Mechelen, Belgium; 19 January 2010 - Galapagos NV (Euronext: GLPG) announced results from the first-in-human trial with candidate drug GLPG0187. GLPG0187 offers a new approach to treat metastases, a severe complication of many cancers. The candidate drug showed good safety and a promising biomarker profile in healthy volunteers. Based on the results from the trial, Galapagos plans to initiate a second Phase I trial including cancer patients later this year. "We are excited that our candidate drug demonstrated a clear biological response in healthy volunteers. With these promising biomarker data and the favorable safety profile, we believe GLPG0187 has strong potential as a cancer drug," said Onno van de Stolpe, CEO of Galapagos. "Therefore, we have decided to broaden the therapeutic focus to metastatic cancer, which is more prevalent than bone metastasis." In the double-blind, placebo-controlled trial, 27 healthy volunteers were given escalating doses of candidate drug GLPG0187 by either subcutaneous injection (17.5 to 315 mg) or oral administration (50 to 1200 mg). For both routes of administration, systemic safety data were favorable with no severe adverse events or changes in vital signs or laboratory parameters observed. Local reactions occurring at or near the injection site were not attributable to the candidate drug. A biomarker relevant to bone metastasis (serum CTX, collagen telopeptide) showed a response lasting 24 hours. Although bioavailability for the oral formulation was low, a clear biomarker response was observed with two oral doses (300 and 1200 mg). Given these results, Galapagos plans to initiate a second Phase I trial including cancer patients later this year. Galapagos is also working to improve the injectable formulation and the bioavailability of the oral formulation. About GLPG0187 GLPG0187, an integrin receptor antagonist (IRA), blocks five integrin receptors known to be present in many metastatic cancers, affording a unique anti-integrin profile. In animal studies, oral administration of GLPG0187 as a single agent has been shown to inhibit multiple processes involved in the spread and growth of metastatic tumors.
