Glycopegylated factor IX
View Patent ↗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.
1. A PEGylated Factor IX protein comprising SEQ ID NO:1 and a glycosyl linking group-linked polyethylene glycol moiety attached to Asn 157, Asn 167 or combinations thereof of SEQ ID NO:1 and having a composition according to 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 linker comprising C(O)NH; and
R′ is a branched poly(ethylene glycol) having a core glycerol moiety and a molecular weight of about 40 kD.