Mechelen, Belgium; 17 February 2014 - Galapagos NV (Euronext: GLPG) announced today that patient recruitment has been completed for the clinical Proof of Concept study with GLPG0974. GLPG0974 presents a novel mode of action for the treatment of ulcerative colitis, a debilitating inflammatory bowel disease. The efficacy and safety of GLPG0974 are being evaluated during a 28-day treatment period. Topline results from this study are expected in June 2014. GLPG0974 is fully proprietary to Galapagos.
As a potent inhibitor of FFA2 (free fatty acid receptor 2), GLPG0974 aims to reduce migration of neutrophils into the gastro-intestinal tract. Over-activity of neutrophils damages the bowel tissue and causes chronic inflammation in ulcerative colitis. FFA2 plays an important role in the migration of neutrophils and is over-expressed in ulcerative colitis patients. In healthy volunteers, 14 days of once- or twice-daily oral dosing of GLPG0974 was well-tolerated and safe up to the highest doses tested. A sustained suppression of a biomarker for neutrophil activation demonstrated the desired pharmacodynamic activity.
Details of the Phase 2a clinical study
The clinical Proof-of-Concept Phase 2 trial for GLPG0974 is designed to recruit 45 patients with mild to moderate ulcerative colitis. The aim is to evaluate the safety, efficacy, pharmacokinetics and effects on selected biomarkers of GLPG0974 in this patient population. Patients are randomized to receive either 200 mg of GLPG0974 twice-daily or placebo (2:1 ratio), for a period of 28 days. This double-blind, placebo-controlled study recruited patients in multiple sites in 4 countries: Belgium, the Czech Republic, Latvia, and Slovakia.
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). Over-activity 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. Bacteria produce free fatty acids by fermentation of food fibers in the gut. These fatty acids attract neutrophils through the activation of the neutrophil FFA2 receptor. 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 evaluated clinically.
About ulcerative colitis
Ulcerative colitis (UC) is one of the idiopathic forms of inflammatory bowel disease (IBD). It is a chronic, relapsing inflammatory disease of the colon, characterized by ulcers in the colon and rectum. Symptoms may include abdominal pain, malnutrition and diarrhea, often bloody. Ulcerative colitis has a prevalence of 200-250 cases per 100,000 individuals per year and a peak incidence between the ages of 15 and 25 years. This chronic condition is without a medical cure and commonly requires a lifetime of care. Current drug treatment includes anti-inflammatory steroids and immuno-suppressive agents such as TNF inhibitors. Over the long term, up to 25-30% of the patients will require surgery to remove the inflamed parts of the bowels.
Galapagos (Euronext: GLPG; OTC: GLPYY) is specialized in novel modes-of-action, with a large pipeline comprising of six Phase 2 studies (three led by GSK), one Phase 1 study, six pre-clinical, and 20 discovery small-molecule and antibody programs in cystic fibrosis, inflammation, antibiotics, metabolic disease, and other indications. In the field of inflammation, AbbVie and Galapagos signed a worldwide license agreement whereby AbbVie will be responsible for further development and commercialization of GLPG0634 after Phase 2B. GLPG0634 is an orally-available, selective inhibitor of JAK1 for the treatment of rheumatoid arthritis and potentially other inflammatory diseases, currently in Phase 2B studies in RA and in Phase 2 in Crohn's disease. Galapagos has another selective JAK1 inhibitor in Phase 2 in ulcerative colitis, psoriasis, and lupus, GSK2586184 (formerly GLPG0778, in-licensed by GlaxoSmithKline in 2012). GLPG0974 is the first inhibitor of FFA2 to be evaluated clinically for the treatment of IBD; this program is currently in a Proof-of-Concept Phase 2 study. GLPG1205 is a first-in-class molecule that targets inflammatory disorders and has completed Phase 1. AbbVie and Galapagos signed an agreement in CF where they work collaboratively to develop and commercialize oral drugs that address two mutations in the CFTR gene, the G551D and F508del mutation. Potentiator GLPG1837 is at the pre-clinical candidate stage. The Galapagos Group, including fee-for-service companies BioFocus, Argenta and Fidelta, has around 800 employees and operates facilities in five countries, with global headquarters in Mechelen, Belgium. Further information at: www.glpg.com
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