BACKGROUND There has been a paucity of antitumor drugs that are active against renal tumors. Irinotecan hydrochloride (CPT-11), a DNA topoisomerase type 1 inhibitor, has demonstrated antitumor activity against human tumors, however, no antitumor effect of CPT-11 on renal tumors has been reported. The antitumor effect of CPT-11 was investigated on 2 human renal tumors (OUR-10 and OUR-20) heterotransplanted into nude mice. METHODS Tumor-bearing nude mice were given daily intraperitoneal injections of multiple anticancer drugs suspended in 0.2 mL of phosphate-buffered saline (PBS) 3 times at 3-day intervals. Control mice were injected with 0.2 mL of PBS. The antitumor effects were evaluated by calculating the T/C ratio (treated tumors/controls) of the tumor volume. RESULTS Among the 10 anticancer drugs tested, 50 mg/kg of CPT-11 showed an active antitumor effect on OUR-20 (T/C ratio 34). However, all drugs tested on OUR-10 failed to show antitumor activity. CONCLUSIONS Since CPT-11 was effective in 1 of 2 renal tumors examined without severe toxicity, this drug could be a candidate for chemotherapy of renal cell carcinoma.