In 2013, Belrose Pharma acquired a comprehensive set of drug formulation technologies pioneered by publicly-traded Enzon Pharmaceuticals based on the chemical attachment of polyethylene glycol (PEG) using one of several chemical linkers designed to maximize the activity of a native molecule.
The FDA has approved a number of PEGylated pharmaceutical products since Enzon first pioneered the technique in the 1980s. Cumulative worldwide revenue of all PEGylated pharmaceutical products have exceeded $30 billion.
Currently Marketed PEGylated Pharmaceuticals
PEGASYS®: PEGylated interferon alpha for use in the treatment of chronic hepatitis C and hepatitis B (Hoffmann-La Roche)
Neulasta®: PEGylated recombinant methionyl human granulocyte colony-stimulating factor for severe cancer chemotherapy-induced neutropenia (Amgen)
Permanent PEGylation compounds have included enzymes, peptides and antibodies, with the chemical attachment of PEG used to improve these compounds’ half lives and toxicity profiles, along with other patient benefits achieved by maximizing the inherent biological activity of the native molecules. Currently marketed pharmaceutical products that demonstrate the legacy of Belrose Pharma’s proprietary Permanent PEGylation technology include Adagen®, CIMZIA®, Macugen®, Omontys®, Oncaspar®, PEGASYS®, PegIntron® and Sylatron®.
Watch the video for a compelling look at the timeline for these products’ development.
Permanent PEGylation, by increasing the molecular weight of a molecule, can impart several significant pharmacological advantages over the unmodified form, including:
- Improved drug solubility
- Increased drug stability
- Enhanced protection from product degradation
- Reduced dosage frequency, without diminished efficacy
- Improved side effect profile, including reduced toxicity
- Extended blood plasma half-life