Drug Candidate MESUPRON®*

The second drug candidate in the uPA program in clinical development in cancer patients is MESUPRON®. MESUPRON® is an oral second generation serine protease inhibitor targeting the uPA (urokinase Plasminogen Activator) system. MESUPRON® is an orally available pro-drug of WX-UK1.

In pre-clinical studies oral MESUPRON® was shown to be safe and well-tolerated and demonstrated good inhibition of tumour growth and metastasis. MESUPRON® was moved into clinical development targeting tumour indications where long-term chronic treatment is necessary.

MESUPRON® has successfully completed two European Phase I studies in healthy volunteers. In a “first-into-man” Phase I single-dose study, MESUPRON® was safe and well tolerated at all dose levels tested and, in addition, showed good oral bioavailability, i.e. absorption by the gut, and efficient conversion to the active drug WX-UK1 in the body. A placebo controlled, double-blind study tested safety, tolerability, and pharmacokinetics of multiple rising doses of MESUPRON® in healthy volunteers. The study has been successfully completed.

Currently, MESUPRON® is being studied in two Phase II studies in patients with pancreatic cancer and breast cancer.