Many intravenously delivered Active Pharmaceutical Ingredients (APIs) are insoluble or poorly soluble in water solutions. This has been recognized as a major hurdle in pharmaceutical development since it may cause promising drugs to fail during the development process and limit the application of approved drugs due to poor solubility. According to some estimates, between 70 and 90% of drugs in development are classified as poorly soluble, with approximately 40% of approved drugs similarly affected.
Techniques to improve intravenously drug solubility, such as the use of solvents in the form of polymers or polyoxyl oil derivatives and ethanol, may give rise to acute and delayed adverse effects that can be severe. Adverse effects caused by carriers have been seen as an unpleasant trade off in cancer treatment and may necessitate the routine use of corticosteroid as premedication and slow infusions that limit patient flow in the busy chemotherapy suites.
To meet this unmet medical need and help improve the efficiency of the drug development process, Vivesto has developed and patented its first generation of a drug delivery platform called XR-17. XR-17 increases the solubility of intravenously delivered compounds and enables Vivesto to develop innovative formulations of APIs. This technology has been successfully applied to the development of the market approved drug Apealea. Vivesto is currently working on the development of a second generation drug delivery technology, XR-18, which has shown improved properties.
By combining XR technology platform and an effective active pharmaceutical substance, Vivesto can create innovative and patent-protected drugs that benefit patients.
XR-17 is based on a composite of two derivatives of vitamin A. XR-17 forms particles, or micelles with an API that are just 20 to 60 nanometers in size. A human hair is about 80-100,000 nanometers wide.
Molecules that are poorly soluble in water are enclosed in the micelle core, where they can release into the blood stream once administered. Because XR-17 is well tolerated, it makes treatments involving otherwise insoluble substances possible, without the high risk of the adverse side effects typically associated with commonly used solvents such as hypersensitivity reactions.
Vivesto’s initial focus for XR-17 is within oncology, however the XR-17 drug delivery is not restricted to a specific therapeutic area and can therefore potentially be used for any poorly soluble API.