Breast cancer [BC] is the deadliest neoplasm in women globally and the second leading cause of cancer associated deaths. Current treatment methods include chemotherapy, hormonal therapy, radiation therapy and surgery. However, BC has shown resistance to these therapies and are often associated with side effects, multidrug resistance, recurrence are the major issues in BC treatment. Currently, dietary phytocompounds have emerged as beneficial agents for the prevention and treatment of cancer because of their safe and cost effective nature. Ursolic acid [UA] is widely spread in fruits and vegetables having the ability to inhibit BC proliferation, angiogenesis and metastasis, arrest cell cycle, induced apoptosis, scavenge free radicals and regulate several anti-apoptotic and pro-apoptotic proteins. UA has also shown potential anticancer, anti-inflammatory and antioxidant activities in several human BC cells. This review paper encompasses the role of UA against BC and their mechanism of action in vitro and in vivo studies.