What is the future of PEGylated therapies?

Expert Opin Emerg Drugs. 2015;20(4):531-6. doi: 10.1517/14728214.2015.1113254. Epub 2015 Nov 19.


The tremendous potential of biologic drugs is hampered by short half-lives in vivo, resulting in significantly lower potency than activity seen in vitro. These short-acting therapeutic agents require frequent dosing profiles that can reduce applicability to the clinic, particularly for chronic conditions. Therefore, half-life extension technologies are entering the clinic to enable improved or new biologic therapies. PEGylation is the first successful technology to improve pharmacokinetic (PK) profiles of therapeutic agents and has been applied in the clinic for over 25 years. Over 10 PEGylated therapeutics have entered the clinic since the early 1990 s, and new PEGylated agents continue to expand clinical pipelines and drug patent life. PEGylation is the most established half-life extension technology in the clinic with proven safety in humans for over two decades. Still, it is one of the most evolving and emerging technologies that will be applied for the next two decades.

Keywords: PEGylation; half-life extension; peptide delivery; protein delivery.

MeSH terms

  • Animals
  • Biological Products / administration & dosage*
  • Biological Products / pharmacokinetics
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Drug Design
  • Half-Life
  • Humans
  • Patents as Topic
  • Polyethylene Glycols / chemistry*


  • Biological Products
  • Drug Carriers
  • Polyethylene Glycols