Common limits for therapeutic application of peptides and proteins are their chemical instability, their short residence time in blood and their tendency to promote an immunological response. Most of these problems may be solved by linking one or more PEG (polyethylene glycol) molecules to these peptides and proteins (PEGylation). This is achieved due to the combination of increased molecular weight and coverage of epitopes or blockage of sequences prone to enzymatic degradation. In addition, PEGylation enhances protein solubility in aqueous solutions.

Currently available PEGylation technologies produce products which are PEGylated at multiple sites in an uncontrolled manner. This inevitably results in a population of molecules PEGylated in locations which crowd the active centre or binding regions resulting in a net decrease in potency versus the un-PEGylated analogue.

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