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.