Galapagos to start Phase 2a study with GLPG0974 in IBD patients

Galapagos to start Phase 2a study with GLPG0974 in IBD patients 
MECHELEN, BELGIUM -- (Marketwire) -- 03/27/13 --  
* Positive Phase 1 study showed clean safety data and strong
response of     biomarker 
* Phase 2a Proof of Concept study in ulcerative colitis will start
next month 
Galapagos NV (Euronext: GLPG) announced today that  GLPG0974, an
inhibitor of FFA2 (free fatty acid receptor 2, formerly known
as 
GPR43)  being  developed  to  treat  chronic  neutrophil-driven
inflammatory
conditions  such  as  inflammatory  bowel  disease 
(IBD), showed a clean safety
profile  and  a  strong  biomarker 
signal.   In  this second Phase 1 study with
GLPG0974,  the safety,
tolerability,  pharmacodynamics and pharmacokinetics were
evaluated 
in 32 healthy volunteers dosed for  2 weeks.  The positive outcome of
this  study  supports  progression  to  a  Proof  of Concept study in
ulcerative
colitis patients that is expected to start in 2Q 2013. 
The  completed Phase 1 study evaluated once-  and twice-daily dosing
regimens in healthy volunteers who received GLPG0974 for 2 weeks. 
This second Phase 1 study
follows the First-in-Human study for
GLPG0974 completed in 2012, in which a dose
range  was given as
single doses.  The current study confirmed that GLPG0974 was safe 
and well  tolerated at  all dose  levels. A  dose dependent
inhibition of neutrophil  activation was shown,  up to a  maintained
24-hour inhibition of the biomarker. 
"GLPG0974 is the first FFA2 inhibitor to be tested clinically, and
these results
are  very encouraging," said Dr Piet Wigerinck, CSO of
Galapagos.  "The multiple
ascending  dose study showed stable PK,
good  safety and tolerability and a good
inhibition  of biomarker
CD11b.  The next step  is a Proof of Concept study with
GLPG0974. 
The aim of this study will be to show a clinical response in
patients
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,
pharmacokinetics
(PK),  and pharmacodynamics (PD)  of oral multiple 
ascending doses of GLPG0974.
 The  randomized,  double-blind, 
placebo-controlled,  single  center study was conducted  in 32
healthy volunteers in Belgiu
m.   GLPG0974 was dosed for 2 weeks
as
once- and twice-daily regimens.  The study was designed to confirm
the strong
biomarker  signal previously observed in  the
First-in-Human Phase 1 study. The
biomarker  that  was  measured  in 
blood  from  healthy volunteers was CD11b, a neutrophil surface
marker.  The presence of CD11b increases when neutrophils are
activated in response to inflammatory stimuli. 
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).
Overactivity  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.   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.   Galapagos
expects  to start a Proof of Concept study ulcerative colitis in 2Q
2013. 
About IBD[1] 
Inflammatory  bowel disease is  a group of  inflammatory conditions
in the small
intestine  and  colon,  the  main  forms  being Crohn's
and ulcerative colitis.
Crohn's  disease can affect the entire wall 
in any part of the gastrointestinal
tract,  while  ulcerative 
colitis  affects  only  the  lining  in the colon and rectum.  
Patients  suffering  from  IBD  conditions  experience abdominal
pain,
vomiting, diarrhea, weight loss, and rectal bleeding, and may
also have symptoms
outside  the bowel, such as problems  with skin,
eyes, and liver. Approximately
0.8% of  the European  population and 
0.7% of the  North American population is diagnosed  annually with
IBD.  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 75% of patients with
Crohn's disease and 25% of those
with ulcerative colitis will require
surgery to remove the inflamed parts of the bowels.   In the  United
States,  IBD accounts  for more  than 700,000 physician
visits  and 
100,000 hospitalizations  per  year,  and  disability  in
119,000
patients. 
About Galapagos 
Galapagos  (Euronext: GLPG; OTC: GLPYY) is specialized in novel
modes-of-action,
with  a  large  pipeline  of  four  clinical, six
pre-clinical, and 30 discovery
small-molecule   and   antibody  
programs  in  cystic  fibrosis, inflammation,
antibiotics, metabolic
disease, and other indications. 
GLPG0634  is an orally-available, selective inhibitor  of JAK1 for
the treatment
of  rheumatoid arthritis and  potentially other
inflammatory  diseases, about to enter  Phase  2b studies.   AbbVie 
and  Galapagos  signed  a  worldwide license
agreement  whereby 
AbbVie  will  be  responsible  for  further development and
commercialization   after   Phase  2b.  Galapagos  has  another 
selective JAK1
inhibitor  in Phase 2 in lupus and psoriasis,
GSK2586184 (formerly GLPG0778,
in-licensed  by GlaxoSmithKline  in
2012).  GLPG0187  is a  novel integrin receptor
antagonist currently
in a Phase 1b patient study in metastasis.  GLPG0974 is the first 
inhibitor of FFA2  to be evaluated  clinically for the  treatment of
IBD;
this program will start a Proof of Concept Phase 2 study in Q2
2013. 
The  Galapagos Group, including fee-for-service  companies BioFocus,
Argenta and Fidelta,  has over 800 employees and operates facilities
in five countries, with
global headquarters in Mechelen, Belgium. 
Further information at: www.glpg.com 
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[1] Sources: Wikipedia, CDC.gov 
Galapagos to start Phase 2a study with GLPG0974 in IBD patients:
htt
p://hugin.info/133350/R/1688491/553965.pdf 
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[HUG#1688491] 
CONTACT 
Galapagos NV
Dr Piet Wigerinck
Chief Scientific Officer
Tel. +32 477 627103 
Elizabeth Goodwin
Director Investor Relations
Tel: +31 6 2291 6240
ir@glpg.com
 
 
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