Table 3.
Summary of the pharmacokinetic parameters in male and female subjects following multiple doses of selisistat
| Parameter | 100 mg selisistat once daily (Male) | 300 mg selisistat once daily (Male) | 100 mg selisistat twice daily (Male) | 100 mg selisistat twice daily (Female) | ||||
|---|---|---|---|---|---|---|---|---|
| Day 1 (n = 6) | Day 7 (n = 6) | Day 1 (n = 6) | Day 7 (n = 6) | Day 1 (n = 6) | Day 7 (n = 6) | Day 1 (n = 6) | Day 7 (n = 6) | |
| AUC(0,τ) (μm h) | 19.2 ± 9.2 | 21.5 ± 12.8 | 108 ± 19.2 | 199 ± 34.7 | 21.5 ± 7.2 | 39.4 ± 22.0 | 49.2 ± 15.9 | 88.3 ± 56.4 |
| (41.0) | (46.8) | (18.3) | (17.0) | (35.5) | (59.1) | (39.8) | (68.2) | |
| AUC(0,∞) (μm h) | 19.3 ± 9.3 | 119 ± 19.7 | 22.1 ± 7.9 | 58.7 ± 23.6 | ||||
| (41.1) | (16.4)* | (37.5) | (50.5) | |||||
| Cmax (μm) | 4.3 ± 1.7 | 4.7 ± 2.2 | 15.3 ± 6.1 | 22.5 ± 9.7 | 5.2 ± 1.0 | 7.3 ± 1.8 | 8.8 ± 2.4 | 13.7 ± 6.2 |
| (36.2) | (38.2) | (41.0) | (45.7) | (21.4) | (24.6) | (28.0) | (41.4) | |
| tmax† (h) | 3.0 | 2.4 | 4.0 | 3.5 | 2.0 | 2.1 | 2.2 | 3.8 |
| (2.00, 4.00) | (1.00, 4.12) | (3.00, 6.00) | (1.02, 6.00) | (1.00, 3.02) | (1.00, 4.00) | (1.00, 3.02) | (3.02, 4.00) | |
| t1/2 (h) | 2.43 ± 0.30 | 4.61 ± 1.26 | 4.76 ± 2.04 | 3.72 ± 0.47 | 1.85 ± 0.51 | 4.55 ± 0.58 | 3.73 ± 1.55 | 4.85 ± 0.70 |
| (12.2) | (28.7) | (42.7)* | (11.9) | (26) | (12.7) | (48.5) | (14.4) | |
| RAobs | 1.12 ± 0.13 | 1.84 ± 0.27 | 1.83 ± 0.48 | 1.79 ± 0.59 | ||||
| (12.1) | (15.9) | (25.7) | (30.0) | |||||
Geometric mean (CV%) data are presented; n = number of subjects studied; *n = 5; †Median (min–max). RAobs, observed accumulation ratio.