Objective To determine the investigation progression on exemestane in the treatment of breast cancer. Methods The literatures of recent years on the studies of exemestane were reviewed. Results Exemestane is an effective steroidal aromatase inactivator with superior tolerability, safety and efficacy in the adjuvant, neo-adjuvant and metastatic therapy of breast cancer. Conclusion With the progression of clinical trial with exmestane, exemestane will be regarded as an important drug in comprehensive therapy of breast cancer.