Mechelen, Belgium; 16 June 2009 – Galapagos NV (Euronext: GLPG) announced that today it has initiated Phase I clinical development of its integrin receptor antagonist (IRA), GLPG0187. This is the second small molecule therapeutic from Galapagos’ internal drug discovery program to enter the clinic in 2009. Candidate drug GLPG0187 could offer a promising new therapeutic approach for treating cancer patients. Initial development will focus on bone metastases from prostate and breast cancer.
Strong anti-cancer therapeutic profile in pre-clinical models
GLPG0187 offers a potentially highly competitive therapeutic profile compared to currently available agents to treat bone metastasis, a severe aspect of many cancers. GLPG0187 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 tumors and the destruction of bone. In these models, GLPG0187 also provided additive benefits to the bone protective action reported for currently used treatments. Based on the pre-clinical safety and efficacy data, Galapagos has been granted permission to initiate a first-in-human Phase I study to evaluate this compound’s safety, tolerability and pharmacokinetic properties, which will aid in evaluating its further development for the treatment of bone metastases.
“We are pleased to announce the transition of GLPG0187 into clinical development,” said Onno van de Stolpe, CEO of Galapagos. “This candidate drug has been shown to affect several steps in cancer disease progression in pre-clinical studies – suggesting that it may slow down the growth of existing bone metastasis as well as protect organs from invading cancer cells.”
Details of the Phase I clinical trial
The primary endpoints of this first-in-human trial will be to determine the safety, tolerability and pharmacokinetics of the candidate drug GLPG0187 as well as the evaluation of biomarkers to aid in the design of later trials. The double-blind, single ascending dose study will be conducted in 18 healthy human volunteers in Belgium over the coming months.
Galapagos (Euronext: GLPG; OTC: GLPYY) is a drug discovery and development company with small molecule programs in bone and joint diseases, bone metastasis, cachexia, anti-infectives and metabolic diseases. It has established risk sharing alliances with GSK, Janssen Pharmaceutica, Eli Lilly and Merck. Through an alliance with MorphoSys, Galapagos is also developing new antibody therapies in bone and joint diseases. Its division BioFocus DPI offers a full suite of target-to-drug discovery products and services to pharmaceutical and biotech companies and to patient foundations, encompassing target discovery and validation, screening and drug discovery through to delivery of pre-clinical candidates. Galapagos currently employs 490 people and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More info at: www.glpg.com.
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028
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 such as zolendronate, the standard prescribed treatment to treat bone loss related to malignancy, and denosumab, an antibody therapeutic currently in late stage clinical trials for treatment of malignancy-related bone loss