The PEGylated Drug

Efficiency and effectiveness are key concepts in the manufacturing of pharmaceutical drugs. The pharmaceutical industry is constantly seeking new ways to improve medications to allow for better patient consumption. One of the growing advancements in drug development is the PEGylation of these drugs to induce better results for patients.

PEGylation involves the attachment of a PEG linker to a molecule such as a protein or peptide. PEGylated products have been proven to be highly beneficial for both the pharmaceutical and research industries due to their biocompatibility. PEG linkers have been found to have low toxicity and immunogenicity. They also have non-antigenic and water-soluble characteristics. The attachment of the PEG linker to a macromolecule increases the overall molecular weight of a protein or peptide which prevents it from renal clearance and extends the lifetime of the drug. The structure of the attached PEG linker correlates to its properties. For example, the introduction of different functional groups allows for more site-specific reactions between the PEG linker and a drug protein. Increasing the length of the PEG linker allows for enhanced solubility. PEG linkers may come in linear or branched forms.

Over the past 28 years, there have been approximately a dozen FDA approved PEGylated drugs on the market as seen in Table 1 below. PEG linkers have been found to improve the effectiveness of both macromolecule and small molecule drugs. PEG linkers can be used in conjunction with different medications to treat a wide variety of diseases. The addition of a PEG linker to a drug such as Oncasper, which is used to treat cancers such as leukemia, has allowed for better water solubility, decreased proteolysis, increased retention time in the body and reduced antigen detection and elimination compared to non-PEGylated versions of the drug.

BroadPharm manufactures over 2,000 high purity PEG Linkers to meet both pharmaceutical and research needs. Visit the link below to learn more about our product.

FDA-approved PEGylated Drugs  
NameManufacturerYear of ApprovalPEG size (Da)Indication
AndagenEnzon1990Multiple linear 5000SCID
OncasparEnzon1994Multiple linear 5000Leukemia
PEG-INTRONSchering-Plough2000Linear 12000Hepatitis C
PEGASYSHoffman-La Roche2001Branched 40000Hepatitis C
NeulastaAmgen2002Linear 20000Neutropenia
SomavertPharmacia & Upjohn20034-6 Linear 5000Acromegaly
MacugenPfizer2004Branched 40000Age-related macular degeneration
MiceraHoffman-La Roche2007Linear 30000Anemia associte with chronic renal failure
CimziaUCB2008Branched 40000Reducing signs and symptoms of Chron's disease
MovantikAstraZeneca2014339Opioid-induced constipation