Beauvericin (BEA) is a cyclic hexadepsipeptide, which derives from Cordyceps cicadae. It
is also produced by Fusarium species, which are parasitic to maize, wheat, rice and other important
commodities. BEA increases ion permeability in biological membranes by forming a complex with essential
cations, which may affect ionic homeostasis. Its ion-complexing capability allows BEA to
transport alkaline earth metal and alkali metal ions across cell membranes. Importantly, increasing
lines of evidence show that BEA has an anticancer effect and can be potentially used in cancer therapeutics.
Normally, BEA performs the anticancer effect due to the induced cancer cell apoptosis via a
reactive oxygen species-dependent pathway. Moreover, BEA increases the intracellular Ca2+ levels and
subsequently regulates the activity of a series of signalling pathways including MAPK, JAK/STAT,
and NF-κB, and finally causes cancer cell apoptosis. In vivo studies further show that BEA reduces
tumour volumes and weights. BEA especially targets differentiated and invasive cancer types. Currently,
the anticancer activity of BEA is a hot topic; however, there is no review article to discuss the
anticancer activity of BEA. Therefore, in this review, we have mainly summarized the anticancer activity
of BEA and thoroughly discussed its underlying mechanisms. In addition, the human exposure
risk assessment of BEA is also discussed. We hope that this review will provide further information for
understanding the anticancer mechanisms of BEA.