Table 3.
Summary of pharmacokinetic parameters for selisistat in male and female subjects following 14 days of treatment at 10 and 100 mg once daily
| Parameter | Males | Females | ||||||
|---|---|---|---|---|---|---|---|---|
| 10 mg (n = 14) | 100 mg (n = 13) | 10 mg (n = 3) | 100 mg (n = 6) | |||||
| Day 1 | Day 14 | Day 1 | Day 14 | Day 1 | Day 14 | Day 1 | Day 14 | |
| AUC(0,τ) (μm h) | 2.87 ± 1.44 | 2.55 ± 1.14 | 33.4 ± 12.11 | 42.5 ± 21.4 | 2.94 ± 1.10 | 3.44 ± 1.53 | 44.9 ± 44.1 | 60.0 ± 49.7 |
| (50.2) | (44.7) | (36.3) | (50.4) | (37.4) | (44.5) | (98.2) | (92.8) | |
| AUC(0,∞) (μm h) | 3.02 ± 1.41 | NA | 34.3 ± 13.9 | NA | 3.03 ± 1.14 | NA | 48.1 ± 49.7 | NA |
| (46.7) | (40.4) | (37.6) | (103.3) | |||||
| Cmax (μm) | 0.65 ± 0.32 | 0.57 ± 0.22 | 5.99 ± 1.49 | 5.87 ± 1.93 | 0.77 ± 0.15 | 0.61 ± 0.07 | 7.51 ± 3.91 | 7.74 ± 4.42 |
| (49.2) | (38.6) | (24.9) | (32.9) | (19.5) | (11.5) | (52.1) | (57.1) | |
| tmax (h) | 3.00 | 2.00 | 3.00 | 3.00 | 3.00 | 3.00 | 3.00 | 3.46 |
| (1.00, 4.15) | (0.50, 4.00) | (1.00, 4.00) | (1.05, 6.00) | (3.00, 3.00) | (3.00, 3.00) | (2.97, 3.32) | (0.98, 4.00) | |
| t1/2 (h) | 2.51 ± 1.42 | 2.33 ± 0.85 | 2.86 ± 1.30 | 3.33 ± 1.56 | 2.12 ± 0.46 | 2.20 ± 0.55 | 3.20 ± 2.04 | 3.41 ± 1.64 |
| (56.6) | (36.5) | (45.5) | (46.8) | (21.7) | (25.0) | (63.8) | (48.1) | |
| RAobs | NA | 0.89 | NA | 1.27 | NA | 1.17 | NA | 1.33 |
Arithmetic means ± SD (coefficient of variation %), except for tmax, where median (range) is reported. τ, dosage interval, 24 h; AUC, area under the plasma concentration–time curve; Cmax, peak plasma concentration; NA, not applicable; RAobs, observed accumulation ratio; t1/2, half-life; tmax, time to peak concentration.