Nivolumab (anti-PD-1)

Nivolumab (anti-PD-1) is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer^[1]. In Vitro: Nivolumab (anti-PD-1) 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 (anti-PD-1) binds to PD-1 on activated T cells with an EC₅₀ of 0.64 nM. Nivolumab (anti-PD-1) 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 (anti-PD-1) (1.5 ng/mL) can enhance T-cell reactivity in the presence of a T-cell receptor stimulus^[1]. In Vivo: Nivolumab (anti-PD-1) (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 (anti-PD-1) exposure increases in an approximately dose-proportional manner between 10 and 50 mg/kg, with no substantial sex differences noted^[1].