Table 3.
Pharmacokinetic parameters of trebananib
| Week 1 | Week 4 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| T max (h) | C max (μg/mL) | AUC0-168 (h*μg/mL) | T max (h) | C max (μg/mL) | AUC0-168 (h*μg/mL) | t 1/2, z (h) | CL (mL/h/kg) | V ss (mL/kg) | AUC0-168 AR | C min (μg/mL) |
| 3 mg/kg | ||||||||||
| n = 6 | n = 6 | |||||||||
| 1.07 (1.03–1.08) | 52.3 (11.3) | 1,760 (582) | 1.07 (1.02–2.03) | 59.0 (10.1) | 2,170 (715) | 95.9 (35.1) | 1.50 (0.423) | 158 (49.0) | 1.24 (0.0514) | 5.32 (2.54) |
| 10 mg/kg | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| n = 6 | n = 5 | |||||||||
| 1.03 (1.02–1.05) | 239 (47.1) | 4,630 (925) | 1.02 (1.02–2.02) | 277 (48.8) | 5,880 (560) | 95.4 (14.8) | 1.71 (0.165) | 121 (22.2) | 1.19 (0.0686) | 7.27 (1.52) |
| 30 mg/kg | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| n = 6 | n = 6 | |||||||||
| 1.17 (1.02–2.00) | 551 (86.8) | 18,000 (4,490) | 1.51 (1.03–2.02) | 689 (105) | 21,200 (2,910) | 93.9 (25.6) | 1.44 (0.191) | 137 (30.3) | 1.21 (0.214) | 45.1 (16.2) |
All parameters are reported as mean (standard deviation) values, except for T max, which is reported as a median (range) value
AUC0-168 = The area under serum concentration–time curve from time 0 to 168 h post-dose, AUC0-168 AR = The AUC0-168 accumulation ratio (=[AUC0-168 on week 4]/[AUC0-168 on week 1]), CL = The apparent total clearance (=[actual dose]/[AUC0-168 on week 4]), C max = The maximum observed serum concentration after dosing, C min = The serum concentration at 168 h after dosing, t 1/2, z = The estimated terminal-phase half-life (=ln(2)/λz, where λz is the terminal rate constant estimated via linear regression of the terminal log-linear decay phase), T max = The time at which C max was observed, V ss = The volume of distribution at steady state (=MRT*CL, where MRT is the mean residence time.)