Tigatuzumab is a humanized monoclonal antibody designed to target TRAILR2 (also known as DR5), a death receptor that triggers apoptosis when activated. Its primary application lies in cancer therapy, particularly in inducing programmed cell death in tumor cells. By binding selectively to TRAILR2 on the surface of cancer cells, tigatuzumab activates the extrinsic apoptotic pathway, leading to tumor cell destruction with minimal impact on normal healthy cells. It has been investigated in clinical trials for various solid tumors, including ovarian, breast, colorectal, and pancreatic cancers. Tigatuzumab is often studied in combination with chemotherapy agents or other targeted therapies to enhance antitumor activity. Its mechanism offers a promising approach for overcoming resistance to conventional treatments, especially in tumors that overexpress TRAILR2. Additionally, its humanized structure reduces immunogenicity, supporting its use in long-term therapeutic regimens.