PEGylation - PEGylated Pharmaceuticals On The Market

PEGylated Pharmaceuticals On The Market

The clinical value of PEGylation is now well established. ADAGEN (PEG- bovine adenosine deaminase) manufactured by Enzon Pharmaceuticals, Inc., US was the first PEGylated protein approved by the U.S. Food and Drug Administration (FDA) in March 1990, to enter the market. It is used to treat X-linked severe combined immunogenicity syndrome, as an alternative to bone marrow transplantation and enzyme replacement by gene therapy. Since the introduction of ADAGEN, a large number of PEGylated protein and peptide pharmaceuticals have followed and many others are under clinical trial or under development stages. Sales of the two most successful products, Pegasys and Neulasta, exceeded $5 billion in 2011. All commercially available PEGylated pharmaceuticals contain methoxypoly(ethylene glycol) or mPEG. PEGylated pharmaceuticals currently on the market (in reverse chronology by FDA approval year) include:

• Omontys: (PEGinesatide) - once-monthly medication to treat anemia associated with chronic kidney disease in adult patients on dialysis (Affymax/Takeda Pharmaceuticals, 2012)

• Pegloticase (Krystexxa) - PEGylated uricase for the treatment of gout (Savient, 2010)

• Cimzia: (Certolizumab Pegol) - for treatment of moderate to severe rheumatoid arthritis and Crohn's disease, an inflammatory gastrointestinal disorder (Nektar/UCB Pharma, 2008)

• Mircera: PEGylated form of erythropoetin to combat anemia associated with chronic kidney disease (Roche, 2007)

• Macugen: (Pegaptanib) - used to treat neovascular age-related macular degeneration (Pfizer, 2004)

• Neulasta: PEGylated recombinant methionyl human granulocyte colony-stimulating factor for severe cancer chemotherapy-induced neutropenia (Amgen, 2002)

• Somavert: (PEG-human growth hormone mutein antagonist) - for treatment of Acromegaly (Pfizer, 2002)

• PEGASYS: PEGylated interferon alpha for use in the treatment of chronic hepatitis C and hepatitis B (Hoffmann-La Roche, 2001)

• Doxil/Caelyx: PEGylated liposome containing doxorubicin for the treatment of cancer (Ortho Biotech / Schering-Plough, 2001)

• Pegintron: PEGylated interferon alpha for use in the treatment of chronic hepatitis C and hepatitis B (Schering-Plough / Enzon, 2000)

• Oncaspar: PEGylated L-asparaginase for the treatment of acute lymphoblastic leukemia in patients who are hypersensitive to the native unmodified form of L-asparaginase (Enzon, 1994). This drug was recently approved for front line use.

• Adagen: (PEG-adenosine deaminase) - for the treatment of Severe Combined Immunodeficiency Disease (SCID) (Enzon, 1990)