Objective: To review the subject of polycystic ovary syndrome and the therapeutic use of insulin-sensitizing agents in patients with this endocrinopathy. Methods: We present background information on this disorder and summarize the pertinent published literature. Results: Polycystic ovary syndrome affects approximately 7.5% of reproductive-age women in the United States. Although specific diagnostic criteria for this condition have not been established, the presence of three major factors-chronic anovulation, hyperandrogenemia, and clinical signs of hyperandrogenism-has been proposed as essential for consideration of the diagnosis. A high ratio of serum luteinizing hormone to follicle-stimulating hormone is found in 60 to 75% of women with this syndrome. Treatment with metformin may yield heterogeneous responses in differing populations with polycystic ovary syndrome, but most studies have shown evidence of restoration of ovulatory cycling. In addition, weight loss and decreases in free and total testosterone levels have been reported. Troglitazone therapy proved somewhat less efficacious than metformin for restoring menstrual cycles and similar to metformin in producing hormonal responses. Because troglitazone is no longer available for clinical use, studies will need to be extended to other thiazolidinediones. Patients treated with another insulin sensitizer, D-chiro-inositol, have demonstrated improved insulin sensitivity, ovulatory rates, and biochemical findings. Conclusion: Current evidence suggests that the use of insulin-sensitizing agents in patients with polycystic ovary syndrome not only improves their sensitivity to the effects of insulin on glucose and lipid metabolism but also ameliorates clinical and biochemical manifestations of hyperandrogenism and increases rates of ovulation. Multicenter studies with larger numbers of patients are needed.