Background: Early treatment for infertile women with polycystic ovary syndrome (PCOS) is likely crucial and includes mainly clomiphene citrate (CC) and metformin.Objectives: To review the literature data regarding the use of CC, metformin, or both for the treatment of infertility in anovulatory patients with PCOS.Materials and Methods: Using PubMed database, all main relevant articles studying therapy naïve patients with PCOS who received CC, metformin or both were searched, reviewed and analyzed.Main Results and Conclusions: In infertile obese PCOS patients, CC is the therapy of choice for inducing ovulation. Combining CC and metformin is not more effective than CC alone. Further studies are needed to define the best first line treatment in non-obese PCOS patients. © 2013 Bentham Science.