Purpose of review <p>The objective of this review is to provide an overview of the clinical progress, administration methods, efficacy, safety, and treatment-related adverse events associated with antibody–drug conjugates.</p> Recent findings <p>Locally advanced or metastatic urothelial carcinoma is an aggressive and lethal malignancy. Cisplatin-based chemotherapy has been the first-line therapy for most patients over the past two decades. However, approximately 50% of patients with locally advanced or metastatic urothelial carcinoma are ineligible for cisplatin-based chemotherapy due to inadequate renal function, poor performance status, or complications. Furthermore, patients who exhibit suboptimal responses or disease progression following platinum-based chemotherapy face therapeutic uncertainty regarding the selection of alternative agents. The emergence of antibody–drug conjugates has provided new options for patients afflicted with this disease, particularly enfortumab vedotin combined with pembrolizumab as a new first-line therapy for advanced urothelial carcinoma or for patients ineligible for platinum-based therapy. Additionally, in the TROPICS-04 trial, sacituzumab govitecan failed to demonstrate significant improvement in overall survival or progression-free survival compared with the physician’s choice of treatment for patients with advanced urothelial carcinoma progressing after platinum-based chemotherapy and PD-(L)1 inhibitor therapy; the FDA withdrew its approval for this indication. ADCs are also being considered for the treatment of muscle-invasive bladder cancer, with ongoing clinical trials.</p>