Glycopegylated factor IX

• US 8,404,809 B2
• Filed: 10/23/2009
• Issued: 03/26/2013
• Est. Priority Date: 05/25/2005
• Status: Active Grant

• Current Assignee: Novo Nordisk A/S
• Original Assignee: Novo Nordisk A/S
• Inventors: DeFrees, Shawn, Bayer, Robert J., Bowe, Caryn L., Panneerselvam, Krishnasamy
• Primary Examiner(s): Ha, Julie
• Application Number:
  US12/605,028
• Publication Number:
  US 20100081791A1
• Time in Patent Office: 1,250 Days
• Field of Search: None
• US Class Current: 530/380
• CPC Class Codes: A61K 38/4846 Factor VII (3.4.21.21); Factor IX (3.4.21.22); Factor Xa (3.4.21.6); Factor XI (3.4.21.27); Factor XII (3.4.21.38)
• CPC Class Codes: A61K 47/549 Sugars, nucleosides, nucleotides or nucleic acids
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 7/04 Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
• CPC Class Codes: C12N 9/644 Coagulation factor IXa (3.4.21.22)
• CPC Class Codes: C12Y 304/21022 Coagulation factor IXa (3.4.21.22)

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

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;