Table 1. PK parameters of JS-001 after single vd administrations of 1, 10, and 75 mg/kg in cynomolgus macaques (mean±SD, n=6).
PK parameters | Units | Group 2 1 mg/kg | Group 3 10 mg/kg | Group 4 75 mg/kg |
---|---|---|---|---|
t1/2_7 d | h | 133.91±19.50 | 168.87±50.96 | 193.79±27.5* |
t1/2_14 d | h | 64.48±41.70 | 114.16±42.82 | 156.32±53.99* |
t1/2a | h | 35.13±16.14 | 36.82±4.75 | 34.96±5.74 |
Tmax | h | 0.5±0 | 0.5±0 | 0.5±0 |
Cmax | μg/mL | 27.70±12.29 | 216.11±34.52** | 1891.72±270.16**,## |
AUC(0–t) | h·μg·mL−1 | 2744.55±834.19 | 31075.53±9849.79** | 269472.4±50585.96**,## |
AUC(0–inf) | h·μg·mL−1 | 2749.51±833.39 | 31096.05±9849.95** | 269488.17±50574.79**,## |
AUC(t–inf)% | % | 0.20±0.26 | 0.07±0.06 | 0.01±0.01# |
Vd | mL/kg | 18.22±3.77 | 17.94±3.63 | 14.28±2.54 |
CLs | mL·h−1·kg−1 | 0.39±0.12 | 0.35±0.09 | 0.29±0.05 |
MRT | h | 121.91±38.84 | 147.5±62.6 | 149.25±24.68 |
note: t1/2_7 d and t1/2_14 d, effective half-time, which was calculated by terminal phase data harvested from the first 7 or 14 d;
a t1/2: terminal t1/2, calculated by total terminal phase data;
*P<0.05,
**P<0.01 vs Group 2;
#P<0.05,
##P<0.01 vs Group 3.