PEGylated Small Molecule Drugs

PEGylated Small Molecule Drugs

Published by BroadPharm on August 20, 2018

PEGylation has been widely used in pharmaceutical research for the past 50 years, with PEG linkers used for a variety of different applications. One of the exciting types of PEGylation technology is in the development of small molecule drugs.

Some of the problems that are often seen in small molecule drugs include their ability to be easily removed from the body, low solubility, and less target-specificity.

The introduction of monodisperse PEG linkers to small molecule drugs increases the drug's solubility and molecular weight. This may allow an extended drug half-life in the body. The use of monodisperse PEG linkers has also improved drug development with its ability to produce homogeneous PEGylated drugs with a specific molecular weight.

Pharmaceutical companies such as NEKTAR and AstraZeneca have made use of PEG linkers attached to small molecule drugs, as exemplified by Movantik (Naloxol). Naloxol incorporates m-PEG7 entity into the drug to enhance the efficacy and reduce transport across the blood-brain barrier to prevent side-effects in the central nervous system (Figure 1).

diagram of antibody drug conjugate linker as well as a description
Figure 1. Movantik, shown above, is a pegylated derivative of α-naloxol.

Polidocanol (Asclera) is another example of a PEG based drug (Figure 2). Asclera can be used as a local anesthetic, in topical ointment form, or injected to treat varicose veins.

diagram of polidocanol(Asclera)
Figure 2. Asclera, formed by the ethoxylation of dodecanol has been patented by Chemische Fabrik Kreussler for the treatment of varicose veins.

As a leading supplier of biochemical reagents worldwide, BroadPharm offers over 4,000 different PEG Linkers to empower our customer's advanced research. These compounds feature great aqueous solubility, smart choice of PEG length, and a broad selection of functional groups to choose from.

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