Technology

Significance

Many potent and specific peptides have yet to reach patients due to their inherently short half-lives. Additionally, it is not uncommon that a peptide must be delivered intravenously to see a therapeutic effect. These poor pharmacokinetic properties are mainly due to rapid proteolysis upon injection or removal of the peptide from circulation by the kidney because of the small size of the peptide. Longer-acting versions of peptide-based drugs are clearly needed, and if developed, have the potential to be life-changing therapeutics for patients.

Approach

Extend Biosciences has a platform technology to prolong the half-life and enhance the absorption and bioavailability of peptides and proteins when delivered subcutaneously. The technology adds a small modification to the peptide that does not interfere with the pharmacodynamics of the drug.

Results

Proof-of-concept studies showed that attachment of this proprietary modification extended the half-life of a peptide from 22 minutes to 8 hours. Our technology also improved the absorption and bioavailability of a small, labile protein 675-fold when administered subcutaneously.

Use of this technology would reduce the amount of drug needed for injections, as well as the frequency of injections, and would allow for efficient subcutaneous administration. For patients, these attributes translate to an improved quality of life and a more patient-friendly drug that can be self-administered. For pharmaceutical companies, this broadly applicable technology can transform a lead peptide into a viable therapeutic drug.

Competitive Advantage

Typically, a large fusion protein or PEG molecule is attached to a protein to extend its half-life. However, with a small peptide, this large modification can significantly reduce the function of the peptide. Additionally, these types of modifications do not address the low bioavailability of peptides. Extend Biosciences’ modification is small and does not interfere with the activity of the peptide, and improves both half-life and bioavailability.

Peptides that are susceptible to proteolysis may need to be administered intravenously in a hospital setting. Using Extend Biosciences’ technology, the modified drug could be administered subcutaneously by the patient at home, reducing healthcare costs and improving patient compliance and quality of life.