Purpose of ReviewIn this review, the role of key terpenoids that are effective against breast cancer and their mechanism of action are discussed in detail.Recent FindingsIn 2023, breast cancer has taken the leading position among all types of cancers around the world with more than 2 million new cases and around 700,000 deaths reported in one year. In women, breast cancer is the most prevalent cancer and the leading cause of death. Currently, there are many treatments for breast cancer including surgery, chemotherapy, radiation therapy, and hormone therapy. However, each of these treatments causes a lot of side effects. In addition, the rate of recurrence of breast cancer is also high and the 5-year survival rate is less than 70%. Hence, increasing research is being conducted on the effects of natural products against breast cancer to minimize the adverse effects of treatment and improve survival rates. Terpenoids are one of the largest classes of natural compounds and have shown to have various therapeutic benefits including antioxidant properties, anti-tumor activity, anti-bacterial and anti-fungal activity, anti-malarial activity, etc. They are reported to be effective against a variety of cancers such as pancreatic, colon, lung, ovarian, and breast cancer.SummaryThis review explores the therapeutic effects and its mediated pathways of few terpenoids on breast cancer. Owing to their promising effect, they can be implemented into clinical settings in the near future.