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。
| 生物活性 | Zimberelimab is a fully humanIgG4anti-PD-1monoclonal antibody with high affinity and selectivity. Zimberelimab shows antitumor activities and can be used for various cancers research including cervicalcancer, non-small cell lungcancerand classical Hodgkin’s lymphoma[1]. |
体外研究
(In Vitro) | Zimberelimab has an EC50of 210 pM for human PD-1 but does not bind to related CD28 family receptors, such as ICOS, CD28 and CTLA-4[1].
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[1].
Zimberelimab dose-dependently enhances IFN-g production and proliferation by CD4+T cells, saturating at concentrations below 100 pM[1].
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体内研究
(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. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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