LAUSR

Antibody‐drug conjugates represent a promising new treatment option that uses the targeting ability of an antibody to deliver cytotoxic drugs directly to tumors. Antibody‐drug conjugates provide the opportunity to deliver drugs to antigen‐expressing cancer cells while minimizing toxicity to normal tissue, achieving wider therapeutic windows. To date, three antibody‐drug conjugates have been approved by the US Food and Drug Administration, and many antibody‐drug conjugates are under clinical development for urological malignancies. In this paper, we review the mechanism, history, and development of antibody‐drug conjugates, and review the current landscape of antibody‐drug conjugates in urological malignancies including 12 targets and 18 antibody‐drug conjugates in prostate cancer, renal cancer, and urothelial cancer. Furthermore, we review the rational combination of antibody‐drug conjugates with immune checkpoint inhibitors and consider future prospects to enhance the therapeutic activity of antibody‐drug conjugates in urological malignancies.