Zearalenone (ZEN) is a well-known mycotoxin present in numerous agricultural products. Humans and animals are therefore at a risk of exposure to zearalenone through consumption of contaminated food. After intake, ZEN is reduced to α- and β-zearalenol (α-ZEL and β-ZEL), zearalanone (ZAN), and α- and β-zearalanol (α-ZAL and β-ZAL). Zearalenone and its metabolites, including Alpha-zearalenol are full agonists for hERα and possess hAR-mediated antagonistic activity in PALM cells. Zearalenone and its derivatives have been shown to be carcinogenic, immunotoxic, and hepatonephrotoxic.