Nivolumab

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].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1

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].

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].

[1]. Wang C, et al. In vitro characterization of the anti-PD-1 antibody nivolumab, BMS-936558, and in vivo toxicology in non-human primates. Cancer Immunol Res. 2014 Sep;2(9):846-56.