Ezabenlimab is a monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death protein 1 (PD-1; PDCD1), with immune checkpoint inhibitory and antineoplastic activities. Upon administration, ezabenlimab selectively binds to and blocks the activation of PD-1, an immunoglobulin (Ig) superfamily transmembrane protein, by its ligands programmed cell death ligand 1 (PD-L1), which is overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on antigen-presenting cells (APCs). This results in the activation of T-cells and T-cell-mediated immune responses against tumor cells. Activated PD-1 negatively regulates T-cell activation and plays a key role in in tumor evasion from host immunity.
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo[1].