On May 8, 2014 XSpray Microparticles reproted that its proprietary HyNap formulation of nilotinib demonstrated significantly improved uptake and reduced food interaction in a Phase I clinical trial compared to previously reported data for the commercial available formulation of nilotinib (Press release XSpray, MAY 8, 2014, View Source [SID:1234500494]).
Protein kinase inhibitors (PKI) are used in the treatment of cancer and inflammation. Food interaction is a common problem with this class of drugs and to have control of the uptake from the gastrointestinal tract into the blood stream, patients are often restricted to be fasting in connection with administration. According to the drug label for the marketed PKI nilotinib, patients need to refrain from food intake for two hours before and one hour after administration of the drug. Several PKIs also suffers from pH dependent absorption which demand patients not to use acid reducing agents together with the PKI treatment.
In the completed cross-over Phase I clinical trial, XSpray measured the exposure of its proprietary HyNap formulation of nilotinib in healthy individuals. When administered in the fasted state, a HyNap nilotinib dose of 150 mg produced the same AUC values as those reported for a dose of 400 mg of the marketed product. After a high-fat meal the study showed an increase in drug exposure of 25 percent for HyNap nilotinib, measured both as peak concentration (Cmax) and area under the curve (AUC). For the marketed product the corresponding increases after a high-fat meal are reported to be 112 percent and 82 percent, respectively.
In addition to the clinical results obtained for HyNap nilotinib, XSpray has in a number of comparative in vivo preclinical studies showed improved results, for both exposure and reduced pH dependency for a number of other marketed PKIs.