A unique technology enables improved cancer treatment

Protein kinase inhibitors (PKIs) have been shown to inhibit the growth of cancer, which results in extended survival and the patient most often being treated for several years — in some cases, for life. The majority of the PKIs being marketed contain crystalline forms of the active substances. One generally known problem with these crystalline forms of the products is that they are difficult to dissolve, and their solubility can vary depending on the pH value (acidity) of the stomach, resulting in high absorption variability. This uneven uptake of the drug into the body is, especially pronounced with concomitant administration of pH-increasing drugs such as omeprazole and alongside the ingestion of food. Variability increases the risk of the loss of therapeutic effect, if the drug´s uptake is too low the cancer can accelerate again, and if the uptake is too high the risk of severe side effects often increases.

Xspray Pharma’s technology is especially suited for overcoming many of the shortcomings that PKI substances generally possess. The company produces stable amorphous PKIs that can be easily dissolved and whose absorption is pH-independent, which means a more even uptake of the drug even alongside the ingestion of food or pH-increasing drugs. Moreover, this technology makes it possible to adjust the extent of the drug´s uptake into the body.

Xspray Pharma´s unique technology is compatible with a majority of the  PKI drugs. The company’s new HyNap product candidates are being developed in the same manner as the company’s initial product, Dasynoc™ (HyNap-Dasa). The process is reproducible and reduces the effective development time for future products in the company’s pipeline.

The technology is based on supercritical fluid (SCF) extraction. Molecules in a supercritical state can move quickly, as in a gas, while the ability to dissolve substances is good, as in a liquid. The supercritical fluid is used as an anti-solvent for controlled particle precipitation of Active Pharmaceutical Ingredient (API) with or without the addition of excipients.

The most important aspect of developing an amorphous product is its stability during storage. Amorphous products tend to return to a more stable crystalline state during storage, which can lead to lower solubility, and thus absorption.

Xspray Pharma’s products have been shown to be completely amorphous during long-term storage. In 2020, the Company’s HyNap-Dasa tablets were examined with an extremely sensitive instrument used to detect crystalline material. The analysis showed no traces of crystalline material, which confirms previous studies that have shown that the Company’s HyNap material remains amorphous and without traces of crystallinity for more than two years at room temperature. The Company’s HyNap materials can therefore become products with a long shelf life, which is crucial for Xspray Pharma’s business model.