Introduction: PEGylation is a well-established technology for improving the therapeutic value of drugs by attaching polyethylene glycol (PEG). The first PEGylated enzyme products appeared on the market in the early 1990s; currently, more than 18 PEGylated products have been approved by Food and Drug Administration, which encompass various classes of drug molecules, such as enzymes, interferons, granulocyte colony-stimulating factors, hormones, antibody fragments, coagulation factors, oligonucleotide aptamers, synthetic peptides, and small organic molecules. Areas covered: While PEGylated products mainly comprise biologic drugs, such as recombinant proteins and enzymes, non-biologic drugs have recently emerged as a target for PEGylation. This review focuses on the recent development of PEGylated non-biologic drugs, such as small organic molecules, synthetic peptides, and aptamers. Expert opinion: Several PEGylated versions of anti-cancer drugs, opioid agonists, glucagon-like peptide-1 receptor agonists, and oligonucleotide aptamers are in active development stage, and it is likely that they will have a dramatic impact on the market. Although some safety concerns about PEG in clinical trials have been recently issued, PEGylation is still a commercially attractive proposition as a half-life extension technology for long-acting drug development.
Trial registration: ClinicalTrials.gov NCT01492101 NCT02367820 NCT00520390 NCT02119819 NCT03520972 NCT03604419 NCT00804986 NCT03672604 NCT01089517 NCT01944839 NCT01940900 NCT01940887 NCT00932100 NCT00715455 NCT01872572 NCT01848106 NCT00432770 NCT00632242 NCT00742612 NCT00507338 NCT02397954 NCT00976378 NCT01486797 NCT01521533 NCT01085292 NCT01547897 NCT01372137 NCT01691040 NCT02079896.
Keywords: PEGylation; aptamers; non-biologic drugs; small organic molecules; synthetic peptides.