Mechelen, Belgium; 9 June 2011- Galapagos NV (Euronext: GLPG) announced today that it has started a Phase II clinical study for GLPG0634, a novel Janus kinase (JAK) inhibitor being developed for inflammatory conditions, such as rheumatoid arthritis (RA). In this clinical trial, the efficacy and safety of GLPG0634 will be tested in RA patients, with plans to complete a four-week study by the end of 2011. GLPG0634 is a fully proprietary program which Galapagos intends to partner.
"We are pleased to initiate this Proof-of-Concept study for GLPG0634, which marks our second patient trial in rheumatoid arthritis. The current study with GLPG0634 is designed to show a fast onset of clinical response and will be completed by the end of this year," said Piet Wigerinck, SVP Development. "The pre-clinical and Phase I studies for this compound show a specific JAK1 inhibition profile, which could differentiate from other JAK compounds in development."
Details of the Phase II clinical trial
The clinical Proof-of-Concept Phase II trial for GLPG0634 will involve 36 patients with active rheumatoid arthritis, showing an insufficient response to the standard-of-care treatment, methotrexate (MTX). The aim is to evaluate the efficacy and safety of GLPG0634 in treating rheumatoid arthritis. Three groups of 12 patients with moderate to severe disease will receive either a once- or twice-daily dose regimen of GLPG0634 or placebo, for a period of four weeks, while all will continue to take their stable background therapy of MTX. The primary efficacy endpoint will be the ACR20 response rate, the standard primary endpoint for RA clinical trials. Secondary endpoints include improvements in DAS28, ACR50 and ACR70 rates and clinical score. The safety and tolerability, and the pharmacokinetics of GLPG0634 in rheumatoid arthritis patients will also be evaluated. Galapagos has received approvals to start the trial at a single Eastern European center, with patient recruitment planned to start in June 2011. The trial has been designed to obtain initial efficacy data by the end of 2011. This phase II trial is part of a broader development program that includes additional pharmacology, Phase I, and preclinical toxicity studies with GLPG0634. The additional studies with GLPG0634 will run in parallel to the efficacy study started today, with the aim to prepare for inclusion of additional dosage arms, should this maximize the potential value of the Phase II study.
About candidate drug GLPG0634
GLPG0634 is an orally-available, novel Janus kinase (JAK) inhibitor with selectivity for JAK1 developed by Galapagos. JAKs are critical components of signaling mechanisms utilized by a number of cytokines and growth factors, including those that are elevated in rheumatoid arthritis patients. JAK inhibitors have shown long-term efficacy in rheumatoid arthritis trials with an early onset of action. Galapagos aims to differentiate GLPG0634 from other JAK inhibitors in development by specifically targeting JAK1, a strategy which could result in a cleaner safety profile.
GLPG0634 has demonstrated excellent activity in in vitro biochemical studies and in vivo models of rheumatoid arthritis, and has successfully completed pre-clinical development and Phase I studies in healthy volunteers.
Galapagos(Euronext: GLPG; OTC: GLPYY) is a mid-size biotechnology company specialized in the discovery and development of small molecule and antibody therapies with novel modes-of-action. The Company is progressing one of the largest pipelines in biotech, with six programs in development and over 50 discovery programs. Through risk/reward-sharing alliances with GlaxoSmithKline, Lilly, Janssen Pharmaceutica, Roche and Servier, Galapagos is eligible to receive up to €2.5 billion in downstream milestones, plus royalties. The Galapagos Group has about 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
Andre Hoekema, SVP Business Development (licensing)
Tel: +31 71 7506 727
Elizabeth Goodwin, Director Investor Relations
Tel: +31 6 2291 6240
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 ACR20 (American College of Rheumatology 20%) response rate signifies a 20% or greater improvement in the number of swollen and tender joints as well as a 20% improvement in three out of five other disease-activity measures.