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CAS No. : 2259860-24-5
MCE 国际站:Zimberelimab
产品活性:Zimberelimab 是一种全人源 IgG4 抗 PD-1 单克隆抗体,具有很高的亲和力和选择性。 Zimberelimab 具有抗肿瘤活性,可用于各种癌症研究,包括宫颈癌、非小细胞肺癌和霍奇金淋巴瘤。
研究领域:Immunology/Inflammation
作用靶点:PD-1/PD-L1
In Vitro: Zimberelimab has an EC50 of 210 pM for human PD-1 but does not bind to related CD28 family receptors, such as ICOS, CD28 and CTLA-4.
Zimberelimab binding to cell-expressed human PD-1 inhibits the interaction of the receptor with both human PD-L1 and PD-L2 with IC50s of 580 pM and 670 pM, respectively.
Zimberelimab dose-dependently enhances IFN-g production and proliferation by CD4+ T cells, saturating at concentrations below 100 pM.
In Vivo: Zimberelimab (10 and 20 mg/kg; i.v.; BIW*3) shows significant anti-tumor effects in mice.
PK parameters of Zimberelimab after single vd administrations of 2, 6, and 18 mg/kg in cynomolgus macaques
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.
相关产品:Rulonilimab | PD-1/PD-L1-IN-19 | [D-Leu-4]-OB3 | NSC622608 | Sulindac | BMS-1166 | PD-1/PD-L1-IN-18 | Pacmilimab | Anti-Mouse PD-L1 Antibody | Vudalimab | PD-1/PD-L1-IN-24 | Cetrelimab | Human PD-L1 inhibitor III | PD-1/PD-L1-IN-20 | PD-1-IN-20 | PD-1/PD-L1-IN 5 | Sintilimab | PD-1/PD-L1-IN-9 hydrochloride | Nivolumab | PD-1/PD-L1-IN-16 | WL12 | PD-1/PD-L1-IN 6 | Acasunlimab | PD-1/PD-L1-IN-14 | PD1-PDL1-IN 1 | Sugemalimab | MAX-10181 | PD-1/PD-L1-IN-23 | D18
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