Zimberelimab (10 and 20 mg/kg; i.v.; BIW*3) shows significant anti-tumor effects in mice[2].
PK parameters of Zimberelimab after single vd administrations of 2, 6, and 18 mg/kg in cynomolgus macaques[2]
| PK parameters | 2 mg/kg | 6 mg/kg | 18 mg/kg |
| C0 (mg/mL) | 103 ± 23.7 (23.0%) | 157 ± 18.7 (11.9%) | 508 ± 48.0 (9.46%) |
| T1/2 (h) | 111 ± 23.7 (30.5%) | 115 ± 32.8 (28.5%) | 129 ± 17.0 (13.1%) |
| Vss (mL/kg) | 48.4 ± 7.48 (15.5%) | 49.4 ± 6.49 (13.1%) | 46.3 ± 5.49 (11.8%) |
| Cl (mL/h/kg) | 0.288 ± 0.0373 (13.0%) | 0.278 ± 0.0308 (11.1%) | 0.183 ± 0.0293 (16.0%) |
| Tlast (h) | 396 ± 141 (35.5%) | 704 ± 203 (28.9%) | 816 ± 0.00 |
| AUC0-last (h*mg/mL) | 6300 ± 1320 (21.0%) | 21300 ± 2570 (12.1%) | 98100 ± 16300 (16.6%) |
| AUCo?inf (h*mg/mL) | 7060 ± 1020 (14.5%) | 21800 ± 2310 (10.6%) | 101000 ± 16700 (16.6%) |
| MRT0-last (h) | 126 ± 23.3 (18.4%) | 164 ± 31.2 (19.0%) | 236 ± 14.8 (6.27%) |
| MRT0-inf (h) | 170 ± 29.7 (17.5%) | 180 ± 29.4 (16.4%) | 255 ± 17.4 (6.82%) |
| AUC0-inf/AUC0-last (%) | 113 ± 11.8 (10.4%) | 103 ± 0.940 (0.916%) | 103 ± 0.940 (0.916%) |
C
0, initial drug concentration; T
1/2, half-life; V
ss, apparent volume of distribution in the steady-state; Cl, clearance; T
last, the last time; AUC, area under the curve; MRT, mean residence time.
| Animal Model: | The human PD-1 knock-in mouse model of MC38 tumors[2] |
| Dosage: | 10 and 20 mg/kg |
| Administration: | Intravenous injection, BIW*3 |
| Result: | Showed statistically significant anti-tumor effects comparable with Pembrolizumab (HY-P9902). |
| Animal Model: | Nine male and nine female cynomolgus monkeys[2] |
| Dosage: | 2, 6, and 18 mg/kg |
| Administration: | Intravenous injection (Pharmacokinetic Analysis) |
| Result: | Displays long-term effects in cynomolgus monkeys, without differences between males and females. |
