Flutamide is a nonsteroidal antiandrogen agent. Since it was marketed in February of 1989 in the USA for treatment of prostate cancer, its potential for hepatotoxicity has been reported in Western countries. Here we report the case of a 72-year-old patient who suffered from general malaise, poor appetite, nausea and jaundice after six months of flutamide therapy for the treatment of prostate cancer. He had no past history of liver disease and was not receiving other medications. Liver biochemistries revealed elevated serum alanine aminotransferase and aspartate aminotransferase concentrations of up to 1,035 U/l and 745 U/l, respectively. Serum total bilirubin concentration was elevated to 7.0 mg/dl. Serologic markers for acute viral hepatitis were all negative. Serum antinuclear antibody, antimitochondrial antibody and antismooth-muscle antibody were also negative. Percutaneous liver biopsy revealed pericentral zonal necrosis with bridging hepatic necrosis. The patient's clinical symptoms and signs began to improve after discontinuation of flutamide, and his liver function had returned to normal three months later. Roussel Uclaf causality assessment for adverse drug reaction confirmed the diagnosis of drug-induced liver injury. This case reminds us that patients who are receiving flutamide should be regularly monitored for liver function. If drug-induced liver injury is suspected, flutamide must be discontinued promptly to avoid progression of liver injury.