Date: 2011-12-21
Type of information:
phase: 1
Announcement: initiation
Company: Galapagos (Belgium)
Product: GLPG0974
Action mechanism: GLPG0974 is an orally available small molecule, nanomolar inhibitor of GPR43 (G-protein coupled receptor), also known as FFAR2 (free fatty acid receptor 2), which was identified by Galapagos as playing a key role in inflammation. GLPG0974 has shown potent inhibition of neutrophil migration (HOW) and successfully passed single dose animal safety evaluation. No other inhibitors of GPR43 are currently known to have been evaluated clinically.
Disease: inflammatory diseases
Therapeutic area: Inflammatory diseases
Country: Belgium
Trial
details: The primary endpoints of the first-in-human trial for GLPG0974 will be to determine the pharmacokinetics and to evaluate biomarker effects of this candidate drug. In addition, the safety and tolerability of a wide dose range will be evaluated. The placebo-controlled, double-blind, single ascending dose study is being conducted in 36 healthy human volunteers in Belgium over the coming months. It follows the design for exploratory single dose trials, as supported by guidelines that EMEA and the FDA designed to boost innovation in drug discovery and development.
Latest
news: * On April 18, 2012, Galapagos gave an R&D update, indicating progress and plans for its portfolio. The company announced that encouraging safety data showed no relevant safety findings, including adverse events, changes in vital signs or laboratory parameters. The favourable PK profile and the highly significant changes in neutrophil biomarkers are consistent with once- or twice-daily oral dosing. Galapagos intends to complete Phase I studies and determine the Phase II clinical strategy before year end 2012.
* On December 21, 2011, Galapagos has announced that it has initiated clinical Phase I development of the first inhibitor of GPR43, a novel target for inflammatory diseases. This target was identified through Galapagos' proprietary target discovery platform. The First-in-Human study with GLPG0974 will focus on providing more information on its pharmacokinetics and pharmacodynamics, using an innovative design for clinical testing specifically intended for early clinical exploration of novel candidate drugs. The GPR43 program has recently been returned to Galapagos by GSK.
