Conjugation-stabilized polypeptide compositions

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 11/08 (2006.01) A61K 9/107 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) C07K 1/107 (2006.01) C07K 14/435 (2006.01) C07K 14/62 (2006.01) C07K 17/08 (2006.01) C12N 9/00 (2006.01) C12N 9/96 (2006.01) A61K 9/48 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2162366

A stabilized conjugated peptide complex comprising a peptide conjugatively coupled to a polymer including lipophilic and hydrophilic moieties, wherein the peptide may be insulin, calcitonin, or an enzyme. In a particular aspect, the invention comprises an insulin composition suitable for parenteral, as well as non-parenteral administration, comprising insulin covalently coupled with a polymer including a linear polyalkylene glycol moiety and a lipophilic moiety, wherein the insulin, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced in vivo resistance to enzymatic degradation, relative to insulin alone. The conjugates of the invention are usefully employed in therapeutic as well as non-therapeutic, or diagnostic, applications as shown in the figure.

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