Recent process in the development of TIM-3 antibodies and small-molecule inhibitors for cancer immunotherapy.

T-cell immunoglobulin and mucin domain 3 (TIM-3) is an immune checkpoint receptor that negatively regulates immune responses and represents a promising therapeutic target for cancer. The development of TIM-3 inhibitors has attracted widespread research interests. In this review, we comprehensively analyze the advancements of TIM-3 inhibitors, including monoclonal antibodies and small-molecule drugs. Specifically, the clinical progress of monoclonal antibodies is discussed, while the preclinical development of small-molecule inhibitors is detailed, focusing on lead compound discovery, structural optimization and biological activities. Moreover, we discuss the potential opportunities and challenges for developing TIM-3 inhibitors. It is hoped that this review will contribute to the development of TIM-3 inhibitors.