Recently, many patients have been treated with aromatase inhibitors(AI), either in an adjuvant setting or as a treatment for recurrence. The efficacy and safety of high-dose toremifene(HD-TOR)were evaluated in 18 patients with advanced/recurrent breast cancer. Twelve of the 18 patients had received AI just prior to the study treatment. The clinical benefit rate was 56%(PR: 28%, long SD: 28%). Progression-free median survival was 5. 5 months. Adverse events were mild and toremifene was well-tolerated. The results suggest that HD-TOR should be considered early on as a second-line treatment, or as a later treatment option for AI-resistant breast cancer.