This article provides a comprehensive review of aromatase inhibitors (AIs) for geriatricians, because it appears that more elderly women will be using these drugs in the near future. Computerized literature searches of Medline were conducted through May 2003. Key words/phrases included in the literature searches were aromatase inhibitors, estrogen, and breast cancer. Limits included English language, age 65 and older, and female sex. All relevant articles were selected and reviewed. AIs suppress intratumoral and plasma estrogen levels significantly. Third-generation AIs have excellent pharmacological profiles, with no significant drug interactions and better tolerability. These drugs have shown superiority compared with conventional therapies. The results of anastrozole, tamoxifen, and combination trials favors anastrozole over tamoxifen for adjuvant treatment, but further follow-up is required. AIs are approved for the treatment of advanced metastatic breast cancer (BC) in postmenopausal women whose disease has progressed during tamoxifen therapy. Recent trials have shown that the highly selective third-generation AIs are effective when used as first-line therapy in metastatic BC. Their possible use in preventive, adjuvant, and neoadjuvant settings is also being explored.