Breast cancer is considered as one of the most important health problems due to its poor prognosis and high rate of mortality and new diagnosed cases. Annually, a great number of deaths are reported in men and women; this means that despite all the improvements in cancer diagnosis and treatment, still, an intense need for more effective approaches exists. Melatonin is a multivalent compound which has a hand in several cellular and molecular processes and therefore, is an appropriate candidate for treatment of many diseases like cancer. Currently, considerable properties of this agent have oriented the research towards investigating its effects specifically in breast cancer. In this review, we gathered a bunch of evidence in order to give a new sight for breast cancer treatment utilizing melatonin. We expect that in coming years, melatonin will become one of the most common therapeutic drugs with lesser side-effects than other chemotherapeutic drugs.