Half-life extended biotherapeutics

Macromolecular protein and peptide therapeutics have proven effective in treating critical human diseases, and over 200 recombinant protein therapeutics have made their way to the pharmaceutical market over the past few decades, including peptides, coagulation factors, hormones, growth factors, etc.

Figure 1. Overview of approved therapeutic proteins and half-life extended derivatives thereof (Kontermann, R.E. 2016)

By comparison, most of these proteins exhibit terminal half-lives below 1 day and are even cleared from circulation in the range of minutes to a few hours. Due to the rapid clearance, frequent applications of the therapeutic protein are required to achieve therapeutic effects. Currently, many protein-based drug formulations in market are administered intravenously (IV) or subcutaneously (SC), and frequent high-dose administration creates dose-fluctuation-related complications and reduces patient compliance.

Extending the plasma half-life can extend the time between applications, which has been recognized by the pharmaceutical industry. About 15% of approved therapeutic proteins have been modified to extend half-life by attaching molecules to the protein that increase overall size or help with receptor mediated recycling, or manipulate amino acid chains in a way to make it easier towards the aggregate formation, etc. Half-life extension technologies have significantly increased the half-life of proteins in circulation (2-100 folds), improved their overall pharmacokinetic (PK) parameters, and have been successfully applied to a variety of protein therapies including hormones and enzymes to interferon.

Figure 2. Factors that limit residence time of protein in circulation and a few ways to address them (Zaman, R.; et al. 2019)

Our Services

Half-life extension technologies have proven to be very effective in every way. Profacgen has invested a lot of effort in researching new protein formulations for the past decade and has successfully overcome some challenges. We offer multiple half-life extension strategies and perform extensive PK and PD studies on any half-life-extended protein formulation to avoid all the drawbacks and eliminate any unwanted side effects.

• Fc Fusion Protein Production Service
• HSA Fusion Protein Production Service
• Polysialylation Services
• Serum IgG Fusion Service
• XTENylation Service

As a professional protein research expert, Profacgen has forward-looking insights and experienced professionals. With our drug development platform, we offer a variety of protein half-life extension strategies, which can be customized according to protein properties. Our competitive prices and extensive expertise have earned us the trust of our collaborators. Contact us to find out how Profacgen could be of assistance.

References

1. Zaman, R.; et al. Current strategies in extending half-lives of therapeutic proteins. Journal of Controlled Release. 2019.
2. Kontermann, R.E. Half-life extended biotherapeutics. Expert Opin Biol Ther. 2016.