Pegylated OXM variants
A composition which includes oxyntomodulin and polyethylene glycol polymer (PEG polymer) linked via a reversible linker such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS) is disclosed. Pharmaceutical compositions comprising the reverse pegylated oxyntomodulin and methods of using same are also disclosed.
1. A homogeneous conjugate represented by the structure of:
wherein R 2 is hydrogen or SO 3 H; or a pharmaceutically acceptable salt thereof.
2. The homogeneous conjugate of claim 1 , wherein said PEG is represented by (CH 2 CH 2 O) n CH 3 , wherein n is 30 (PEG30), 40 (PEG40) or 60 (PEG60).
3. The homogeneous conjugate of claim 1 , wherein said pharmaceutically acceptable salt is a TFA salt, an HCl salt, or an acetate salt.
4. A pharmaceutical composition comprising the conjugate of claim 1 , and a pharmaceutically acceptable carrier.
5. The pharmaceutical composition of claim 4 , wherein said PEG is represented by (CH 2 CH 2 O) n CH 3 , wherein n is 30 (PEG30), 40 (PEG40) or 60 (PEG60).
6. A method of reducing food intake comprising administering to a subject in need thereof the composition of claim 4 .
7. A method of treating obesity comprising administering to a subject in need thereof the composition of claim 4 .
8. A method of reducing body weight comprising administering to a subject in need thereof the composition of claim 4 .
9. A method of increasing energy expenditure comprising administering to a subject in need thereof the composition of claim 4 .
10. A method of reducing food intake comprising administering to a subject in need thereof the conjugate of claim 1 .
11. A method of treating obesity comprising administering to a subject in need thereof the conjugate of claim 1 .
12. A method of reducing body weight comprising administering to a subject in need thereof the conjugate of claim 1 .
13. A method of increasing energy expenditure comprising administering to a subject in need thereof the conjugate of claim 1 .