PEG Functionality —-Guideline for Protein / Peptide Conjugation

The pegylation of bioengineered protein/peptide drugs (hereinafter referred to as PEG-protein drugs) has received intensive attentions. Future broader applications in interferon, insulin, erythropoietin (EPO), interleukin, and growth hormone, are critical to the treatment on severe diseases including malignant tumors, diabetes and cardiovascular diseases, etc..

 PEGylation technology is now widely used for the modification of proteins, peptides, antibody fragments, oligonucleotides, and small molecules, as putative New Molecule Entities (pNMEs).  Among the advantages of PEGylation technology are the following:

       Increased solubility and stability;

       Decreased immunogenicity and toxic profile;

       Optimized pharmacokinetics leading to increased blood circulation of the drug and systemic drug exposure, as well as increased bioavailability for small molecules;

       Increased in vivo efficacy and clinical effectiveness;

       Decreased frequency of administration leading to high patient compliance

So far, about 22 kinds of PEG-drug received U.S. FDA approval to market. The PEG of drugs already on the market showed good therapeutics efficacy, which in turn stimulates the enthusiasm of the major pharmaceutical companies and research institutions PEG. Currently, there are dozens of drugs in clinical or pre-clinical research stage.





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