Abstract: Bladder cancer (BC) is a common malignant tumor of the urinary system. Common white light cystoscopy is the most important method in the diagnosis and treatment of BC, but its ability to identify small tumors and residual tumors at surgical sites is limited, so it is urgent to develop new diagnosis and treatment techniques. With the rise of the concept of precision medicine, a group of targeted molecules that can specifically bind to BC at the cellular and molecular levels have been discovered in recent years, and the molecular image and targeted therapy based on them can significantly improve the diagnosis and treatment efficiency of BC, with a great potential for clinical application. Based on the latest progress and the research work of our research group, this paper comprehensively analyzes and systematically summarizes the application of targeted molecular carriers in the diagnosis and treatment of BC.