Tislelizumab is a next-generation PD-1 monoclonal antibody developed to overcome the limitations of earlier immune checkpoint inhibitors. By eliminating Fcγ receptor binding, it avoids macrophage-mediated T-cell clearance and enhances the antitumor immune response. Unlike conventional PD-1 inhibitors, tislelizumab binds to PD-1 in a way that more closely mimics the natural PD-L1 interaction, potentially improving efficacy and reducing immune-related toxicity. This review highlights its structural advantages, clinical efficacy across multiple cancers, and recent global regulatory approvals. We also discuss key pharmacokinetic features and current challenges, including the need for predictive biomarkers, immune-related adverse events, and combination therapy strategies. Together, these insights may guide the more effective and safer use of tislelizumab in cancer immunotherapy.

Tislelizumab is a next-generation PD-1 monoclonal antibody developed to overcome the limitations of earlier immune checkpoint inhibitors. By eliminating Fcγ receptor binding, it avoids macrophage-mediated T-cell clearance and enhances the antitumor immune response. Unlike conventional PD-1 inhibitors, tislelizumab binds to PD-1 in a way that more closely mimics the natural PD-L1 interaction, potentially improving efficacy and reducing immune-related toxicity. This review highlights its structural advantages, clinical efficacy across multiple cancers, and recent global regulatory approvals. We also discuss key pharmacokinetic features and current challenges, including the need for predictive biomarkers, immune-related adverse events, and combination therapy strategies. Together, these insights may guide the more effective and safer use of tislelizumab in cancer immunotherapy.