FDA approved PEGylated Products

PEGylation has been the most clinically proven half-life extension technology since the early 1990s, and its safety has been demonstrated in humans for more than 30 years. PEGylated drugs are approved in most countries for intravenous, oral, and dermal use in humans. Currently, PEGylation modification can be used to modify proteins and peptides, oligonucleotides, antibody fragments, organic small molecules, and nanoparticles.

Groups of PEGylated agents based on sizes of PEG and parent drugsFig. 1. Groups of PEGylated agents based on sizes of PEG and parent drugs (Bioeng Transl Med. 2023, 9(1): e10600).

Because most protein drugs, peptide drugs, and chemical drugs are accompanied by some insurmountable problems when exerting their effects, such as short action cycles, large immunogenicity, and toxic and side effects. Polyethylene glycol is neutral, non-toxic, has unique physical and chemical properties and good biocompatibility, and is one of the few chemical substances approved by the FDA for in vivo injection. Therefore, chemically linking activated polyethylene glycol to proteins, peptides, small molecule drugs and liposomes, that is, PEGylation of drug molecules, can effectively increase the biological half-life of drug molecules and reduce their toxic side effects.

Representative PEGylated Drugs

Since 1990, PEGylated biopharmaceuticals have been introduced into the marketplace as drugs for human use. Most are PEGylated proteins and one is a PEGylated aptamer (Macugen®) administered intravitreally. The PEG components of these biopharmaceuticals vary widely in size, branching structure and attachment type. Table 1 marketed PEGylated products.

Functional Group on PEG: Succinimidyl ester; Aldehyde; Maleimide; Biotin; Amine; Azide; Boc/Fmoc; Carboxylic Acid; Cholesterol; DBCO, etc.

FDA Approved PEGylated Therapeutics
EntryTrade NameCompanyParent DrugPEG Size (kDa)PEG TopologyIndicationApproved Year
Macromolecular Drugs
[Pegunigalsidase alfa‐iwx]
Chiesi Farmaceutici S.p.AHuman α‐galactosidase‐A2.3Linear (dual‐functional)Fabry disease2023
Amneal Pharmaceuticals LLCG‐CSF20LinearInfection during chemotherapy2022
Fresenius KabiG‐CSF20LinearInfection during chemotherapy2022
Spectrum PharmaceuticalsG‐CSF3.4Linear (dual‐functional)Infection during chemotherapy2022
AscendisHuman growth hormone (Somatropin)40Branched (4 arms)Growth hormone deficiency2021
[Ropeginterferon alfa‐2b‐njft]
PharmaEssentia CorpInterferon‐α‐2b40Branched (2 arms)Polycythemia vera2021
Pfizer, Inc.G‐CSF20LinearInfection during chemotherapy2020
[Turoctocog alfa pegol]
Novo NordiskCoagulation Factor VIII40Branched (2 arms)Hemophilia A2019
SandozG‐CSF20LinearInfection during chemotherapy2019
[Damoctocog alfa pegol]
Bayer HealthcareCoagulation Factor VIII (B‐domain deleted)60Branched (2 arms)Hemophilia A2018
BioMarin PharmaceuticalPhenylalanine ammonia‐lyase20LinearPhenylketonuria2018
Leadiant BioscienceAdenosine deaminase5.6LinearADA‐SCID2018
[Calaspargase pegol‐mknl]
Servier PharmaL‐asparaginase5LinearAcute lymphoblastic leukemia2018
Mylan GmbHG‐CSF20LinearInfection during chemotherapy2018
Coherus BiosciencesG‐CSF20LinearInfection during chemotherapy2018
[Nonacog beta pegol]
Novo NordiskCoagulation Factor lX40Branched (2 arms)Hemophilia B2017
[Rurioctocog alfa pegol]
BaxaltaCoagulation Factor VIII (ADVATE)20Branched (2 arms)Hemophilia A2015
[Peginterferon beta‐1a]
BiogenInterferon β‐1a20LinearMultiple sclerosis2014
[Peginterferon alfa‐2b]
Horizon PharmaUrate oxidase10LinearChronic gout2010
[Certolizumab pegol]
UCB, Inc.anti‐TNFα Fab'40Branched (2 arms)Crohn's Disease, Rheumatoid arthritis, Psoriatic arthritis, Ankylosing spondylitis2008
[Methoxy polyethylene glycol‐epoetin beta]
RocheErythropoietin30LinearAnemia associated with chronic kidney disease2007
PfizerHuman growth hormone5LinearAcromegaly2003
AmgenG‐CSF20LinearInfection during chemotherapy2002
[Peginterferon alfa‐2a]
RocheInterferon‐α‐2a40Branched (2 arms)Chronic hepatitis C, Chronic hepatitis B, Cirrhosis and compensated liver disease, CHC/HIV coinfection2002
[Peginterferon alfa‐2b]
ScheringInterferon‐α‐2b12LinearChronic hepatitis C2001
EnzonL‐asparaginase5LinearAcute lymphoblastic leukemia1994
[Pegademase bovine]
EnzonAdenosine deaminase5LinearADA‐SCID1990
Small molecules
Apellis Pharmaceuticals, Inc.Complement C3 inhibitor peptide40Linear (dual‐functional)Geographic atrophy secondary to AMD2023
Apellis Pharmaceuticals, Inc.Complement inhibitor peptide40Linear (dual‐functional)Paroxysmal nocturnal hemoglobinuria2021
AstraZenecaNaloxone0.323LinearOpioid‐induced constipation2014
TakedaErythropoietin mimetic peptide40Branched (2 arms)Anemia due to chronic kidney disease2012
[Pegaptanib sodium]
PfizerRNA aptamer40Branched (2 arms)Neovascular (wet) age‐related macular degeneration2004
Nanoparticles/ Liposomes
[COVID‐19 Vaccine, mRNA]
ModernamRNA in LNPs2Linear (on NPs)COVID‐192022
[COVID‐19 Vaccine, mRNA]
BioNTech/PfizermRNA in LNPs2Linear (on NPs)COVID‐192021
Alnylam PharmaceuticalssiRNA in LNPs2Linear (on NPs)Polyneuropathy of hereditary transthyretin‐mediated amyloidosis2018
[Irinotecan liposome]
Merrimack PharmaceuticalsIrinotecan in liposome2Linear (on NPs)Metastatic adenocarcinoma of the pancreas post gemcitabine treatment2015
[Doxorubicin HCl liposome]
ScheringDoxorubicin in liposome2Linear (on NPs)Ovarian cancer, Multiple myeloma, AIDS‐related Kaposi's Sarcoma1995

What are the Examples of PEGylated Drugs?

Adagen® & Oncaspar®

First 2 marketed PEG protein products through PEGylation technique are pegademase (Adagen®) and pegaspargase (Oncaspar®), which results in a stable amide linkage of multiple PEGs attached to the protein ε-lysines. Information on toxicities of these two pharmaceuticals was not available on the FDA web pages.


Krystexxa® (Pegloticase) is mammalian engineered uricase (urate oxidase) used to treat gout. Humans do not naturally have the enzyme, and nonmammalian sources of the enzyme are highly immunogenic. PEGylation of the mammalian-derived enzyme may reduce some of the immunogenicity but does not eliminate it completely.



PEG-Intron®, a mono-PEGylated INF-a2b, is synthesized by using a succinimidyl carbonate PEG with 12 kDa. The mPEG reagent forms a covalent carbamate and/or urethane linker with amine groups on the protein. The PEG-Intron® consists of 14 positional isomers and the distribution of positional isomers is dependent on the PEGylation reaction pH value.



Pegasys® (PEG INF-a2a) is mono-PEGylated with a single 40-kDa branched PEG, consisting of 4 major positional isomers, Lys31, Lys121, Lys131, and Lys134, which is approved for the treatment of patients with chronic hepatitis C or chronic hepatitis B. The branching PEG structure, as shown on the right, was achieved by using lysine to link the 2 PEG chains.



Mircera® (mPEG-Epoetin Beta)is a mono-PEGylated extended half-life version using mPEG succinimidyl butanoate (30 kDa PEG). PEGylation occurs primarily at Lys 52 and Lys 56.


Omontys® (Recalled in 2014)

Omontys® (Peginesitide), is a PEGylated peptide that has no sequence homology to erythropoietin. It consists of 2 identical 21 amino acid chains peptides, covalently bound via a linker to a 40-kDa lysine branched PEG for a 45 kDa overall size. The structure of Omontys® is unique in that a linker comprised iminodiacetic acid and b alanine is used to connect the 2 peptides creating a peptide dimer. The peptide dimer is then connected by a single coupling point to the branches, which guarantee the construction of the linker only have one positional isomer.


Macugen® (Pegaptanib) is a PEGylated 28 nucleotide aptamer for intravitreal treatment of wet age-related macular degeneration in the eye. Aptamers generally have a short half-life in vivo as they are subject to cleavage by nucleases. PEG, in this case, is a good modifier to make them suitable for a pharmaceutical product. The candidate which was most effective at inhibiting in vivo vascular leakage (guinea pig model) was chosen for PEGylation with a single 40-kDa lysine branched PEG attached to an amine at the 5' end.


Neulasta® (Pegfilgrastim) is a PEGylated form of recombinant human granulocyte colony-stimulating factor (GCSF) and was approved for the treatment of neutropenia. Neulasta® is made with 20-kDa PEG and application of aldehyde chemistry using selective N terminal amine conjugation at low pH.


Plegridy® (Peginterferon Beta-1) is an INF beta-1a to which a single, linear 20 kDa mPEG-O-2-methylpropionaldehyde molecule (as shown in the right) is covalently attached to the α-NH2 group of amino acid residue via reductive amination with sodium cyanoborohydride. The non-PEGylated IFN b-1a is also marketed under the name Avonex® (IFN b-1a) for the same indication.



Cimzia® (Certolizumab Pegol) has an engineered thiol for PEGylation, which is the only thiol-engineered PEG conjugate currently marketed. Coupling chemistries that bind PEG to free thiol groups in the protein yield a disulfide linked conjugate. Thiol-reactive agents may provide site-selective PEGylation limiting the number of positional isomers.

	Cimzia

PEG Modification Process

Step1: Before performing PEG modification, you need to find high-purity PEG raw materials and then modify them.

Step2: Activate PEG. PEG modification of proteins is mainly achieved through the reaction of PEG terminal hydroxyl groups with protein amino acid residues. However, PEG terminal hydroxyl groups have very poor activity, so they must be activated with an activator to covalently modify proteins under mild conditions in the body.

Step3: Select appropriate protein amino acid residue sites or small molecule drug sites for site-directed modification. Use activated PEG to carry out site-specific modification of appropriate protein amino acid residues to improve the efficacy of natural proteins.

Step 4: After obtaining the PEG-drug complex, in order to avoid other impurities contained in the complex from adversely affecting the drug efficacy, it is separated and purified to obtain a single complex.

PEG Derivatives by Functional Groups

BOC Sciences offers a variety of PEG products modified with different functional groups to meet specific research needs. Some common functional groups that can be incorporated into PEG molecules include carboxylic acid (-COOH), amine (-NH2), thiol (-SH), and hydroxyl (-OH). For example, BOC Sciences offers PEG products modified with carboxylic acid groups that can be used to conjugate to molecules containing amine groups through the formation of amide bonds. These PEG products can be used in drug delivery systems, protein conjugation, and surface modification of nanoparticles. Similarly, PEG products modified with amine groups can be used to conjugate molecules containing carboxylic acid groups through the formation of amide bonds. These PEG products are commonly used in protein labeling, drug delivery, and bioconjugation applications.


  1. Gao, Y. et al. PEGylated therapeutics in the clinic. Bioeng Transl Med. 2023, 9(1): e10600.
  2. Hamidi, M. et al. Pharmacokinetic consequences of pegylation. Drug delivery. 2006, 13(6): 399-409.
  3. Turecek, P.L. et al. PEGylation of biopharmaceuticals: a review of chemistry and nonclinical safety information of approved drugs. Journal of pharmaceutical sciences. 2016, 105 (2): 460-475.
  4. Dozier, J.K. et al. Site-specific PEGylation of therapeutic proteins. International journal of molecular sciences. 2015, 16(10): 25831-25864.

Why BOC Sciences?

  • Large Stock

    More than 2000+ products in inventory

  • Global Delivery

    Warehouses in multiple cities to ensure fast delivery

  • mg to kg

    Multi specification for academic research and industrial production

  • 24/7 Technical Support

    Strict process parameter control to ensure product quality



Our Feature

BOC Sciences supplies a unique variety of PEG derivatives and functional PEG polymers. Our products offer the most diverse collection of reactivity, ready-to-use functionality, and molecular weight options that you will not find anywhere else.

  • Our Feature icon1
  • Our Feature icon2
  • Our Feature icon3
  • Our Feature icon4
PEGylation of Peptides and Proteins

PEGylation of Peptides
and Proteins

Reduce the Immunogenicity of Peptide/Protein Drugs

Learn More



PEG linkers For Drug

Improved Circulation Half-Life

Learn More

Have Customer Reviewed On Us?


Chat With Us

Online Inquiry

Verification code

Copyright © 2024 BOC Sciences. All rights reserved.