Table 2.
Pharmacokinetics of filgotinib and its primary metabolite after repeated oral doses of filgotinib 200 mg once daily
| Source | Subjects | Filgotinib | Primary metabolite | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Cmax, µg/mL | tmax, h | AUCτ, μg·h/mL | t½, h | Cmax, µg/mL | tmax, h | AUCτ, μg·h/mL | t½, h | ||
| Namour et al. [13] |
Healthy subjects (n = 6) |
1.20 (42.0) | 2.00 (1.00–2.00) | 4.45 (30.0) | 5.17 (39.1)a | 3.54 (21.2) | 5.00 (3.00–5.00) | 69.9 (25.6) | 27.3 (7.81) |
| Namour et al. [29] |
Japanese healthy subjects (n = 6) |
3.77 (53.2) | 6.08 (27.8) | 6.35 (35.4) | 5.09 (8.99) | 81.4 (12.5) | 16.7 (14.6) | ||
| Namour et al. [29] |
White healthy subjects (n = 6) |
3.06 (51.0) | 5.58 (21.3) | 10.7 (67.9) | 3.87 (36.4) | 62.1 (27.0) | 19.6 (23.7) | ||
| SmPC [10] | RA (n = 37) | 2.15 (48.1) | 6.77 (43.7) | 4.43 (29.3)b | 83.2 (27.3)b | ||||
| SmPC [10] | UC (n = 13) | 2.12 (50.3) | 6.15 (28.1)c | 4.02 (30.5) | 72.1 (33.9)d | ||||
Estimates are arithmetic means (CV%) except median (range) for tmax.
AUC∞ area under the plasma concentration–time curve from time zero to infinity, AUCτ area under the plasma concentration–time curve during a dosage interval (τ), Cmax maximum (peak) plasma drug concentration, CV coefficient of variation, RA rheumatoid arthritis, SmPC summary of product characteristics, t½ apparent terminal half-life, tmax time to reach Cmax following drug administration, UC ulcerative colitis
an = 5
bn = 33
cn = 12
dn = 1