GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) being developed by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases. JAKs are critical components of signaling mechanisms utilized by a number of cytokines and growth factors, including those that are elevated in rheumatoid arthritis (RA) patients. JAK inhibitors have shown long-term efficacy in RA trials with an early onset of action.
In November 2011 Galapagos announced that GLPG0634 achieved the primary endpoint (ACR20) of significant improvement in the signs and symptoms of rheumatoid arthritis at four weeks in a single center study. 83% of patients receiving GLPG0634 reached the ACR20 score and half of the GLPG0634-treated patients went into either disease remission or low disease activity. Furthermore, this compound showed a unique safety profile, with a clean profile on LDL/cholesterol and no anemia observed. In a second Phase 2, dose-range finding clinical trial in multiple centers reported in November 2012, 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, and this strategy could result in a cleaner safety profile than other JAK inhibitors.
On 29 February 2012 Galapagos signed a global agreement with AbbVie to develop and commercialize GLPG0634. For more information about the deal, read the press release.
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