Belgium-based biotechnology company Galapagos has announced that its investigational medicine GLPG0778, a kinase target GT623 inhibitor, has demonstrated selective effects on a biomarker in a Phase I proof-of-mechanism study in healthy volunteers.

Galapagos has initiated the first-in-human trial for GLPG0778 in December 2010 as part of an immuno-inflammatory alliance with GlaxoSmithKline

The study included 45 healthy volunteers, who were divided into five cohorts, receiving in total four different dosages for two weeks, and provided information on the safety and pharmacokinetic profile of GLPG0778.

In the study, GPLG0778 has showed dose-dependent and selective suppression of an induced inflammatory response in the volunteers, indicating specific inhibition of the medicine’s target in vivo.

The primary endpoints of the first-in-human trial for GLPG0778 included determination of safety, tolerability and pharmacokinetics, while the secondary endpoint was to examine biomarker effects of the candidate drug.

GSK has announced that the results meet the criteria of clinical Proof of Mechanism, thereby triggering a Euro single-digit millions payment to Galapagos.

Previous studies performed in biochemical and animal models showed that GPLG0778 has excellent activity and safety, and the drug has successfully completed pre-clinical development.

In May 2011, the company commenced a second Phase I proof-of-mechanism study in its immuno-inflammation alliance with GlaxoSmithKline, which follows the positive outcome of the first-in-human trial conducted for GLPG0778.

The study will evaluate GLPG0778’s effect on a specific target, and its ability to suppress an induced inflammatory response in healthy volunteers.

Galapagos CEO Onno van de Stolpe said that GLPG0778 is the company’s second drug candidate to demonstrate targeted activity in clinical trials.

"We believe GLPG0778’s biomarker and safety profile support its further development in a Phase II clinical study in a patient population," Stolpe said.

Galapagos is a mid-size biotechnology company specialised in the discovery and development of small molecule and antibody therapies with novel modes-of-action.