Protease Stabilized, Pegylated Insulin Analogues
AssigneeNovo Nordisk A/S
InventorsPeter Madsen, Thomas Hoeg-Jensen, Thomas Børglum Kjeldsen, Tina Møller Tagmose
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Abstract
Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K.
Claims13
A PEGylated insulin analogue wherein, in the daughter insulin, at least two hydrophobic amino acids have been substituted with hydrophilic amino acids relative to the parent insulin, wherein the substitutions are within or in close proximity to two or more protease cleavage sites of the parent insulin and wherein such daughter insulin optionally further comprises one or more additional mutations, and wherein the PEG moiety, via a linker, is attached to the ε amino group of the lysine residue in position B29 in said daughter insulin.
Dependencies are inferred from the claim text.