Androgens are effective therapeutic agents in postmenopausal women with metastatic breast cancer. Early studies with testosterone propionate showed objective regression rates of slightly more than 20%. Subsequent work with synthetic androgens has failed to show a significant reduction in toxicity or an increase in therapeutic efficacy over testosterone propionate. Calusterone (7β,17α-dimethyltestosterone), in early clinical trials, showed both of these qualities and was believed by some to be the “ideal androgen.” As with many new drugs, subsequent work failed to confirm these early findings, and most of the later data gathered on calusterone are inconsistent. We conclude from our knowledge at present that calusterone offers no real advantages or disadvantages over other androgens in the treatment of breast cancer.