Aromatase inhibitors (AIs) were originally developed for the treatment of advanced breast cancer in postmenopausal women. Their use in reproductive medicine has been extensively studied in the past decade. We reviewed the current strategies for ovulation induction for anovulatory women, mostly women with polycystic ovarian syndrome (PCOS), and the scientific basis for use of AIs in reproductive medicine. The AI, letrozole, is effective in ovulation induction in women with PCOS resistant to clomifene citrate and ovarian stimulation for intrauterine insemination and in vitro fertilization (IVF). Letrozole is an attractive option with its oral route of administration, cost, safety profile and effectiveness in ovulation induction and ovarian stimulation. Letrozole has the potential to be the first-line treatment option for ovulation induction in PCOS women, while its use in ovarian stimulation for IVF deserves further study.