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

Name Manufacturer Year of Approval PEG size (Da) Indication
Andagen Enzon 1990 Multiple linear 5000 SCID
Oncaspar Enzon 1994 Multiple linear 5000 Leukemia
PEG-INTRON Schering-Plough 2000 Linear 12000 Hepatitis C
PEGASYS Hoffman-La Roche 2001 Branched 40000 Hepatitis C
Neulasta Amgen 2002 Linear 20000 Neutropenia
Somavert Pharmacia & Upjohn 2003 4-6 Linear 5000 Acromegaly
Macugen Pfizer 2004 Branched 40000 Age-related macular degeneration
Micera Hoffman-La Roche 2007 Linear 30000 Anemia associated with chronic renal failure
Cimzia UCB 2008 Branched 40000 Reducing signs and symptoms of Chron's disease
Puricase1 / Krystexxa Savient 2010 10000 Gout
Sylatron Merck 2011 Multiple Linear 12,000 Melanoma
Omontys Takeda 2012 2 Linear 20,000 Anemia
Plegridy Biogen 2014 Linear 20,000 Multiple sclerosis
Adynovate Baxalta 2015 Multiple Linear 20,000 Hemophilia A
Jivi Bayer Healthcare 2017 2 Branched 30,000 Hemophilia A
Rebinyn Novo Nordisk 2017 Linear 40,000 Hemophilia B
Udenyca Coherus Biosciences 2018 Multiple Linear 20,000 Infection during chemotherapy
Palynziq BioMarin Pharmaceutical 2018 9 Linear 20,000 Phenylketonuria
Revcovi Leadiant Bioscience 2018 Linear 80,000 ADA-SCID
Fulphila Mylan GmbH 2018 Linear 20,000 Infection during chemotherapy
Asparlas Servier Pharma 2018 Multiple Linear 5,000 Leukemia
Esperoct Novo Nordisk 2019 Linear 40,000 Hemophilia A
Ziextenzo Sandoz 2019 Linear 20,000 Infection during chemotherapy
Nyvepria Pfizer Inc. 2020 Linear 20,000 Neutropenia 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.