Galapagos initiates clinical studies with GLPG0187, a candidate drug for bone metastasis

17-Jun-2009 - Belgium

Galapagos NV announced that 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.

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.

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.

https://www.bionity.com/en/news/102133/galapagos-initiates-clinical-studies-with-glpg0187-a-candidate-drug-for-bone-metastasis.html