.
Dependencies are inferred from the claim text.