Filgotinib at the ACR 2015 Meeting in San Francisco

There have been seven publications on Filgotinib at the ACR 2015 Annual Meeting in San Francisco. Filgotinib (already known as: GLPG0634) is a novel oral, potent and selective JAK1 inhibitor.

R Westhovens and colleagues presented results from a phase 2B dose ranging study over 12 weeks. Conclusion: "Over 12 weeks, filgotinib in combination with MTX demonstrated consistent efficacy on signs and symptoms of active RA with a rapid onset of action. [...]"

Arthur Kavanaugh et al. also looked at results from a phase 2B dose ranging study over 12 weeks. The reported on filgotinib as monotherapy. Conclusion: "Over 12 weeks, filgotinib as monotherapy demonstrated clear efficacy in treating the signs and symptoms of active RA with a rapid onset of action. Overall safety profile was favorable and consistent with previous studies conducted in RA with filgotinib."

Namour Florence and colleagues presented data in the influende of age and renal impairment from phase 1 studies. Conclusion: "Higher age and mild to moderate impairment of renal function has a limited impact on the PK [pharmacokinetics] of filgotinib. In severe renal impairment, the exposure to filgotinib’s active metabolite is elevated, consistent with its renal elimination pathway. This was not associated with safety signals in these Phase 1 studies."

There were of course more studies: René Galien and colleagues (filgotinib) decreases plasma markers of inflammation and joint damage), René Galien and another team (filgotinib changes lipid profile with a preferential increase in HDL), Namour Florence et al. (filgotinib shows similar pharmacokinetics and pharmacodynamics profiles in Japanese and Caucasian healthy volunteers), and René Galien and colleagues (further evidence for the JAK1 selectivity of filgotinib).

All in all, filgotinib has presented data up to 12 weeks. We have to wait for a phase 3 study ... and much longer for data on radiographic progression.

References:

Westhovens R, Alten R, Pavlova D, Enríquez-Sosa F, Mazur M, Greenwald M, Van der Aa A, Vanhoutte F, Tasset C, Harrison P. Filgotinib (GLPG0634), an Oral JAK1 Selective Inhibitor Is Effective in Combination with Methotrexate in Patients with Active Rheumatoid Arthritis: Results from a Phase 2B Dose Ranging Study [abstract]. Arthritis Rheumatol.2015; 67 (suppl 10). http://acrabstracts.org/abstract/filgotinib-glpg0634-an-oral-jak1-selective-inhibitor-is-effective-in-combination-with-methotrexate-in-patients-with-active-rheumatoid-arthritis-results-from-a-phase-2b-dose-ranging-study/. Accessed November 18, 2015.

Kavanaugh A, Ponce L, Cseuz R, Reshetko O, Stanislavchuk MA, Greenwald M, Van der Aa A, Vanhoutte F, Tasset C, Harrison P. Filgotinib (GLPG0634), an Oral JAK1 Selective Inhibitor Is Effective As Monotherapy in Patients with Active Rheumatoid Arthritis: Results from a Phase 2B Dose Ranging Study [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/filgotinib-glpg0634-an-oral-jak1-selective-inhibitor-is-effective-as-monotherapy-in-patients-with-active-rheumatoid-arthritis-results-from-a-phase-2b-dose-ranging-study/. Accessed November 18, 2015.

Florence N, Fagard L, Van der Aa A, Goss S, Harrison P, Tasset C. Influence of Age and Renal Impairment on Pharmacokinetics of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/influence-of-age-and-renal-impairment-on-pharmacokinetics-of-filgotinib-glpg0634-a-selective-jak1-inhibitor/. Accessed November 18, 2015.

Galien R, Van der Aa A, Blanque R, Darquenne S, Harrison P, Tasset C. Selective JAK1 Inhibition with Filgotinib (GLPG0634) Decreases Plasma Markers of Inflammation and Joint Damage in Patients with Rheumatoid Arthritis [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/selective-jak1-inhibition-with-filgotinib-glpg0634-decreases-plasma-markers-of-inflammation-and-joint-damage-in-patients-with-rheumatoid-arthritis/. Accessed November 18, 2015.

Galien R, Harrison P, Brys R, Van der Aa A, van 't Klooster G, Tasset C. 4-Week Treatment of Rheumatoid Arthritis Patients with the JAK1-Selective Inhibitor Filgotinib (GLPG0634) Changes Lipid Profile with a Preferential Increase in HDL [abstract]. Arthritis Rheumatol.2015; 67 (suppl 10). http://acrabstracts.org/abstract/4-week-treatment-of-rheumatoid-arthritis-patients-with-the-jak1-selective-inhibitor-filgotinib-glpg0634-changes-lipid-profile-with-a-preferential-increase-in-hdl/. Accessed November 18, 2015.

Florence N, Vayssière B, Galien R, Fagard L, Van der Aa A, Goss S, Harrison P, Tasset C. Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, Shows Similar Pharmacokinetics and Pharmacodynamics Profiles in Japanese and Caucasian Healthy Volunteers [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/filgotinib-glpg0634-a-selective-jak1-inhibitor-shows-similar-pharmacokinetics-and-pharmacodynamics-profiles-in-japanese-and-caucasian-healthy-volunteers/. Accessed November 18, 2015.

Galien R, Brys R, Van der Aa A, Harrison P, Tasset C. Absence of Effects of Filgotinib on Erythrocytes, CD8+ and NK Cells in Rheumatoid Arthritis Patients Brings Further Evidence for the JAK1 Selectivity of Filgotinib [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/absence-of-effects-of-filgotinib-on-erythrocytes-cd8-and-nk-cells-in-rheumatoid-arthritis-patients-brings-further-evidence-for-the-jak1-selectivity-of-filgotinib/. Accessed November 18, 2015.

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