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Details for Patent: 8,258,262

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Details for Patent: 8,258,262

Title:N-terminally chemically modified protein compositions and methods
Abstract: Provided herein are methods and compositions relating to the attachment of water soluble polymers to proteins. Provided are novel methods for N-terminally modifying proteins or analogs thereof, and resultant compositions, including novel N-terminally chemically modified G-CSF compositions and related methods of preparation. Also provided is chemically modified consensus interferon.
Inventor(s): Kinstler; Olaf B. (Thousand Oaks, CA), Gabriel; Nancy Elise (Thousand Oaks, CA), Farrar; Christine E. (Newbury Park, CA), DePrince; Randolph B. (Raleigh, NC)
Assignee: Amgen Inc. (Thousand Oaks, CA)
Filing Date:Dec 16, 2009
Application Number:12/639,398
Claims:1. A substantially homogenous preparation of N-terminally chemically modified granulocyte colony stimulating factor (G-CSF) or analog thereof, optionally in a pharmaceutically acceptable diluent, carrier or adjuvant, wherein a water soluble polymer attached to the G-CSF N-terminus via an amine linkage.

2. A preparation of claim 1 where said water soluble polymer is selected from the group consisting of dextran, poly(n-vinyl pyrrolidone), polyethylene glycols, polypropylene glycol homopolymers, polypropylene oxide/ethylene oxide co-polymers, polyoxyethylated polyols and polyvinyl alcohols.

3. A preparation of claim 2 where said water soluble polymer is polyethylene glycol.

4. A preparation of claim 3 wherein said polyethylene glycol has a molecular weight of between about 2 kDa and 100 kDa.

5. A preparation of claim 4 wherein said polyethylene glycol has a molecular weight of between about 6 kDa and 25 kDa.

6. A preparation of claim 1 wherein said preparation is comprised of at least 90% N-terminally monopegylated G-CSF or analog thereof and at most 10% unpegylated G-CSF or analog thereof.

7. A preparation of claim 6 wherein said preparation is comprised of at least 95% N-terminally monopegylated G-CSF or analog thereof and at most 5% unpegylated G-CSF or analog thereof.

8. A preparation of claim 1 wherein said G-CSF has the sequence identified in SEQ. ID No. 2.

9. A substantially homogenous preparation of N-terminally monopegylated granulocyte colony stimulating factor (G-CSF), optionally in a pharmaceutically acceptable diluent, carrier or adjuvant, wherein: (a) said G-CSF has the amino acid sequence identified in SEQ. ID No. 2; and (b) said G-CSF is monopegylated with a polyethylene glycol moiety having a molecular weight of about 12 kDa.

10. A pharmaceutical composition comprising: (a) a substantially homogenous preparation of monopegylated granulocyte colony stimulating factor (G-CSF), said monopegylated G-CSF consisting of a polyethylene glycol moiety having a molecular weight of about 12 kDa connected to a G-CSF moiety solely at the N-terminus thereof via an amine linkage; (b) fewer than 5% non-pegylated G-CSF molecules; and (c) a pharmaceutically acceptable diluent, adjuvant or carrier.

11. A method of treating a hematopoietic disorder comprising administering a therapeutically effective dose of a preparation of claim 1.

12. A method of attaching a polyethylene glycol molecule to a granulocyte colony stimulating factor (G-CSF) molecule, wherein said polyethylene glycol molecule has a single reactive aldehyde group, said method comprising: (a) reacting said G-CSF with said polyethylene glycol molecule under reducing alkylation conditions, at a pH sufficiently acidic to selectively activate the .alpha.-amino group at the amino terminus of said G-CSF; and (b) obtaining the pegylated G-CSF and (c) optionally, separating the pegylated G-CSF from non-pegylated G-CSF.

13. A method of claim 12 wherein said polyethylene glycol molecule has a molecular weight of about 6 kDa to about 25 kDa.

14. The peyglated G-CSF product produced by the process of claim 12.
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