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Nat Rev Drug Discov. 2003 Mar;2(3):214-21.

Effect of pegylation on pharmaceuticals.

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Nektar Therapeutics, 490 Discovery Drive, Huntsville, Alabama 35806, USA.


Protein and peptide drugs hold great promise as therapeutic agents. However, many are degraded by proteolytic enzymes, can be rapidly cleared by the kidneys, generate neutralizing antibodies and have a short circulating half-life. Pegylation, the process by which polyethylene glycol chains are attached to protein and peptide drugs, can overcome these and other shortcomings. By increasing the molecular mass of proteins and peptides and shielding them from proteolytic enzymes, pegylation improves pharmacokinetics. This article will review how PEGylation can result in drugs that are often more effective and safer, and which show improved patient convenience and compliance.

[Indexed for MEDLINE]

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