Mechelen, Belgium; 8 January 2015 - Galapagos NV (Euronext: GLPG) announced today it has initiated a Phase 2 Proof-of-Concept study in ulcerative colitis with GPR84 inhibitor GLPG1205, a potential novel treatment for Inflammatory Bowel Diseases. GLPG1205 arises from Galapagos' target discovery platform and is fully proprietary to Galapagos.
GLPG1205 ('1205) inhibits GPR84, a novel mechanism of action developed by Galapagos for Inflammatory Bowel Diseases (IBD). Galapagos has shown that GPR84 plays a key role in IBD and that '1205 is a selective inhibitor of GPR84 and very effective in pre-clinical models for IBD. In Phase 1 studies, '1205 showed good safety, full blockage of GPR84, and favorable drug-like properties. The first patients in this double-blind, placebo controlled study will initiate their treatment this week.
Details of the Phase 2 clinical study
The clinical Proof-of-Concept Phase 2 trial for '1205 will involve approximately 60 patients with moderate to severe ulcerative colitis. The aim is to evaluate the efficacy, safety and tolerability and pharmacokinetics of '1205, and to explore the effects of '1205 on selected biomarkers in this patient population. Patients will receive either 100 mg of '1205 or placebo (2:1 ratio) once-daily, for a period of twelve weeks. The primary endpoint will be the change in Mayo scores versus baseline at 8 weeks, which includes endoscopic confirmation on improvement of ulceration. This randomized, double-blind study will recruit patients in multiple sites in 6 countries: Belgium, Hungary, Poland, Czech Republic, Germany and Russia. Galapagos has received full approvals to start the trial in Belgium, Hungary, Germany and the Czech Republic, with patient recruitment already underway. Approvals in Russia and Poland are expected to follow this first quarter. The trial is anticipated to deliver top line data in H1 2016.
About ulcerative colitis
Ulcerative colitis (UC) is one of the 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.
G-coupled protein receptor 84 (GPR84) is involved in the regulation of macrophages, monocytes, and neutrophils in the human immune system. Galapagos identified GPR84 as playing a key role in inflammation, using its proprietary target discovery platform. GPR84 is over-expressed in patients with both forms of IBD - UC and Crohn's disease - as well as in multiple sclerosis. Galapagos has demonstrated in pre-clinical trials that GPR84 inhibition prevents neutrophil and macrophage chemotaxis induced by specific triggers, and that '1205 prevents IBD disease progression in animal models. '1205 is also the first selective inhibitor of GPR84 to be tested in humans; it has shown good safety, inhibition of GPR84, and favorable drug-like properties in Phase 1 studies.
Galapagos (Euronext: GLPG; OTC: GLPYY) is specialized in novel modes-of-action, with a large pipeline comprising three Phase 2 programs, two Phase 1 studies, five pre-clinical, and 25 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 an agreement for the development and commercialization of GLPG0634. 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, GSK2586184 (formerly GLPG0778, in-licensed by GlaxoSmithKline in 2012). GLPG1205, a first-in-class inhibitor of GPR84, is currently being tested in a Phase 2 Proof-of-Concept study in ulcerative colitis patients. GLPG1690 is a first-in-class compound that targets pulmonary diseases and is currently in a Phase 1 study. AbbVie and Galapagos signed an agreement in cystic fibrosis to develop and commercialize molecules that address mutations in the CFTR gene. Potentiator GLPG1837 started Phase 1 last month, and corrector GLPG2222 is at the pre-clinical candidate stage. The Galapagos Group, including fee-for-service subsidiary Fidelta, has around 400 employees, operating from its Mechelen, Belgium headquarters and facilities in The Netherlands, France, and Croatia. Further information at: www.glpg.com
Elizabeth Goodwin, Head of Corporate Communications & IR
Tel: +31 6 2291 6240
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