Drozitumab is a fully human monoclonal antibody that targets TRAILR2 (also known as DR5), a death receptor involved in the extrinsic pathway of apoptosis. Its primary application lies in cancer therapy, particularly in inducing programmed cell death in tumor cells. By binding to TRAILR2, drozitumab activates caspase signaling cascades, leading to selective apoptosis in cancer cells that overexpress this receptor, while sparing most normal cells.

It has been investigated in clinical trials for various solid tumors and hematologic malignancies, including non-small cell lung cancer, colorectal cancer, lymphoma, and pancreatic cancer. Drozitumab is often studied in combination with other chemotherapeutic agents or targeted therapies to enhance its pro-apoptotic effects and overcome resistance mechanisms in tumor cells.

Due to its mechanism of action, drozitumab represents a promising approach in targeted cancer treatment, especially for tumors resistant to conventional therapies. However, clinical development was discontinued following phase II trials due to challenges related to efficacy and patient selection, prompting research into biomarkers that predict response. It is now primarily utilized as a reference antibody in preclinical and research settings.