Wilex AG has initiated a phase Ib/IIa clinical trial with WX-UK1, a small molecule inhibitor of the uPA (Urokinase-type plasminogen activator) system which has been shown to play a key role in the progression and metastasis of various solid tumors. The dose escalation study will evaluate tolerability and biological activity of WX-UK1 in patients with advanced gastric, pancreatic and ovarian cancers.

The national multicenter trial is being conducted by Prof. Christian Peschel, director of the III. Medical Department at the Technical University of Munich. First preliminary results are expected in second half of 2003.

In the phase Ib part of the trial, late stage cancer patients, for which currently no standard therapy exists, will be treated for four weeks with WX-UK1 to determine the maximum tolerable dose (MTD) and pharmacokinetics. In the phase IIa part, 30 patients will be treated up to 12 weeks with the MTD to evaluate and confirm the safety and tolerability of this dosing schedule. In addition, the biological activity of the substance will be analyzed in order to assess biological markers in blood and urine, which might indicate effects of WK-UK1 on the tumor. Finally a tumor assessment will be carried out to evaluate changes in tumor growth.

Prof. Olaf G. Wilhelm, founder and CEO of Wilex commented, "WX-UK1 is the first urokinase inhibitor to be administered to cancer patients in a clinical setting. It is our goal to develop WX-UK1 to slow down and block metastasis in cancer patients who express a high level of uPA in their tumors and, thus, bear a high risk of developing metastasis. We consider this trial an additional important step towards the development of a cancer medicine of the future, which entails individualized treatment tailored to the specific needs of cancer patient subpopulations."

Wilex is developing WX-UK1 for the treatment of patients with solid tumors, such as breast, ovarian, gastric, colon, lung or pancreatic cancer, who express in their tumors high levels of the uPA-system. This applies to approximately 30 percent of all patients in these indications. Animal models have already demonstrated the ability of WX-UK1 to substantially slow down tumor growth and to block metastasis. In a first clinical phase Ia trial with healthy volunteers, WX-UK1 proved to be safe and well tolerated. Wilex plans to initiate Ib/IIa trials in further indications in the following months.