Objective:To study the selective killing effects of immunotoxin BDI-1-PEA against human-bladder cancer cell line E-J and nude mice bearing human bladder tumor. Methods:MTT was used to measure the killing ratio of BDI-1-PEA, mixtures of BDI-1 and PEA, PEA against human-bladder cancer cell line E-J at different concentrations in vitro. When the tumor size reached 0.3 cm, BDI-1-PEA,BDI-1 and IgG were injected respectively to each group of mice though tail vein every other day for 6 times. Determined the inhibitory effects of BDI-1-PEA, BDI-1 and IgG in nude mice bearing human bladder tumor. Results: The results indicated that BDI-1-PEA showed stronger cytotoxicity against human bladder cancer cell line E-J than PEA and mixtures of BDI-1 and PEA, and stronger cytotoxicity against nude mice bearing human bladder tumor than BDI-1 and IgG.Compared with cytotoxicity against non-target cell,the difference was significant (P<0.01). Conclusion: Immunotoxin BDI-1-PEA is a largely potential anticancer drug, the result is a good foundation for the further clinical study.