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Nivolumab

CAS No. : 946414-94-4

產(chǎn)品活性：Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.

研究領域：Immunology/Inflammation

作用靶點：PD-1/PD-L1

In Vitro: Nivolumab binds to CHO cells expressing PD-1 with an EC₅₀ of 1.66 nM, but does not bind to the parental CHO cell line. Nivolumab binds to PD-1 on activated T cells with an EC₅₀ of 0.64 nM. Nivolumab also inhibits the interaction between PD-1 and its ligands, PD-L1 and PD-L2, with IC₅₀ values of 2.52 and 2.59 nM, respectively. Nivolumab (1.5 ng/mL) can enhance T-cell reactivity in the presence of a T-cell receptor stimulus.

In Vivo: Nivolumab (10 and 50 mg/kg, i.v.) is well tolerated in cynomolgus monkeys. Serum chemistry changes are limited to a reversible 28% decrease in T3 at week 13 in females treated with 50 mg/kg. T4 and TSH levels are unchanged. In males treated with 50 mg/kg, there are no changes in T3, T4, or TSH levels. Nivolumab exposure increases in an approximately dose-proportional manner between 10 and 50 mg/kg, with no substantial sex differences noted.

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