PEGylated Protein Drugs

PEGylated Protein Drugs

Published by BroadPharm on August 20, 2018

Efficiency and effectiveness are key concepts in the development of pharmaceutical drugs. As discussed in the article what are PEG linkers, the pharmaceutical industry is constantly seeking new ways to develop or improve medications using polyethylene glycol (PEG) technology.

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, immunogenicity, are non-antigenic, and have good water-soluble characteristics. A good example of this is Adagen (Figure 1), which is comprised of the protein Adenosine Deaminase that has 11-17 PEG 5K chains. The drug's size is increased due to the PEG chains, which prevents it from renal clearance and extends the lifetime of the drug. Increasing the length of the PEG linker allows for enhanced solubility and decreases the accessibility for proteolytic enzymes and antibodies.

diagram of antibody drug conjugate linker as well as a description
Figure 1. Adagen, shown above, has 11-17 PEG 5K chains attached to the protein's lysine groups that prevents it from renal clearance and extends the lifetime of the drug

Over the past 31 years, there have been approximately a dozen FDA approved PEGylated drugs on the market as seen in Table 1 below. PEGs can be used in conjunction with different macromolecules to treat a wide variety of diseases.

Table 1. The following list of ADCs that have been approved by the FDA as of July 2021.

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 associated with chronic renal failure
CimziaUCB2008Branched 40000Reducing signs and symptoms of Chron's disease
Puricase1 / KrystexxaSavient201010000Gout
SylatronMerck2011Multiple Linear 12,000Melanoma
OmontysTakeda20122 Linear 20,000Anemia
PlegridyBiogen2014Linear 20,000Multiple sclerosis
AdynovateBaxalta2015Multiple Linear 20,000Hemophilia A
JiviBayer Healthcare20172 Branched 30,000Hemophilia A
RebinynNovo Nordisk2017Linear 40,000Hemophilia B
UdenycaCoherus Biosciences2018Multiple Linear 20,000Infection during chemotherapy
PalynziqBioMarin Pharmaceutical20189 Linear 20,000Phenylketonuria
RevcoviLeadiant Bioscience2018Linear 80,000ADA-SCID
FulphilaMylan GmbH2018Linear 20,000Infection during chemotherapy
AsparlasServier Pharma2018Multiple Linear 5,000Leukemia
EsperoctNovo Nordisk2019Linear 40,000Hemophilia A
ZiextenzoSandoz2019Linear 20,000Infection during chemotherapy
NyvepriaPfizer Inc.2020Linear 20,000Neutropenia Associated with Chemotherapy

For more information on the different types of PEG polymer types, please read the article Monodispersed and Polydispersed PEG.

As a leading PEG supplier worldwide, BroadPharm offers over 4,000 different PEG Linkers to empower our customer's advanced research. These compounds feature great aqueous solubility, smart choice of PEG length, linear or branched, and a wide selection of functional groups to choose from.