Mechelen, Belgium; 24 October 2012 – Galapagos NV (Euronext: GLPG) announced today that it has started its second Phase I clinical study with GLPG0974, a GPR43 inhibitor being developed to treat chronic, neutrophil-driven inflammatory conditions such as inflammatory bowel disease (IBD). In this clinical study, the safety and tolerability of GLPG0974 will be evaluated for 2 weeks in 32 healthy volunteers. Aim of the study is also to confirm the strong biomarker signal and the once-daily (QD) dosing of the compound after 14 days. Results of the study are expected to be reported early next year.
“GLPG0974 is one of our novel mode-of-action compounds in clinical development. The clear inhibition of biomarker CD11b and the clean safety profile seen in the First-in-Human Phase I study looked promising, and this second Phase I study will provide us with valuable information about the drug’s profile after multiple administration. Patients suffering from IBD are in need of effective therapies which treat the root cause of the disease. GLPG0974 targets GPR43, which Galapagos has identified as playing a key role in IBD,” said Dr Piet Wigerinck, Chief Scientific Officer of Galapagos.
Details of the second Phase I clinical study
The aim of this study is to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of oral multiple ascending doses of GLPG0974. The randomized, double-blind, placebo-controlled, single center study will be conducted in 32 healthy volunteers in Belgium. The study is designed to confirm the strong biomarker signal and QD dosing possibilities observed in the First-in-Human Phase I study.
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 GPR43 (also known as FFA2). Overactivity of neutrophils is a cause of tissue damage in illnesses such as inflammatory bowel disease, and this anti-inflammatory mechanism may provide for a novel treatment approach. GLPG0974 is the first inhibitor of GPR43 to be evaluated clinically. Galapagos intends to determine the Phase II clinical strategy before year end 2012.
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 treatment includes anti-inflammatory steroids and immuno-suppressive agents such as TNF inhibitors. Each year in the United States, IBD accounts for more than 700,000 physician visits, 100,000 hospitalizations, and disability in 119,000 patients. Over the long term, up to 75% of patients with Crohn’s disease and 25% of those with ulcerative colitis will require surgery.
Galapagos (Euronext: GLPG; OTC: GLPYY) is a mid-size clinical stage biotechnology company specialized in the discovery and development of small molecule and antibody therapies with novel modes-of-action. The Company is progressing its JAK1 inhibitor GLPG0634, as well as one of the largest pipelines in biotech, with four programs in development and over 30 discovery programs. The Galapagos Group has over 800 employees and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More info at: www.glpg.com
Piet Wigerinck, SVP Development
Tel: +32 477 62 7103
Elizabeth Goodwin, Director Investor Relations
Tel: +31 6 2291 6240
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.
 Sources: Wikipedia, CDC.gov