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Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma[1][2]. | [in vivo]
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. |
| [References]
[1] Markham A. Zimberelimab: First Approval. Drugs. 2021 Nov;81(17):2063-2068. DOI:10.1007/s40265-021-01628-5
[2] Lou B, et al. Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer. Front Oncol. 2021 Sep 15;11:736955. DOI:10.3389/fonc.2021.736955 |
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