The targeted therapeutics and imaging agents in Kereos' pipeline are based on proprietary ligand-targeted oil and water nanodroplet technologies. Individual nanodroplets consist of a perfluorocarbon core surrounded by a lipid monolayer. This lipid layer both stabilizes the droplet and provides anchoring sites for targeting ligands and therapeutic payloads. The result is an oil-in-water emulsion of droplets with an average size of 250 – 350 nanometers. Both in terms of size and composition, the emulsion droplets are designed to be both safe and effective using excipients that have been previously studied in humans.
The current ligand being incorporated in the emulsion targets the ανβ3 integrin, a well-known marker for angiogensis associated with cancer, cardiovascular, and auto-immune disease. The targeting ligand allows for delivery of the therapeutic payload to the disease area, at quantities much greater than antibody-based targeting since each nanodroplet contains many copies of the therapeutic payload.
The nanodroplet formuation is highly versatile, and can carry a wide range of therapeutic payloads. Fragile peptide therapeutics can be loaded and safely stored on the nanodroplets until they reach the site of activity. Highly toxic natural products can be safely sequestered within the nanodroplets, resulting in much lower systemic toxicity. Improvements in efficacy and/or toxicity of existing drugs can be achieved by modifying them to be loaded onto nanodroplets, resulting in reformulations with improved performance.
Kereos has incorporated a number of therapeutic payloads onto the nanodroplets, with more efficient delivery of the drug and minimization of side effects.