TABLE 4.
Arithmetic means ± standard deviation of different pharmacokinetic parameters of the SAD study, measured in plasma. SAD, single ascending dose
| SAD pharmacokinetics in plasma | |||||
|---|---|---|---|---|---|
| LTI‐291 dose | 3 mg (n = 8) | 10 mg (n = 8) | 10 mg (n = 8) | 30 mg (n = 8) | 90 mg (n = 8) |
| Nutritional state | Fasted | Fasted | Fed | Fasted | Fasted |
| Cmax (ng/mL) | 110 ± 13 | 350 ± 131 | 243 ± 75 | 997 ± 283 | 2750 ± 786 |
| t½ (h) | 23.6 ± 11.1 | 23.6 ± 8.3 | 25.3 ± 10.1 | 24.3 ± 7.7 | 23.9 ± 6.1 |
| λz (h−1) | 0.0366 ± 0.0185 | 0.0334 ± 0.0137 | 0.0324 ± 0.0156 | 0.0314 ± 0.0109 | 0.0304 ± 0.0064 |
| AUC0‐last (ng*h/mL) | 1600 ± 383 | 5760 ± 965 | 5950 ± 1130 | 18 700 ± 3920 | 48 400 ± 8790 |
| AUC0‐inf (ng*h/mL) | 2350 ± 703 | 7820 ± 2300 | 8860 ± 2670 | 24 800 ± 3050 | 64 000 ± 10 200 |
| CL/F (L) | 1.38 ± 0.40 | 1.37 ± 0.35 | 1.22 ± 0.36 | 1.23 ± 0.15 | 1.44 ± 0.21 |
| Vz/F (L) | 42.7 ± 15.8 | 43.5 ± 9.9 | 40.7 ± 9.9 | 43.4 ± 15.8 | 49.1 ± 12.4 |
| Cmax/dose (ng/mL/mg) | 36.7 ± 4.4 | 35 ± 13.1 | 24.3 ± 7.5 | 33.2 ± 9.4 | 30.5 ± 8.7 |
| AUC0‐inf/dose (ng*h/mL/mg) | 783 ± 234 | 782 ± 230 | 886 ± 267 | 827 ± 102 | 711 ± 113 |
| Median T max (h) (min, max) | 1.48 (1.00, 2.00) | 1.01 (1.00, 4.02) | 8.00 (4.00, 12.00) | 3.02 (1.00, 4.00) | 2.00 (1.00, 8.17) |