TABLE 3.
Parameter | Cohort 1 (300 mg) |
Cohort 2 (600 mg) |
Cohort 3 (1,200 mg) |
Cohort 4 (1,800 mg) |
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---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
n | Mean | SD | CV% | n | Mean | SD | CV% | n | Mean | SD | CV% | n | Mean | SD | CV% | |
Tmax (h) | 6 | 2.18 | 0.94 | 43.15 | 6 | 2.25 | 1.54 | 68.49 | 6 | 1.75 | 1.13 | 64.52 | 6 | 2.50 | 1.52 | 60.66 |
Cmax (ng/mL) | 6 | 408 | 109 | 26.81 | 6 | 782 | 211 | 27.06 | 6 | 1,440 | 571 | 39.62 | 6 | 1,550 | 633 | 40.85 |
AUClast (h · ng/mL) | 6 | 1,810 | 490 | 27.11 | 6 | 3,690 | 694 | 18.80 | 6 | 7,720 | 3,060 | 39.63 | 6 | 11,400 | 5,350 | 47.08 |
AUCinf (h · ng/mL) | 6 | 1,880 | 482 | 25.56 | 6 | 3,810 | 686 | 18.01 | 6 | 8,020 | 3,160 | 39.45 | 5 | 14,100 | 5,880 | 41.66 |
AUCextrap (%) | 6 | 4.43 | 1.90 | 42.90 | 6 | 3.14 | 1.12 | 35.52 | 6 | 3.80 | 1.64 | 43.17 | 5 | 7.23 | 6.31 | 87.33 |
λz (h−1) | 6 | 0.175 | 0.0308 | 17.67 | 6 | 0.134 | 0.0585 | 43.59 | 6 | 0.0851 | 0.0194 | 22.83 | 5 | 0.0774 | 0.0442 | 57.13 |
t1/2 (h) | 6 | 4.08 | 0.773 | 18.93 | 6 | 5.74 | 1.61 | 28.00 | 6 | 8.48 | 1.79 | 21.07 | 5 | 11.7 | 6.80 | 58.05 |
Tlast (h) | 6 | 17.3 | 4.13 | 23.83 | 6 | 23.7 | 4.46 | 18.83 | 6 | 40.0 | 9.03 | 22.58 | 6 | 42.0 | 9.30 | 22.13 |
Clast (ng/mL) | 6 | 13.2 | 1.31 | 9.92 | 6 | 14.0 | 2.45 | 17.53 | 6 | 23.8 | 11.6 | 48.84 | 6 | 51.2 | 42.0 | 81.99 |
CL/F (L/h) | 6 | 167 | 38.2 | 22.83 | 6 | 161 | 27.1 | 16.78 | 6 | 167 | 54.8 | 32.89 | 5 | 145 | 55.4 | 38.25 |
Vz/F (L) | 6 | 990 | 335 | 33.82 | 6 | 1,360 | 436 | 32.09 | 6 | 2,060 | 898 | 43.60 | 5 | 2,040 | 382 | 18.71 |