Galapagos to start Phase 2a study with GLPG0974 in IBD patients

Date: 27/03/2013

Mechelen, Belgium; 27 March 2013 – Galapagos NV (Euronext: GLPG) announced today that GLPG0974, an inhibitor of FFA2 (free fatty acid receptor 2, formerly known as GPR43) being developed to treat chronic neutrophil-driven inflammatory conditions such as inflammatory bowel disease (IBD), showed a clean safety profile and a strong biomarker signal.  In this second Phase 1 study with GLPG0974, the safety, tolerability, pharmacodynamics and pharmacokinetics were evaluated in 32 healthy volunteers dosed for 2 weeks.  The positive outcome of this study supports progression to a Proof of Concept study in ulcerative colitis patients that is expected to start in 2Q 2013.

The completed Phase 1 study evaluated once- and twice-daily dosing regimens in healthy volunteers who received GLPG0974 for 2 weeks.  This second Phase 1 study follows the First-in-Human study for GLPG0974 completed in 2012, in which a dose range was given as single doses.  The current study confirmed that GLPG0974 was safe and well tolerated at all dose levels. A dose dependent inhibition of neutrophil activation was shown, up to a maintained 24-hour inhibition of the biomarker.

“GLPG0974 is the first FFA2 inhibitor to be tested clinically, and these results are very encouraging,” said Dr Piet Wigerinck, CSO of Galapagos.  “The multiple ascending dose study showed stable PK, good safety and tolerability and a good inhibition of biomarker CD11b.  The next step is a Proof of Concept study with GLPG0974.  The aim of this study will be to show a clinical response in patients with ulcerative colitis.  It is expected to start next month.”


Details of the second Phase 1 clinical study

The aim of this study was to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of oral multiple ascending doses of GLPG0974.  The randomized, double-blind, placebo-controlled, single center study was conducted in 32 healthy volunteers in Belgium.  GLPG0974 was dosed for 2 weeks as once- and twice-daily regimens.  The study was designed to confirm the strong biomarker signal previously observed in the First-in-Human Phase 1 study.  The biomarker that was measured in blood from healthy volunteers was CD11b, a neutrophil surface marker.  The presence of CD11b increases when neutrophils are activated in response to inflammatory stimuli.


About candidate drug GLPG0974

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 FFA2 (free fatty acid receptor 2, formerly known as GPR43).  Overactivity of neutrophils is a cause of tissue damage in illnesses such as inflammatory bowel disease.  A reduction of neutrophil activation and migration by inhibition of FFA2 may provide for a novel anti-inflammatory treatment approach.  By inhibiting FFA2, GLPG0974 prevents free fatty acid-induced activation and migration of neutrophils towards an inflammatory site, such as in the gut of patients with inflammatory bowel disease.  GLPG0974 is the first inhibitor of FFA2 to be