Monoclonal antibody-drug conjugate was applied in a clinical trial for patients with bladder cancer. Monoclonal antibody HB7A from a mouse splenocyte immunized against human bladder cancer was used as a drug carrier. The anti-cancer drug adriamycin (ADR) was bound to HB7A through a dextran (DEX) bridge to form the conjugate HB7A-DEX-ADR. The in vitro cytotoxic effect of the conjugate on BIU-87 bladder cancer cells was similar to that of free ADR and the mixture of HB7A and ADR. Seven patients with bladder cancer were given HB7A-DEX-ADR intravenously. The immunoperoxidase studies of the resected specimens showed that HB7A was localized specifically in cancer, and histological studies revealed degenerative and necrotic changes of the tumor cells. Patients receiving the conjugate did not experience serious side effects. This study suggests that immunotargeting chemotherapy with HB7A-DEX-ADR is well tolerated by patients and its cytotoxicity on tumor is substantial.