Polymer factor VIII moiety conjugates

  • US 8,143,378 B2
  • Filed: 12/11/2009
  • Issued: 03/27/2012
  • Est. Priority Date: 02/26/2003
  • Status: Active Grant
First Claim
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1. A composition comprising a plurality of conjugates, each conjugate comprising one, two or three water-soluble polymers each covalently attached to a Factor VIII moiety polypeptide via a hydrolytically stable linkage, wherein:

  • (i) the Factor VIII polypeptide is selected from the group consisting of Factor VIII, Factor VIIIa, Factor VIII;

    C, Factor VIII;

    vWF and B-domain deleted Factor VIII;

    (ii) the water-soluble polymer is selected from the group consisting of a poly(alkylene glycol), a poly(oxyethylated polyol), a poly(olefinic alcohol), a poly(vinylpyrrolidone), a poly(hydroxyalkylmethacrylamide), a poly(hydroxyalkylmethacrylate), a poly(saccharide), a poly(α

    -hydroxy acid), a poly(vinyl alcohol), a polyphosphazene, a polyoxazoline, a poly(N-acryloylmorpholine), and combinations thereof; and

    (iii) the composition is bioactive, comprising an in-vitro activity of at least 15% compared to that of a Factor VIII polypeptide composition in unconjugated form.

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