IP Library › Patent Application 14598478
Patent Application
App. No. 14/598,478

Glycopegylated Factor IX

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Quick Facts
Patent No.
US None
App. No.
14/598,478
Abstract

Conjugates between Factor IX and PEG moieties. are disclosed in the present application. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.

Claims (17)

1 .- 5 . (canceled)

6 . A PEGylated Factor IX conjugate comprising a Factor IX peptide and a poly(ethylene glycol) moiety, wherein the poly(ethylene glycol) moiety is attached to the Factor IX peptide via a glycosyl linking group of a glycosyl residue as set forth by the formula:

wherein

R 2 is COOH;

R 3 is H;

R 4 is OH;

D is OH; and

G is R 1 -L-

wherein

L is a substituted heteroalkyl linker comprising C(O)CH 2 NH;

R 1 is the poly(ethylene glycol) moiety, wherein the poly(ethylene glycol) moiety comprises a branched poly(ethylene glycol) having a core glycerol moiety, and wherein the branched poly(ethylene glycol) has a molecular weight of about 40 kDa.

7 . The conjugate according to claim 6 , wherein the Factor IX peptide comprises an amino acid sequence set forth as SEQ ID NO:1.

8 . The conjugate according to claim 7 , wherein the poly(ethylene glycol) moiety is conjugated to the Factor IX peptide at Asn 157 or Asn 167.

9 . A pharmaceutical formulation comprising a PEGylated Factor IX conjugate according to claim 6 and a pharmaceutically acceptable carrier.

10 . A method of stimulating blood coagulation in a mammal, comprising administering to the mammal a PEGylated Factor IX conjugate according to claim 6 .

11 . A method of treating hemophilia, comprising administering to a subject in need thereof an effective amount of a PEGylated Factor IX conjugate according to claim 6 .

12 . The method according to claim 9 , wherein hemophilia is hemophilia B.