NCA parameter | | | | | |
Cmax (ng/ml) | 1268 | 3733 | 8826 | | |
Cmax/dose (ng/ml)/(mg/kg) | 127 | 124 | 147 | | |
Tmax (h) | 0.25 | 0.5 | 0.25 | | |
AUCinf (ng/h per milliliter) | 1781 | 5522 | 13,877 | | |
AUCinf/dose (ng/h per milliliter)/(mg/kg) | 178 | 184 | 231 | | |
t1/2 (h) | 1.1 | 1.0 | 1.5 | | |
Modeled parameters (using C(T) = D/V × exp(–K10 × T)) | | | | | |
V (ml/kg) | 6378 | 6459 | 5436 | | 6091 |
K10 (1/h) | 0.8424 | 0.7811 | 0.8075 | | 0.810 |
| Rat, Sexes Combined | | | | |
| 15 mg/kg | 45 mg/kg | 90 mg/kg | | Meanb |
NCA parameter | | | | | |
Cmax (ng/ml) | 2769 | 6982 | 24,899 | | |
Cmax/dose (ng/ml)/(mg/kg) | 185 | 155 | 277 | | |
Tmax (h) | 0.25 | 0.25 | 0.25 | | |
AUCinf (ng/h per milliliter) | 4199 | 14,114 | 52,563 | | |
AUCinf/dose (ng/h per milliliter)/(mg/kg) | 280 | 314 | 578 | | |
t1/2 (h) | 1.18 | 1.95 | 1.91 | | |
Modeled parameters (using C(T) = A × exp(–alpha × T) + B × exp(–beta × T)) | | | | | |
V1 (ml/kg) | 3816 | 3862 | 1518 | | 3839 |
K10 (1/h) | 0.87 | 0.77 | 1.09 | | 0.82 |
K12 (1/h) | 0.61 | 1.63 | 3.49 | | 1.12 |
K21 (1/h) | 1.14 | 1.68 | 2.31 | | 1.41 |
| Cynomolgus Macaque, Sexes Combined | | | | |
| 1 mg/kg | 3 mg/kg | 10 mg/kg | 30 mg/kg | Meanc |
NCA parameter | | | | | |
Cmax (ng/ml) | 161 | 539 | 1599 | 4633 | |
Cmax/dose (ng/ml)/(mg/kg) | 161 | 180 | 160 | 154 | |
Tmax (h) | 4.0 | 3.5 | 3.75 | 5.75 | |
AUCinf (ng/h per milliliter) | 2287 | 5710 | 21,746 | 65,372 | |
AUCinf/dose (ng/h per milliliter)/(mg/kg) | 2287 | 1903 | 2175 | 2179 | |
t1/2 (h) | 11.5 | 6.49 | 6.95 | 6.27 | |
Modeled parameters (using C(T) =K × (D/V) × T × exp(–K × T)) | | | | | |
V_F (ml/kg) | 2466 | 2171 | 2324 | 2663 | 2406 |
K (1/h) | 0.3 | 0.32 | 0.26 | 0.22 | 0.274 |
Tlag (h)d | 0.39 | 0.45 | 0.41 | 0.52 | 0.440 |