Galapagos initiates clinical study with GLPG0974, the first anti-inflammatory candidate drug targeting GPR43

  • Galapagos initiates Phase I First-in-Human trial with GLPG0974
  • GLPG0974 is a potent inhibitor of GPR43, a novel Galapagos target
  • Galapagos has been returned full rights to GLPG0974 by GSK

Mechelen, Belgium; 21 December 2011 – Galapagos NV (Euronext: GLPG) announced today 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.  

GLPG0974 is an orally available small molecule that reduces migration of neutrophils, one of the critical cell types in inflammatory processes by potent inhibition of GPR43 (also known as FFAR2).  Overactivity of neutrophils is a cause of tissue damage in illnesses such as inflammatory bowel disease, and this anti-inflammatory mechanism may provide for a novel treatment approach.  This will be the first inhibitor of GPR43 to be evaluated clinically.

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.

“GSK has decided to return the GPR43 program to Galapagos, and consequently we will not receive a milestone for initiation of this study,” said Onno van de Stolpe, CEO of Galapagos.  “We are encouraged by the results of this program thus far and have made the decision to continue moving forward with GLPG0974 on our own.”

Details of GLPG0974 First-in-Human trial
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.

About GLPG0974
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.

About Galapagos
Galapagos (Euronext: GLPG; OTC: GLPYY) is a mid-size biotechnology company specialized in the discovery and development of small molecule and antibody therapies with novel modes-of-action.  The Company is progressing GLPG0634, as well as one of the largest pipelines in biotech, with seven programs in development and over 50 discovery programs.  The Galapagos Group has over 800 employees and operates facilities in six countries, with global headquarters in Mechelen, Belgium.  More info at:


Galapagos NV
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028

Elizabeth Goodwin, Director Investor Relations
Tel: +31 6 2291 6240

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