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:  This   release   may  contain  forward-looking  statements,  including, without limitation,   statements   containing   the   words  "believes," "anticipates," "expects,"  "intends,"  "plans,"  "seeks,"  "estimates," "may," "will," "could," "stands  to," and  "continues," as  well as  similar expressions.  Such forward-looking  statements may involve known and unknown risks, uncertainties and other factors  which might cause the  actual results, financial condition, performance or  achievements of Galapagos,  or industry results,  to be materially different from  any  historic  or  future  results,  financial  conditions, performance or achievements  expressed  or  implied  by  such forward-looking statements. Given these  uncertainties, the reader is  advised not to place  any undue reliance on such  forward-looking statements. These forward-looking statements speak only as of  the date of publication of  this document. Galapagos expressly disclaims any obligation  to update  any such  forward-looking statements  in this document to reflect  any change  in its  expectations with  regard thereto  or any change in events, conditions or circumstances on which any such statement is based, unless required by law or regulation.  [1] Sources: Wikipedia,  Galapagos to start Phase 2a study with GLPG0974 in IBD patients: htt p://  This announcement is distributed by Thomson Reuters on behalf of Thomson Reuters clients. The owner of this announcement warrants that:  (i) the releases contained herein are protected by copyright and     other applicable laws; and  (ii) they are solely responsible for the content, accuracy and      originality of the information contained therein.  Source: Galapagos NV via Thomson Reuters ONE  [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    
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