Bladder cancer (Bca) is the second most common malignant tumor of the genitourinary system in Chinese male population with high potential of recurrence and progression. The overall prognosis has not been improved significantly for the past 30 years due to the lack of early theranostic technique. Currently the early theranostic technique for bladder cancer is mainly through the intravesical approach, but the clinical outcomes are poor due to the limited tumor-targeting efficiency. Therefore, the targeting peptides for bladder cancer provide possibility to advance intravesical theranostic technique. However, no systematic review has covered the wide use of the targeting peptides for intravesical theranostic techniques in bladder cancer. Herein, a summary of original researches introduces all aspects of the targeting peptides for bladder cancer, including the peptide screening, the targeting mechanism and its preclinical application.