Breast cancer is one of the most common causes of the death among women worldwide. Metabolic disorders, alcohol consumption, hormone replacement therapy, genetic susceptibility and not having children are well known risk factors for breast cancer. Surgical resection, radiation therapy, and chemotherapy are among the limited treatment options for breast cancer. Thus, there is growing need to find new chemopreventive agents that may be effective in prevention and/or management of breast cancer. Natural products such as flavonoids provide a variety of anticancer compounds which can be useful for prevention or treatment of breast cancer. The usefulness of dietary phytochemicals in the prevention of this disease is supported by a plethora of experimental and epidemiological studies. Apigenin, a well-known flavone, is found in several dietary plant foods such as parsley, celery, thyme, celeriac, chamomile, onions, lemon balm, and oranges. Extensive studies have shown that apigenin have potent antioxidant, anti-inflammatory, and anticarcinogenic properties. The aim of the present communication is to establish the therapeutic potential of apigenin against breast cancer through critical analysis of data from 5 in vitro and in vivo studies. We also review the molecular mechanisms underlying the anticancer effects, natural sources, bioavailability, as well as the chemistry of apigenin.