MECHELEN, BELGIUM--(Marketwire - March 27, 2013) -
* Positive Phase 1 study showed clean safety data and strong response of
* Phase 2a Proof of Concept study in ulcerative colitis will start next
Galapagos NV (Euronext: GLPG) announced today
that GLPG0974, an inhibitor of FFA2 (free fatty acid receptor 2, formerly
as GPR43) being developed to treat chronic neutrophil-driven
conditions such as inflammatory bowel disease (IBD), showed a clean
profile and a strong biomarker signal. In this second Phase 1 study
GLPG0974, the safety, tolerability, pharmacodynamics and pharmacokinetics
evaluated in 32 healthy volunteers dosed for 2 weeks. The positive
this study supports progression to a Proof of Concept study in
colitis patients that is expected to start in 2Q 2013.
The completed Phase 1 study evaluated once- and twice-daily dosing
healthy volunteers who received GLPG0974 for 2 weeks. This second Phase 1
follows the First-in-Human study for GLPG0974 completed in 2012, in which a
range was given as single doses. The current study confirmed that
safe and well tolerated at all dose levels. A dose dependent
neutrophil activation was shown, up to a maintained 24-hour inhibition
"GLPG0974 is the first FFA2 inhibitor to be tested clinically, and these
are very encouraging," said Dr Piet Wigerinck, CSO of Galapagos. "The
ascending dose study showed stable PK, good safety and tolerability and a
inhibition of biomarker CD11b. The next step is a Proof of Concept study
GLPG0974. The aim of this study will be to show a clinical response in
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,
(PK), and pharmacodynamics (PD) of oral multiple ascending doses of
The randomized, double-blind, placebo-controlled, single center
conducted in 32 healthy volunteers in Belgium. GLPG0974 was dosed for 2
as once- and twice-daily regimens. The study was designed to confirm the
biomarker signal previously observed in the First-in-Human Phase 1 study.
biomarker that was measured in blood from healthy volunteers was
neutrophil surface marker. The presence of CD11b increases when
activated in response to inflammatory stimuli.
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
Overactivity of neutrophils is a cause of tissue damage in illnesses
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
Proof of Concept study ulcerative colitis in 2Q 2013.
Inflammatory bowel disease is a group of inflammatory conditions in the
intestine and colon, the main forms being Crohn's and ulcerative
Crohn's disease can affect the entire wall in any part of the
tract, while ulcerative colitis affects only the lining in the
rectum. Patients suffering from IBD conditions experience abdominal
vomiting, diarrhea, weight loss, and rectal bleeding, and may also have
outside the bowel, such as problems with skin, eyes, and liver.
0.8% of the European population and 0.7% of the North American
diagnosed annually with IBD. This chronic condition is without a medical
and commonly requires a lifetime of care. Current drug treatment includes
anti-inflammatory steroids and immuno-suppressive agents such as TNF
Over the long term, up to 75% of patients with Crohn's disease and 25% of
with ulcerative colitis will require surgery to remove the inflamed parts
bowels. In the United States, IBD accounts for more than 700,000
visits and 100,000 hospitalizations per year, and disability in
Galapagos (Euronext: GLPG; OTC: GLPYY) is specialized in novel
with a large pipeline of four clinical, six 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 will start a Proof of Concept Phase 2 study in Q2 2013.
The Galapagos Group, including fee-for-service companies BioFocus,
Fidelta, has over 800 employees and operates facilities in five countries,
global headquarters in Mechelen, Belgium. Further information at:
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limitation, statements containing the words "believes,"
"expects," "intends," "plans," "seeks," "estimates," "may," "will,"
"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
such forward-looking statements. These forward-looking statements speak
of the date of publication of this document. Galapagos expressly
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required by law or regulation.
 Sources: Wikipedia, CDC.gov
Galapagos to start Phase 2a study with GLPG0974 in IBD patients:
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