Lexatumumab is a fully human monoclonal antibody that targets TRAILR2 (also known as DR5), a death receptor expressed on the surface of many cancer cells. Its primary application is in cancer therapy, where it induces apoptosis (programmed cell death) by activating the extrinsic apoptotic pathway. When lexatumumab binds to TRAILR2, it triggers receptor trimerization and formation of the death-inducing signaling complex (DISC), leading to caspase activation and tumor cell death.

This antibody has shown antitumor activity in preclinical studies against a range of solid tumors and hematological malignancies, including lung, colon, and prostate cancers, as well as leukemia and lymphoma. Because TRAILR2 is preferentially overexpressed in tumor cells compared to normal tissues, lexatumumab offers a targeted approach with potentially reduced off-target toxicity.

Lexatumumab has been investigated in early-phase clinical trials, often in combination with chemotherapy or other targeted agents, to enhance tumor cell killing. Its ability to synergize with conventional therapies makes it a candidate for use in multimodal cancer treatment strategies. Research continues to explore optimal dosing, patient selection, and combination regimens to maximize therapeutic benefit.