GLPG0634 at the EULAR 2013

GLPG0634 is selective inhibitor of Janus kinase 1 (JAK-1). And I had been quite thrilled by this new drug at the ACR 2012 in Washington. Now, I was eager to see, what new developments would be presented at the EULAR 2013 in Madrid.

B. Vayssiere and colleagues presented a rodent study [THU0116]: “Biological effects of the jak1 selective inhibitor GLPG0634 on inflammation markers in arthritic mice”. Conclusions: “ … These data establish that selective JAK1 inhibition by GLPG0634 is sufficient to mediate strong efficacy in an established arthritis model …”. That wasn’t so thrilling.

F. P. Vanhoutte and colleagues presented [THU0229]: “Safety and efficacy of GLPG0634, a selective JAK1 inhibitor in patients with rheumatoid arthritis: results of a 4-week phase II a dose ranging, multi-center trial”. Conclusions: “These early clinical results demonstrate that selective inhibition of JAK1 by once-daily dosing of GLPG0634 from 75 mg to 300 mg is efficacious and generally well tolerated for 4-weeks treatment of RA, and confirm data from a previous study at a 200 mg daily dose. A dose of 30 mg QD was suboptimal for efficacy. Larger, longer term studies in RA are being initiated to evaluate optimal doses for efficacy and safety.” I looked into the results and agree with the authors’ conclusions.

F. Namour and colleagues presented a third study [THU0236]: “Once-daily dosing of GLPG0634, a selective JAK1 inhibitor, is supported by its active metabolite“. Conclusions: “The results of these studies indicate that an active metabolite supports the activity of GLPG0634. The long half-life of this metabolite provides a lasting effect, though at a lower level of JAK1 inhibition than GLPG0634. …”.

As EMEA seems to be reluctant to approve tofacitinib, maybe GLPG0634 has a better chance. With two PK inhibitors prices might come down to level, where it’s affordable for society. So I wish both drugs good luck!

Link:
http://rheumatologe.blogspot.de/2012/12/glpg0634-at-acr-2012-in-washington.html