TABLE 3.
Filgotinib and GS‐829845 plasma pharmacokinetic parameters and statistical comparisons following administration of filgotinib alone or after multiple doses of rifampin
| Pharmacokinetic parameters |
Filgotinib N = 14 |
Filgotinib + rifampin N = 14 |
%GLSM ratio (90% CI) |
|---|---|---|---|
| Filgotinib | |||
| AUCinf (ng*h/ml) | 6960 (24.7) | 5070 (22.8) | 72.7 (69.1, 76.5) |
| AUClast (ng*h/ml) | 6980 (24.6) | 5050 (22.7) | 72.7 (69.1, 76.5) |
| C max (ng/ml) | 2190 (31.7) | 1640 (34.3) | 74.3 (83.4, 86.4) |
| Tmax (h) | 1.00 (1.00, 2.00) | 1.50 (1.00, 2.00) | — |
| t1/2 (h) | 8.40 (6.70, 10.0) | 7.70 (5.90, 8.60) | — |
| CL/F (L/h) | 30.1 (21.0) | 41.3 (21.2) | — |
| GS−829845 | |||
| AUCinf (ng*h/ml) | 77,400 (25.3) | 47,200 (17.1) | 61.9 (57.9, 66.1) |
| AUClast (ng*h/ml) | 76,700 (24.8) | 47,100 (17.0) | 62.3 (58.4, 66.4) |
| C max (ng/ml) | 2900 (15.1) | 2340 (12.8) | 81.0 (76.8, 85.4) |
| Tmax (h) | 4.00 (3.00, 4.00) | 4.00 (3.00, 4.00) | — |
| t1/2 (h) | 15.9 (14.8, 18.9) | 12.4 (11.7, 13.9) | — |
| Combined exposure | |||
| AUCeff (ng*h/ml) | 66.6 (58.6, 75.7) | ||
Data are presented as mean (percentage coefficient of variation) except for t 1/2 and T max which are presented as median (first quartile and third quartile).
Abbreviations: AUCeff, effective area under the concentration versus time curve; AUCinf, area under the concentration versus time curve to infinity; AUClast, area under the concentration versus time curve from time zero to the last quantifiable concentration; CI, confidence interval; CL/F, total apparent clearance; Cmax, maximum concentration; GLSM ratio, geometric least square mean ratio; t1/2, terminal half‐life; Tmax, time to maximum concentration.