The antiestrogen tamoxifen was originally introduced as a therapy for advanced breast cancer. Today, tamoxifen is used to treat selected patients with all stages of breast cancer, and trials are underway to evaluate its effectiveness as a potential breast cancer preventive. When tamoxifen is used as an adjuvant or preventive, extended patient survival times can be expected, and concerns about iatrogenic complications arising from long-term treatment become important. This review discusses currently available laboratory and clinical data regarding the toxicology of tamoxifen and focuses in particular on the gynecologic complications potentially associated with long-term tamoxifen administration.