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.
.
No comments:
Post a Comment