Long-acting oxyntomodulin formulation and methods of producing and administering same

A pharmaceutical formulation comprising a buffer, a tonicity agent, and a reverse PEGylated oxyntomodulin consisting of an oxyntomodulin, a polyethylene glycol polymer (PEG) and 9-fluorenylmethoxycarbonyl (Fmoc) or sulfo-9-fluorenylmethoxycarbonyl (FMS), wherein said PEG polymer is attached to the amino terminus of said oxyntomodulin via a Fmoc or a FMS linker, or is attached to a lysine residue on position number twelve (Lys 12) or to a lysine residue on position number thirty (Lys30) of said oxyntomodulin's amino acid sequence, via a Fmoc or a FMS linker.

A pharmaceutical composition for a once a week administration to a subject comprising a reverse PEGylated oxyntomodulin consisting of an oxyntomodulin, a polyethylene glycol polymer (PEG) and 9-fluorenylmethoxycarbonyl (Fmoc) or sulfo-9-fluorenylmethoxycarbonyl (FMS), wherein said PEG polymer is attached to the amino terminus of said oxyntomodulin via a Fmoc or a FMS linker, or is attached to a lysine residue on position number twelve (Lys 12) or to a lysine residue on position number thirty (Lys30) of said oxyntomodulin's amino acid sequence, via a Fmoc or a FMS linker;

• and a pharmaceutically acceptable carrier and/or excipient.

A lyophilized reverse PEGylated oxyntomodulin formulation comprising a reverse PEGylated oxyntomodulin, wherein said reverse PEGylated oxyntomodulin consists of an oxyntomodulin, a polyethylene glycol polymer (PEG) and 9-fluorenylmethoxycarbonyl (Fmoc) or sulfo-9-fluorenylmethoxycarbonyl (FMS), wherein said PEG polymer is attached to the amino terminus of said oxyntomodulin via a Fmoc or a FMS linker, or is attached to a lysine residue on position number twelve (Lys 12) or to a lysine residue on position number thirty (Lys30) of said oxyntomodulin's amino acid sequence, via a Fmoc or a FMS linker.