Table 2.
Pharmacokinetic parameters of TAS‐205 in the single‐ and repeated‐dose periods
| Single‐dose period | |||||||
|---|---|---|---|---|---|---|---|
| Step | Summary statistics | t1/2 (h) | t max (h) | C max (ng/mL) | AUC0‐48 (ng·h/mL) | AUC0‐inf (ng·h/mL) | Ae (%) |
| 1 (n = 5) | Mean (SD) or median (min–max) | 8.61 (4.20) | 2.00 (0.50–2.00) | 839 (383) | 2729 (901) | 2759 (936) | 24.98 (3.81) |
| CV (%) | 48.7 | NA | 45.6 | 33.0 | 33.9 | 15.3 | |
| 2 (n = 5) | Mean (SD) or median (min–max) | 7.70 (3.16) | 2.00 (1.00–2.00) | 1847 (996) | 5946 (2967) | 5962 (2967) | 26.53 (3.84) |
| CV (%) | 41.1 | NA | 53.9 | 49.9 | 49.8 | 14.5 | |
| 3 (n = 5) | Mean (SD) or median (min–max) | 7.05 (4.07) | 2.00 (1.00–2.00) | 3202 (1493) | 9401 (3493) | 9446 (3646) | 31.89 (9.40) |
| CV (%) | 57.8 | NA | 46.6 | 37.2 | 38.6 | 29.5 | |
| Repeated‐dose period | |||||||
| Day 1 | Day 7 | Day 4 | Day 7 | ||||
| Step | Summary statistics | t max, day 1 (h) | C max, day 1 (ng/mL) | t max, day 7 (h) | C max, day 7 (ng/mL) | Cpre, day 4 (ng/mL) | Cpre, day 7 (ng/mL) |
| A (n = 5) | Mean (SD) or median (min–max) | 2.00 (1.00–2.00) | 1004 (656) | 2.00 (2.00–2.00) | 891 (297) | 42.9 (19.9) | 41.1 (14.2) |
| CV (%) | NA | 65.3 | NA | 33.3 | 46.3 | 34.6 | |
| B (n = 5) | Mean (SD) or median (min–max) | 2.00 (1.00–2.00) | 1894 (691) | 2.00 (1.00–2.00) | 2322 (776) | 68.94 (41.0) | 70.9 (36.0) |
| CV (%) | NA | 36.5 | NA | 33.4 | 59.6 | 50.7 | |
| C (n = 3) | Mean (SD) or median (min–max) | 2.00 (2.00–4.00) | 2635 (2813) | 2.00 (0.50–2.00) | 4660 (3671) | 75.9 (34.7) | 98.7 (55.7) |
| CV (%) | NA | 106.8 | NA | 78.8 | 45.8 | 56.5 | |
SD, standard deviation; CV, coefficient of variation; C max, maximum plasma concentration; AUC0‐48, area under the plasma concentration–time curve from 0 to 48 h post‐dose; AUC0‐inf, AUC to infinite time; t1/2, half‐life of elimination; Ae, urinary excretion rate; t max, time to maximum plasma concentration; Cpre, trough plasma concentration.