Breast cancer is the most common cancer in females. The treatment of this cancer is one of the challenges facing the world’s health system. Metastasis and cancer cell invasion are the reasons for the difficulty in treating this cancer. Also, the formation of new blood vessels, or angiogenesis, facilitates metastasis in cancer patients. Therefore, researchers are seeking new therapeutic drugs. One of the important factors in the processes of angiogenesis and metastasis is vascular endothelial growth factor and its receptor. Agents that can inhibit this molecule and its receptor will have helpful therapeutic potential for treating breast cancer. Apatinib is a drug that has drawn the attention of cancer researchers in the last decade, and many studies have been conducted on its effectiveness in cancer treatment, especially breast cancer. In this review article, we aimed to summarize the therapeutic potential of apatinib in vivo and animal models, with a focus on clinical trials.