Avermectins can affect biological processes of multiple tumor, including tumor cell proliferation and metastasis, cell cycle arrest, induction of apoptosis and autophagy, regulation of tumor microenvironment and tumor stem cells. Avermectins can be administered alone or combined with chemotherapeutic drugs to reverse multidrug resistance. To further explore the anti-tumor mechanism of avermectins will provide reliable experimental and theoretical guidance for future clinical application.