Pegylated factor VII glycoforms

• US 8,053,410 B2
• Filed: 02/13/2009
• Issued: 11/08/2011
• Est. Priority Date: 06/21/2002
• Status: Expired due to Fees

• Current Assignee: Novo Nordisk Health Care AG (Novo Nordisk A/S)
• Original Assignee: NOVO Nordisk Biotech Incorporated (Novo Nordisk A/S)
• Inventors: Bjorn, Soren, Klausen, Niels Kristian, Garibay, Patrick William, Behrens, Carsten
• Primary Examiner(s): KAM, CHIH MIN
• Application Number:
  US12/371,156
• Publication Number:
  US 20090227504A1
• Time in Patent Office: 998 Days
• Field of Search: 514/2, 514/12, 530/384, 435/69.1, 435/325, 435/69.6, 435/183, 435/254.1, 435/348, 435/358
• US Class Current: 514/12
• 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 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 7/04 Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
• CPC Class Codes: C07K 14/755 Factors VIII , e.g. factor VIII C (AHF), factor VIII Ag (VWF)

Abstract

The invention concerns a preparation comprising a plurality of Factor VII polypeptides or Factor VII-related polypeptides, wherein the polypeptides comprise asparagine-linked and/or serine-linked oligosaccharide chains, and wherein at least one oligosaccharide group is covalently attached to at least one polymeric group.

Claims

1. A preparation comprising a Factor VII polypeptide comprising SEQ ID NO:

1, wherein the Factor VII polypeptide has (1) a valine substituted with aspartic acid at position 158 of SEQ ID NO;

1, (2) a glutamic acid substituted with valine at position 296 of SEQ ID NO;

1 and (3) a methionine substituted with glutamine at position 298 of SEQ ID NO;

1, and wherein the Factor VII polypeptide comprises one or more oligosaccharide chains, wherein the oligosaccharide chains are selected from the group consisting of asparagine-linked oligosaccharide chains, serine-linked oligosaccharide chains, and combinations thereof, and wherein at least one of said oligosaccharide chains is covalently attached to at least one polyethylene glycol (PEG).

2. A preparation comprising a Factor VII polypeptide comprising SEQ ID NO:

1 or Factor VII related polypeptide, wherein the Factor VII polypeptide has a serine substituted with alanine at position 52 as of SEQ ID NO;

1, wherein the Factor VII polypeptide comprises one or more oligosaccharide chains, wherein the oligosaccharide chains are selected from the group consisting of asparagine-linked oligosaccharide chains, serine-linked oligosaccharide chains, and combinations thereof, and wherein at least one of said oligosaccharide groups is covalently attached to at least one polyethylene glycol (PEG).