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Cetrelimab

CAS No. : 2050478-92-5

MCE 国际站：Cetrelimab

产品活性：Cetrelimab (JNJ 63723283; JNJ 3283) 是一种靶向 PD-1 的人源化 IgG4κ 单克隆抗体。Cetrelimab 结合 PD-1 的 K_d 为 1.72 nM (HEK293 细胞)。由此，Cetrelimab 阻断 PD-1 与 PD-L1 和 PD-L2 的相互作用 (IC₅₀ 分别为 111.7 ng/mL 和 138.6 ng/mL)。Cetrelimab 还刺激外周 T 细胞，增加细胞因子 (IFN-γ, IL-2, TNF-α) 水平，并抑制体内肿瘤生长。

研究领域：Immunology/Inflammation | Apoptosis

作用靶点：PD-1/PD-L1 | Interleukin Related | TNF Receptor

In Vitro: Cetrelimab (0.01-30 nM; 5 d) binds to endogenous PD-1 on activated CD4⁺ ａnd CD8⁺ T cells with EC₅₀s of 0.16-0.22 g/mL ａnd 0.17-0.22 g/mL, respectively.
Cetrelimab (0.01-30 µg/mL; 24 h) reverse PD-1-mediated suppression of TCR signaling in Jurkat-PD-1 NFAT reporter cells with CHO-K1 expressing PD-L1.
Cetrelimab (0.001-100 nM; 6 d) increases IFN-γ, IL-2, ａnd TNF-α with EC₅₀s of 0.08 ng/mL, 0.07 ng/mL, ａnd 0.02 ng/mL, respectively.
Cetrelimab binds to PD-1 in cynomolgus with a K_d value of 0.9 nM.

In Vivo: Cetrelimab (10 mg/kg; i.p.; single dose) has antitumor efficacy, ａnd decreases tumor volume in PD-1 knock-in (hPD-1KI) mice with MC38 tumor.
Cetrelimab (10 mg/kg; i.p.; once every 5 days for 30 d) results significant increases in peripheral blood CD8⁺ T cells in patient-derived xenograft (PDX) lung model in mice.
Cetrelimab (10-100 mg/kg; i.v.; once weekly for 5 weeks) has well tolerance in cynomolgus model.
Cetrelimab (0.1-10 mg/kg; i.v.; single dose, monitored for 57 d) shows an nonlinear pharmacokinetics (PK) in cynomolgus, possibly attributable to target-mediated drug deposition (TMDD).

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