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Model system for the transcyclization reaction.

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Improving the Stability of Maleimide–Thiol Conjugation for Drug Targeting

Abstract Maleimides are essential compounds for drug conjugation reactions via thiols to antibodies, peptides and other targeting units. However, one main drawback is the occurrence of thiol exchange reactions with, for example, glutathione resulting in loss of the targeting ability. A new strategy to overcome such retro-Michael exchange processes of maleimide–thiol conjugates by stabilization of […]

The next stop for PEGylated protein drugs: Biosimilar

Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor analog filgrastim. It serves to stimulate the level of white blood cells. Pegfilgrastim has a human half-life of 15 to 80 hours, much longer than the parent filgrastim (3–4 hours). Pharma Companies & PEGylated Drug Development Multiple major pharma companies have been busy […]

PEG Reagents for Surface Functionalization of Carbon Nanotubes and Graphenes

PEGylated pyrene derivatives can be used for the surface functionalization of carbon nanotubes and graphenes via the strong (close to irreversible) pi-pi stacking between the pyrene and the aromatic rings on single wall and multi-walled carbon nanotubes. How Surface Functionalization Works Pyrene is conjugated to PEG through a very stable amide bond. It is a […]

FDA-Approved PEGylated Drugs

To date, only eleven PEGylated proteins, antibody fragments, oligonucleotides, and small molecules that have been approved by the FDA are on the market. Available PEGylated Drugs This includes PEGylated bovine adenosine deaminase: pegademase bovine (Adagen); and PEGylated l-asparaginase: pegaspargase (Oncaspar); PEGylated products of interferon-alpha (IFN-alpha): peginterferon-2b (PegIntron) and peginterferon-2a (Pegasys); PEGylated granulocyte colony stimulating factor […]