Interferon conjugates

• US 7,201,897 B2
• Filed: 02/27/2003
• Issued: 04/10/2007
• Est. Priority Date: 05/31/1996
• Status: Expired due to Fees

• Current Assignee: Hoffmann-La Roche Incorporated (Roche Holding AG)
• Original Assignee: Hoffmann-La Roche Incorporated (Roche Holding AG)
• Inventors: Bailon, Pascal Sebastian, Palleroni, Alicia Vallejo
• Primary Examiner(s): RUSSEL, JEFFREY E
• Application Number:
  US10/377,892
• Publication Number:
  US 20040030101A1
• Time in Patent Office: 1,503 Days
• Field of Search: 530/351, 530/405, 530/409, 424/85.1, 424/85.4, 424/85.7
• US Class Current: 424/85.7
• 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 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/02 Immunomodulators

Abstract

Physiologically active PEG-IFNα conjugate having a formula as follows:

Claims

1. A PEG-IFNα

2a conjugate having the formula

2. The conjugate of claim 1 wherein the average sum of n and m is about 910.

3. The conjugate of claim 1 wherein one of n and m is 420.

4. The conjugate of claim 1 wherein one of n and m is 520.

5. The conjugate of claim 1 wherein each of n and m is independently 455.

6. A method of inhibiting the proliferation of a cancer cell comprising contacting the cancer cell with the PEG-IFNα

2a conjugate of claim 1.

7. A method of treating a proliferative disorder in an animal comprising the step of administering to the animal a therapeutically effective amount of the PEG-IFNα

2a conjugate of claim 1.

8. The method of claim 7 wherein the animal is a human.

9. The method of claim 7 wherein the proliferative disorder is selected from the group consisting of hairy cell leukemia, chronic myelogenous leukemia and Kaposi'"'"'s sarcoma.

10. The method of claim 7 wherein the proliferative disorder is a renal proliferative disorder.

11. A method of inhibiting the growth or replication of a virus in a plurality of cells comprising the step of contacting one of the cells with the PEG-IFNα

2a conjugate of claim 1.

12. A method of treating a viral infection in an animal comprising the step of administering to the animal a therapeutically effective amount of the PEG-IFNα

2a conjugate of claim 1.

13. The method of claim 12 wherein the animal is a human.

14. A composition comprising the conjugate of claim 1 in an aqueous solution.

15. The composition of claim 14 wherein the PEG-IFNα

2a conjugate is separated by cation exchange chromatography from unmodified IFNα

2a and from PEG-IFNα

2a conjugates having more than one branched polyethylene glycol attached.

16. The composition of claim 14 wherein the composition is free from unmodified IFNα

2a and from PEG-IFNα

2a conjugates having more than one branched polyethylene glycol attached.

17. The composition of claim 14 that is at least about 99% by weight, relative to the amount of the PEG-IFNα

2a conjugate, free from unmodified IFNα

2a and from PEG-IFNα

2a conjugates having more than one branched polyethylene glycol attached.

18. The composition of claim 14 that has about 7% of the antiviral Residual Activity of a composition of a similar amount of unmodified IFNα

-2a when determined in a cell culture bioassay employing Madin-Darby kidney cells challenged with vesicular stomatitis virus.