· In a 4-week multicenter trial GLPG0634 repeats its excellent safety profile: it shows no serious adverse events and an absence of anemia and changes to LDL and liver enzymes, which are typical side-effects reported for other JAK inhibitors
· Clinical improvements seen in RA patients with once-daily dosages of 75-300mg, significant over placebo and the lower 30 mg dose
· Statistically significant improvements in ACR, HAQ-DI, CRP, and DAS28
Mechelen, Belgium; 8 November 2012 – Galapagos NV (Euronext: GLPG) announced today that a second Phase 2A clinical trial with GLPG0634 repeated the excellent safety of the drug, as well as the clinical benefit to RA patients within 4 weeks. Clinical improvements were seen in RA patients with once-daily dosages of 75-300mg. GLPG0634 is the first selective JAK1 inhibitor in development for RA. In February 2012, Galapagos and Abbott announced a global collaboration for GLPG0634 to treat autoimmune diseases.
In this four week, multi-center, Phase 2A trial in 91 RA patients, GLPG0634 was administered in five study arms at a wide range of once-daily dosages of placebo, 30, 75, 150 or 300 mg. Despite the fact that the study was not powered for statistical significance, GLPG0634 did achieve statistically significant improvement in CRP (C-reactive protein), DAS28, HAQ-DI and ACR response rates at the 300mg dose. Efficacy endpoints showed a rapid onset and sustained effect until the end of the study. GLPG0634 was well-tolerated, with none of the patients discontinuing the trial for safety reasons. No serious adverse events were reported. The safety profile of GLPG0634 was confirmed: an absence of the typical findings reported with other JAK inhibitors such as anemia, increases in blood lipids (LDL) and effects on liver enzymes (ALT/AST). An improvement rather than a decrease in hemoglobin was observed in patients receiving GLPG0634.
“This larger, multi-center Phase 2A trial further supports the competitive positioning of GLPG0634: clinical efficacy combined with a differentiated safety profile. This distinguishes GLPG0634 from other JAK inhibitors in development in RA. Dosing between 75 and 300 mg once daily demonstrated activity across several clinical parameters,” said Dr Piet Wigerinck, Chief Scientific Officer of Galapagos. “These results enable us to move rapidly forward into global Phase 2B trials early next year.”
Details of the Phase 2A clinical trial design
The Phase 2A trial for GLPG0634 enrolled 91 patients with active RA (rheumatoid arthritis), showing an insufficient response to the standard-of-care treatment, methotrexate (MTX). The aim was to evaluate the efficacy, safety, tolerability and pharmacokinetics of once-daily dosing of 30 to 300mg of GLPG0634 in treating rheumatoid arthritis. Five groups of patients with active disease took the once-daily regimen of GLPG0634 or placebo for a period of four weeks, while all continued to take their stable background therapy of MTX. Efficacy endpoints included the ACR20 and ACR50 response rates, the disease activity score DAS28, and the reduction in C-reactive protein (CRP), the primary blood marker of inflammation. Galapagos conducted the study in 19 test centers in Hungary (4 sites), Moldova (1), Russia (5), and Ukraine (9).
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 studies with an early onset of action. GLPG0634 differentiates from other JAK inhibitors in development by specifically targeting JAK1, a strategy which could result in a better efficacy and safety profile. GLPG0634 showed excellent clinical benefit and safety in Phase 2A studies in RA patients. GLPG0634 is a fully proprietary program to Galapagos. Upon successful completion of the RA Phase 2B trials, Abbott will license the program and will assume sole responsibility for Phase 3 clinical development, global manufacturing and registration.
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 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 about 800 employees and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More info at: www.glpg.com
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Definitions of clinical parameters
ACR = American College of Rheumatology scores. These response rates signify a 20%, 50% or 70% or greater improvement in the number of swollen and tender joints as well as a similar percentage improvement in three out of five other disease-activity measures.
DAS28 =Disease activity score based on measurement of 28 pre-defined joints.
HAQ-DI = Health Assessment Questionnaire Disability Index, which measures patient health based on a questionnaire completed by the patient.
CRP = C-reactive protein, a blood biomarker for inflammation.