MECHELEN, BELGIUM--(Marketwired - April 23, 2013) - Galapagos NV (EURONEXT BRUSSELS: GLPG)
the start of the first Phase 2 clinical study with GLPG0974. This is the
compound from Galapagos' pipeline to enter Phase 2 studies, and its first
for patients with gastro-intestinal inflammation. GLPG0974 presents a
mode of action for the treatment of ulcerative colitis, a
inflammatory bowel disease. The efficacy and safety of GLPG0974 will be
in a four-week study with 45 patients and will deliver topline results
As a potent inhibitor of FFA2, oral treatment with GLPG0974 aims to
migration of neutrophils into the gastro-intestinal tract. Excessive
this type of white blood cells damages the bowel tissue and causes
inflammation in ulcerative colitis. The start of the Phase 2
study follows the excellent Phase 1 results with GLPG0974. In
volunteers, 2 weeks of once- or twice daily oral dosing was
safe up to the highest doses tested. A sustained suppression of
neutrophil activation demonstrated the desired pharmacodynamic activity.
"We are very excited about the start of the Phase 2 study with
discovered the role of the FFA2 target in inflammatory diseases,
developed GLPG0974 as a drug to inhibit FFA2. With this clinical
expand our scope from rheumatology to gastroenterology," said Dr Piet
CSO of Galapagos. "GLPG0974 is the first FFA2 antagonist being
clinically, and we are looking forward to the results in ulcerative
patients. If the drug shows efficacy in these patients, this will
important step, as there is currently no cure for this disease. We
report the results of the study in early 2014."
Details of the Phase 2A clinical study
The clinical Proof-of-Concept Phase 2 trial for GLPG0974 will
patients with mild to moderate ulcerative colitis. The aim is to
efficacy, effects on selected biomarkers, safety and tolerability
pharmacokinetics of GLPG0974 in this patient population. Patients with
moderate disease will receive either 200 mg of GLPG0974 twice-daily or
(2:1 ratio), for a period of four weeks. This randomized,
placebo-controlled study will recruit patients in multiple sites in 4
Belgium, Latvia, Czech Republic and Slovakia. Galapagos has already
approvals to start the trial in Belgium, with patient recruitment starting
month. The trial is anticipated to complete by year end and deliver top
data by Q1 2014.
About candidate drug GLPG0974
GLPG0974 is an orally available small molecule that reduces
neutrophils, one of the critical cell types in inflammatory processes, by
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
by inhibition of FFA2 may provide for a novel anti-inflammatory
approach. By inhibiting FFA2, GLPG0974 prevents free fatty
activation and migration of neutrophils towards an inflammatory site, such
the gut of patients with inflammatory bowel disease. GLPG0974 is the
inhibitor of FFA2 to be evaluated clinically. Galapagos expects to
results of the Proof of Concept in early 2014.
About ulcerative colitis
Ulcerative colitis (UC) is one of the idiopathic forms of inflammatory
disease (IBD). It is a chronic, relapsing inflammatory disease of the
characterized by ulcers in the colon and rectum. Symptoms may include
pain, malnutrition, and diarrhea, often bloody. Ulcerative colitis
prevalence of 200-250 cases per 100,000 individuals per year and a
incidence between the ages of 15 and 25 years. This chronic
without a medical cure and commonly requires a lifetime of care. Current
treatment includes anti-inflammatory steroids and immuno-suppressive agents
as TNF inhibitors. Over the long term, up to 25-30% of the patients
require surgery to remove the inflamed parts of the bowels.
Galapagos (EURONEXT BRUSSELS: GLPG) (PINKSHEETS: GLPYY) is specialized in
with a large pipeline of four clinical, seven pre-clinical, and 30
small-molecule and antibody programs in cystic fibrosis,
antibiotics, metabolic disease, and other indications.
GLPG0634 is an orally-available, selective inhibitor of JAK1 for the
of rheumatoid arthritis and potentially other inflammatory diseases,
enter Phase 2b studies. AbbVie and Galapagos signed a worldwide
agreement whereby AbbVie will be responsible for further
commercialization after Phase 2b. Galapagos has another selective
inhibitor in Phase 2 in lupus and psoriasis, GSK2586184 (formerly
in-licensed by GlaxoSmithKline in 2012). GLPG0187 is a novel integrin
antagonist currently in a Phase 1b patient study in metastasis. GLPG0974
first inhibitor of FFA2 to be evaluated clinically for the treatment of
this program is currently in a Proof-of-Concept Phase 2 study.
The Galapagos Group, including fee-for-service companies BioFocus,
Fidelta, has around 800 employees and operates facilities in five
with global headquarters in Mechelen, Belgium. Further information
This release may contain forward-looking statements, including,
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"stands to," and "continues," as well as similar expressions. Such
forward-looking statements may involve known and unknown risks,
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factors which might cause the actual results, financial condition,
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these uncertainties, the reader is advised not to place any undue
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of the date of publication of this document. Galapagos expressly
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Galapagos starts Phase 2A study with GLPG0974 in ulcerative colitis:
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