Emerging PEGylated non-biologic drugs

ABSTRACT

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 identifier: NCT01492101.

Trial registration: ClinicalTrials.gov identifier: NCT02367820.

Trial registration: ClinicalTrials.gov identifier: NCT00520390.

Trial registration: ClinicalTrials.gov identifier: NCT02119819.

Trial registration: ClinicalTrials.gov identifier: NCT03520972.

Trial registration: ClinicalTrials.gov identifier: NCT03604419.

Trial registration: ClinicalTrials.gov identifier: NCT00804986.

Trial registration: ClinicalTrials.gov identifier: NCT03672604.

Trial registration: ClinicalTrials.gov identifier: NCT01089517.

Trial registration: ClinicalTrials.gov identifier: NCT01944839.

Trial registration: ClinicalTrials.gov identifier: NCT01940900.

Trial registration: ClinicalTrials.gov identifier: NCT01940887.

Trial registration: ClinicalTrials.gov identifier: NCT00932100.

Trial registration: ClinicalTrials.gov identifier: NCT00715455.

Trial registration: ClinicalTrials.gov identifier: NCT01872572.

Trial registration: ClinicalTrials.gov identifier: NCT01848106.

Trial registration: ClinicalTrials.gov identifier: NCT00432770.

Trial registration: ClinicalTrials.gov identifier: NCT00632242.

Trial registration: ClinicalTrials.gov identifier: NCT00742612.

Trial registration: ClinicalTrials.gov identifier: NCT00507338.

Trial registration: ClinicalTrials.gov identifier: NCT02397954.

Trial registration: ClinicalTrials.gov identifier: NCT00976378.

Trial registration: ClinicalTrials.gov identifier: NCT00976378.

Trial registration: ClinicalTrials.gov identifier: NCT01486797.

Trial registration: ClinicalTrials.gov identifier: NCT01521533.

Trial registration: ClinicalTrials.gov identifier: NCT01085292.

Trial registration: ClinicalTrials.gov identifier: NCT01547897.

Trial registration: ClinicalTrials.gov identifier: NCT01372137.

Trial registration: ClinicalTrials.gov identifier: NCT01691040.

Trial registration: ClinicalTrials.gov identifier: NCT02079896.

KEYWORDS:

• PEGylation
• non-biologic drugs
• small organic molecules
• synthetic peptides
• aptamers

Author contributions

Eun Ji Park and Jiyoung Choi contributed equally to this work.

Declaration of interest

EJ Park, KC Lee and DH Na have received grants from the National Research Foundation of Korea funded by the Ministry of Science and ICT (NRF-2016R1A2B4006914 and NRF-2018R1A2B3004266). J Choi has received support from the Chung-Ang University Research Scholarship Grants in 2018. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer Disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This research was supported by the Chung-Ang University Research Scholarship Grants in 2018 and the National Research Foundation of Korea (NRF) grant funded by the Ministry of Science and ICT (NRF-2018R1A2B3004266).