As a kind of traditional Chinese medicine, toad is used to treat breast cancer systemically by oral administration or treat advanced breast cancer locally by external application, yet it is rarely used. Recent studies have shown that toad preparations and monomers have multi-pathway and multi-target anti-tumor properties. Their effective components can induce apoptosis of breast cancer cells, inhibit cell proliferation, and sensitize chemotherapy drugs to achieve drug resistance reversal, showing good anti-breast cancer effects. This paper reviews the anti-breast cancer effect and mechanism of toad preparations and effective monomers. Toad preparations and its effective monomers can induce apoptosis of breast cancer cells through 2 ways, and effective monomer bufalin can reduce toxicity, enhance efficacy, and reverse drug resistance in combination with chemotherapeutic drugs.