10
2.3.1 PEGylated Drugs on the Market
PEGylation refers to the covalent conjugation of one or more PEG polymers to a
desired compound (Veronese and Pasut 2005). This methodology was initially
developed to improve the therapeutic index of biopharmaceutical drugs, e.g. proteins and enzymes, and then was extended to applications in low Mw drugs poorly
water soluble (Li et al. 2013). The clinical success of PEG-protein drug gives birth
to six commercialized products such as Pegasys®, PEG-Intron®, Neulasta®,
Somavert®, Micera® and Sylatron® (Table  2.2). PEGylated drugs have demonstrated greater hydrophilicity and biological response to the immune system, which
leads to prolonged circulation time, reduced toxicity of the drug and a decrease in
Table 2.2 FDA-approved PEG drug conjugates
Commercial
name
Company
PEG
molecular
weight
Year of
approval
Conjugated
drug
References
Adagen
Enzon
Linear 5000 Da
1990
Enzyme
Alconcel et al.
(2011)
Oncaspar
Enzon
Liner 5000 Da
1994
Enzyme
Alconcel et al.
(2011)
Doxil
Ortho/
ScheringPlough
Not provided 1995
Liposome
Knop et al.
(2010)
Pegasys
Roche
Branched 40,000 Da
2001
Protein
Alconcel et al.
(2011)
PEG-Intron
ScheringPlough
Linear
12,000 Da
2001
Protein
Alconcel et al.
(2011)
Neulasta
Amgen
Linear
20,000 Da
2002
Protein
Alconcel et al.
(2011)
Somavert
Pfizer
Linear
20,000 Da
2003
Protein
Alconcel et al.
(2011)
Macugen
Pfizer
Branched
40,000 Da
2004
Aptamer
Knop et al.
(2010)
Micera
Roche
Linear
30,000 Da
2007
Protein
Alconcel et al.
(2011)
Cimzia
UCB
Branched
40,000 Da
2008
Anti-TNF-α
Fab’
Alconcel et al.
(2011)
Krystexxa
Savient
10,000 Da
2010
Enzyme
Alconcel et al.
(2011)
Sylatron
Merck
120,00 Da
2011
Protein
Swierczewska
et al. (2015)
Omontys
Affymax/
Takeda
Branched
40,000 Da
2012
Peptide
Swierczewska
et al. (2015)
Movantik
Astra Zeneca/
Nektar
< 1000 Da
2014
Small molecule Swierczewska
et al. (2015)
Adynovate
Baxalta
20,000 Da
2015
Anti-hemophilic
factor VIII
Stidl et al. (2018)
X. Guo et al.