IT-143

Intezyne's second chemotherapeutic agent, IT-143, utilizes daunorubicin as its active drug. Daunorubicin is part of the anthracycline family of chemotherapy drugs, many of which are widely prescribed for a variety of solid tumors. Despite their 50 year clinical use, significant cardiotoxicity and poor circulation lifetimes are associated with anthracycline chemotherapy treatments. Intezyne's IT-143 addresses both of these shortcomings by encapsulating daunorubicin in the IVECT Method, allowing the drug to circulate for long periods of time and accumulate at the tumor environment.

One study to examine the circulation lifetime of IT-143 compared to free drug was performed in rats. Groups of rats were dosed with equal amounts of daunorubicin as IT-143, uncrosslinked daunorubicin micelles, and free daunorubicin. Small samples of blood were collected at various time points, then assayed for the concentration of daunorubicin in the blood.

The amount of daunorubicin in blood is very similar for both the free daunorubicin and the uncrosslinked daunorubicin micelle. However, a 90-fold increase in daunorubicin concentration is observed for IT-143, demonstrating the impact that the IVECT Method has on micelle stability within the bloodstream.

IT-143 also allows preferential accumulation of drug within the tumor environment. In another experiment, mice growing human lung cancer tumors were treated with equal amounts of free daunorubicin and IT-143. The concentration of daunorubicin was assayed at various time points after administration in the tumor and other organs.

Remarkably, IT-143 shows 75 times more daunorubicin in the tumor when compared to free daunorubicin. By directing more of the drug to the tumor environment, chemotherapy with IT-143 is expected to be much more effective. Furthermore, IT-143 is tolerated at doses three times higher than free daunorubicin, resulting in a safer and more effective treatment.

Intezyne is currently performing additional preclinical safety and efficacy studies on IT-143.