Urothelial carcinoma (UC) refers to the malignancies originating from transitional epithelium located on the upper and lower urinary tract. Precise diagnosis of UC is crucial since it dictates the treatment efficacy and prognosis of UC patients. Conventional diagnostic approaches of UC mainly fall into four types, including liquid biopsy, imaging examination, endoscopic examination, and histopathological assessment, among others, each of them has contributed to a more accurate diagnosis of the condition. Therapeutically, UC is primarily managed through surgical intervention. In recent years, minimally invasive surgery (MIS) has been incrementally used and is showing superiority in terms of lowered perioperative morbidity and quicker recovery with similar oncological outcomes achieved. For advanced UC (aUC), medical therapy is dominant. While platinum-based chemotherapies are the standard first-line option for aUC, some novel treatment alternatives have recently been introduced, such as immune checkpoint inhibitors (ICIs), targeted therapies, and antibody-drug conjugates (ADCs). ADCs, a group of sophisticated biopharmaceutical agents consisting of monoclonal antibodies, cytotoxic payload, and linker, have been increasingly drawing the attention of clinicians. In this review, we synthesize the recent developments in the precise diagnosis of UC and provide an overview of the treatment options available, including MIS for UC and emerging medications, especially ADCs of aUC.