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With over a decade of experience and state-of-the-art drug development platforms, Creative Biolabs is confident to offer a series of strategies for the half-life extension of drugs. Our specialized and dedicated team will accelerate the development and potential application of your drugs.

Overview of Glyco-PEGylation Based Half-Life Extension

The size of the drugs and their hydrophobicity make therapeutics prone to kidney filtration and hepatic metabolism. Short half-life and quick elimination are the results of protein pharmacokinetic properties. Over the past few years, there have been tremendous efforts to develop half-life extension technologies for therapeutic drugs. Half-life can be prolonged by various techniques, such as increasing protein size (hydrodynamic volume) and molecular weight. One way is by attaching protein to a moiety, such as polyethylene glycol (PEG). Half-life extension technologies that dramatically enhance half-lives of proteins in circulation (2-100 folds) and improve their overall pharmacokinetic (PK) parameters have been successfully applied on a wide range of therapeutics.

Fig.1 PEGylation-based half-life extension strategy. (Zaman, 2019)

Glyco-PEGylation for Drug Half-Life Extension

PEGylation is considered the most popular protein half-life extension technology for increasing the duration of the effect of therapeutic drugs. PEG itself is an uncharged hydrophilic polymer that is non-biodegradable and non-immunogenic. Highly flexible PEG that is easily attached to therapeutic molecules could increase the molecular weight and hydrodynamic radius of a product. It could improve solubility, increase stability, prevent degradation, and extend circulating half-life to reduce renal clearance.

Creative Biolabs is a leading company with a robust and standardized platform supporting drug research and development. Over the decades, scientists at Creative Biolabs have been professional in developing PEG conjugated drug candidates by modifying and conjugating PEG to other moieties such as the site-specific PEG conjugation to glycans (Glyco-PEGylation). The glycol-PEGylation technology allows selective PEGylation to complex N-glycans, generating a series of drug-PEG derivatives. This method can minimize isoform formations and enhance PEG performance on half-life. The site-specific glyco-PEGylation can enable the extension of half-life without compromising efficacy, and clinical studies have reported a low incidence of adverse effects and suggested that PEG is rapidly eliminated. Long-term treatment of patients with these glyco-PEGylated products has demonstrated their acceptable safety and efficacy, and there are dozens of glyco-PEGylated molecules currently in clinical trials.

In drug development, glycol-PEGylation is an established approach to extending the circulation half-life of therapeutic proteins. This technology is expected to continue playing an essential role in future therapeutic drug development. With extensive experience, Creative Biolabs offers the most suitable solutions in all aspects of drug development and half-life extension strategy. Please contact us for detailed information. We look forward to discussing your inquiry and finding the solution for your needs.

Reference

1. Zaman, R.; et al. Current strategies in extending half-lives of therapeutic proteins. Journal of controlled release. 2019, 301, 176-189.