Table 3.
Summary of pharmacokinetic parameters following dose 1 and 2, and the last dose of GA101
| Parameter | Cohort 1 n = 3 | Cohort 2 n = 3 | Cohort 3 n = 3 | Cohort 4 n = 3 |
|---|---|---|---|---|
| Cycle 1 day 1 (mean ± SD) | ||||
| Dose (mg) | 200 | 400 | 800 | 1200 |
| AUClast (μg × day/mL) | 305 ± 39.5 | 768 ± 109 | 1470 ± 297 | 1970 ± 624 |
| Cmax (μg/mL) | 79.0 ± 17.2 | 157 ± 24.4 | 358 ± 37.2 | 415 ± 81.7 |
| CL (mL/day) | 257 ± 12.6 | 220 ± 49.0 | 347 ± 82.4 | 248 ± 155 |
| t 1/2 (day) | 9.65 ± 2.00 | 10.9 ± 1.80 | 6.11 ± 0.617 | 14.5 ± 8.87 |
| Cycle 1 day 8 (mean ± SD) | ||||
| Dose (mg) | 400 | 800 | 1200 | 2000 |
| AUClast (μg × day/mL) | 1630 ± 283 | 4190 ± 1190 | 6540 ± 1070 | 9340 ± 2060 |
| Cmax (μg/mL) | 201 ± 40.5 | 421 ± 56.4 | 669 ± 124 | 833 ± 186 |
| CL (mL/day) | 115 ± 43.9 | 80.2 ± 43.4 | 108 ± 16.9 | 69.1 ± 11.2 |
| t 1/2 (day) | 17.1 ± 4.68 | 28.1 ± 19.7 | 14.2 ± 1.44 | 30.3 ± 7.88 |
| Cycle 8 (mean ± SD) | ||||
| Dose (mg) | 400 | 800 | 1200 | 2000 |
| AUClast (μg × day/mL) | 3470 ± 1820 | 11 900 ± 7130 | 10 800 ± 722 | 25 100 ± 4970 |
| Cmax (μg/mL) | 359 ± 118 | 1200 ± 698 | 1040 ± 146 | 1910 ± 156 |
| CL (mL/day) | 38.8 ± 31.5 | 29.3 ± 2.61 | 44.1 ± 9.29 | NC |
| t 1/2 (day) | 37.0 ± 19.4 | 25.2 ± 15.0 | 27.2 ± 6.23 | NC |
AUClast, area under curve from time zero to last quantifiable result; CL, clearance; Cmax, maximum concentration; NC, not calculated; t1/2, half‐life.