Galapagos completes patient recruitment in Proof of Concept study with GLPG0974 in ulcerative colitis
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. Â 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. Â 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. Â 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. Â The aim is to evaluate
the safety, efficacy, pharmacokinetics and effects on selected biomarkers of
GLPG0974 in this patient population. Â 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). Â Over-
activity of neutrophils is a cause of tissue damage in illnesses such as
inflammatory bowel disease. Â A reduction of neutrophil activation and migration
by inhibition of FFA2 may provide for a novel anti-inflammatory treatment
approach. Â Bacteria produce free fatty acids by fermentation of food fibers in
the gut. Â These fatty acids attract neutrophils through the activation of the
neutrophil FFA2 receptor. Â 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. Â 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). Â It is a chronic, relapsing inflammatory disease of the colon,
characterized by ulcers in the colon and rectum. Â Symptoms may include abdominal
pain, malnutrition and diarrhea, often bloody. Â 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. Â Current drug
treatment includes anti-inflammatory steroids and immuno-suppressive agents such
as TNF inhibitors. Â Over the long term, up to 25-30% of the patients will
require surgery to remove the inflamed parts of the bowels.
About Galapagos
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. Â 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. Â 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
CONTACT
For media and investor inquiries:
Elizabeth Goodwin, Head of Corporate Communications & Investor Relations
Tel: +31 6 2291 6240
ir@glpg.com
For business development inquiries:
Andre Hoekema, Senior VP Corporate Development
Tel: +31 71 7506 700
bd@glpg.com
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