GLPG0634 at the ACR 2012 in Washington

New data from the EULAR 29013 in Madrid: http://rheumatologe.blogspot.de/2013/06/glpg0634-at-eular-2013.html

GLPG0634 is selective inhibitor of Janus kinase 1 (JAK-1). If you look at the development of NSAIDs you see a similar phenomenon: non-selective NSAIDs that also block COX-1 have certain side effects, whereas COX-2 selective NSAIDs don’t have these side effects. With JAK-inhibitors it seems that JAK-2-driven side effects limit the use of non-selective JAK-inhibitors. GLPG0634 has a 30-fold selectivity for JAK-1 over JAK-2 in human whole blood.

F. Namour and colleagues presented: "Once Daily High Dose Regimens of GLPG0634 in Healthy Volunteers Are Safe and Provide Continuous Inhibition of JAK1 but Not JAK2." (Abstract No. 1331). Conclusion: “At high doses, exceeding those showing high level efficacy in a 4-week RA patient study, GLPG0634 was well tolerated and safe in healthy volunteers. No safety signals were found with GLPG0634; …”

F. Vanhoutte and colleagues presented: "Selective JAK1 Inhibition in the Treatment of Rheumatoid Arthritis: Proof of Concept with GLPG0634" (Abstract No. 2489). Results included: “GLPG0634 met the primary endpoint of significant improvement in ACR20 response rate.” Conclusions included: "These early clinical results are the first to demonstrate that selective inhibition of JAK1 is efficacious and safe for the treatment of RA. Consistent with the lack of inhibition of JAK2, no anemia was observed. ..."

Let´s see if this compound by Galapagos NC is going to make it. If it shows the same efficacy as tofacitinib and has less side effects because of JAK-1 selectivity, well then … but let’s not dream and wait for results of further studies. Of course, we wait eagerly! Good luck, Galapagos!