A humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1; programmed death-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, anti-PD-1 monoclonal antibody TSR-042 binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells. PD-1, a transmembrane protein in the Ig superfamily expressed on T cells, functions as an immune checkpoint protein that negatively regulates T-cell activation and T-cell-mediated immune responses when activated by its ligands programmed cell death receptor ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity. Check for active clinical trials using this agent.