Parameter Statistic 5 mg 15 mg 40 mg 80 mg 80 mg fed 120 mg
n/nmiss 6/0 6/0 6/0 6/0 6/0 a 5/0
AUC0-∞ (nmol∙h/L) Mean (SD) 786 (298) 2360 (481) 6280 (1650) 9180 (1510) 14800 (5650) a 17300 (4620)
Median (Min, Max) 707 (516, 1280) 2150 (1970, 3120) 6490 (3660, 7960) 9400 (6570, 10900) 11700 (11400, 21300) 15900 (11900, 22900)
Geometric mean 743 2330 6070 9060 14200 16800
Geometric CV (%) 37.2 19.4 30.2 17.9 36.5 27.5
AUC0-t (nmol∙h/L) Mean (SD) 633 (281) 2160 (412) 5760 (1500) 8260 (1230) 6410 (2330) 17100 (4680)
Median (Min, Max) 544 (371, 1120) 1990 (1790, 2840) 5900 (3490, 7350) 8460 (6000, 9630) 5430 (4700, 11000) 15700 (11500, 22700)
Geometric mean 588 2130 5580 8170 6140 16600
Geometric CV (%) 43.2 18.2 29.1 16.4 31.4 28.5
AUC0-8h (nmol∙h/L) Mean (SD) NC NC NC 4900 (685) 6410 (2330) NC
Median (Min, Max) 5070 (3580, 5550) 5430 (4700, 11000)
Geometric mean 4850 6140
Geometric CV (%) 15.6 31.5
Cmax (nmol/L) Mean (SD) 73.6 (18.4) 227 (33.0) 756 (298) 936 (224) 1370 (607) 1940 (326)
Median (Min, Max) 72.3 (51.6, 104) 233 (179, 276) 633 (469, 1240) 905 (678, 1330) 1120 (880, 2530) 2050 (1550, 2260)
Geometric mean 71.8 225 712 916 1280 1910
Geometric CV (%) 25.0 14.9 38.3 23.2 39.2 17.5
tmax (h) Median (Min, Max) 1.0 (0.7, 3.0) 2.0 (1.0, 4.0) 1.5 (0.7, 3.0) 1.0 (0.7, 3.0) 3.0 (1.0, 8.0) 1.0 (0.7, 1.0)
t1/2 (h) Mean (SD) 6.4 (1.9) 6.6 (0.9) 6.6 (0.9) 7.1 (1.0) 6.7 (1.4) a 6.9 (1.2)
Median (Min, Max) 6.3 (4.1, 9.0) 6.8 (5.1, 7.6) 6.5 (5.6, 7.6) 6.7 (6.2, 8.8) 6.9 (5.2, 8.1) 7.3 (4.9, 7.7)
CL/F (L/h) Mean (SD) 25.7 (8.6) 23.8 (4.3) 24.9 (8.1) 32.5 (6.2) 21.3 (6.6) a 26.6 (7.2)
Median (Min, Max) 25.8 (14.2, 35.1) 25.4 (17.4, 27.7) 22.4 (18.2, 39.7) 31.0 (26.5, 44.2) 24.8 (13.6, 25.4) 27.5 (19.0, 36.6)
Geometric mean 24.4 23.4 23.9 32.1 20.5 25.9
Geometric CV (%) 37.2 19.4 30.2 17.9 36.5 27.5
Vz/F (L) Mean (SD) 225 (58.6) 223 (41.7) 234 (64.3) 328 (59.0) 205.3 (77.6) a 260 (56.5)
Median (Min, Max) 230 (159, 316) 227 (167, 275) 219 (160, 320) 304 (276, 430) 191 (136, 289) 260 (196, 327)
Geometric mean 219 220 226 324 196 256
Geometric CV (%) 26.7 19.4 28.0 17.0 39.3 22.3