What are the advantages of using monodisperse PEG in drug development?

Monodispersed PEG linkers are pure compounds with a single molecular weight. In contrast, polyPEG linkers contain variations in molecular weight with an average molecular weight. The use of polyPEG linkers in drug development has led to problems in biological applications due to steric hindrance and binding.1

With advancements in both synthetic and purification chemistry over the past two decades, monodispersed PEG linkers have become more commercially viable.  Monodispersed PEG linkers have been found to be beneficial in drug design, specifically in small molecule drugs. Some of the problems that are often seen in small molecule drugs include its ability to be easily removed from the body, low solubility and less target-specificity.2 The introduction of monodispersed 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.3 The use of monodispersed PEG linkers has also improved drug development with its ability to produce homogeneous PEGylated drugs with a specific molecular weight.

Figure 1: Chemical structure of Movantik. Movantik is used for to reduce the occurrence of OIC and OBD upon the consumption of opioids for pain management.

Pharmaceutical companies such as NEKTAR and AstraZeneca have made use of attached PEG linkers to small molecule drugs. OBD and OIC medications such as Movantik (naloxol) incorporate monodispersed PEG linkers to enhance the efficacy of the drug. Movantik includes an m-PEG7 linker. The introduction of this linker to Movantik reduced transport across the blood-brain barrier preventing side-effects to the central nervous system.

ADC Bio
MabPlex
Lonza
 

 


Reference

1 Povoski, Stephen P et al. “Single Molecular Weight Discrete PEG Compounds: Emerging Roles in Molecular Diagnostics, Imaging and Therapeutics.” Expert review of molecular diagnostics 13.4 (2013): 315–319. PMC. Web. 6 July 2018.

2 Pasut, Gianfranco, Veronese, Francesco M., Drug Discovery 10, 21 (2005).

3 Swierczewska, Magdalena, Kang Choon Lee, and Seulki Lee. “What Is the Future of PEGylated Therapies?” Expert opinion on emerging drugs 20.4 (2015): 531–536. PMC. Web. 6 July 2018.

 

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David Zhang, PhD
BroadPharm® is a leading customer-focused biotech company in San Diego, California. We are dedicated to manufacturing and supplying high purity PEG linkers, Click Chemistry Reagents and advanced Bio-labeling reagents such as Dye Labeling and Biotin Labeling compounds to our clients worldwide. In addition, we also offer IP-protected custom synthesis for our clients in the pharmaceutical and biotech industries. We provide timely technical support to address our client’s need and offer technical advice for the best use of our new products.Founded in 2009, BroadPharm® takes our customer needs as our highest priority. We have over 2,000 discrete, high purity PEG reagents in stock which can be shipped to our clients immediately.PEG is an abbreviation for Polyethylene Glycol which consists of repeating ethylene oxide units. Unlike traditional PEGs, all of BroadPharm®’s PEG products represent a specific, single chemical structure with high purity. Each product is synthesized and purified using BroadPharm®’s proprietary advanced technology and characterized by modern NMR and LC/MS.BroadPharm®’s PEG products offer many advantages over traditional linkers such as increased water solubility, reduced aggregation and low immunogenicity. These PEG reagents have been widely used in bioconjugation, antibody-drug conjugates (ADCs) therapeutic, drug delivery and diagnostics field.With our strong expertise in modern chemistry, innovative & novel PEG technology and state-of-the-art equipment, BroadPharm® can help our customers to accelerate their research through cost-effective and efficient solutions.