The metabolism of zearalenone (ZEA) and analytical methods for determining the presence of ZEA and its metabolites are discussed in this study. Similar to phytoestrogens, solid metaloestrogens, pharmaceuticals, and selected pesticides, ZEA is a substance that displays endocrine activity. ZEA is accumulated in living organisms, and it is capable of contaminating all trophic levels of the food chain, from grain, maize, and other crop plants to human consumers. Zearalenone has a structure similar to that of estrogen (the presence of a macrocyclic lactone ring), it has an affinity for estrogen receptors, and it competes with 17β-estradiol for binding the estrogen receptor in natural pathways. As endocrine disruptors, zearalenone and its metabolites can also contribute to carcinogenic mutations associated with female secondary sex characteristics. The determination of zearalenone and its metabolites in various matrices, first of all biological and environmental samples, poses significant problems. A variety ways of extracting and purifying zearalenone, including liquid-liquid extraction and solid-phase extraction, are described. Furthermore, it describes the possibility of applying a plurality of sensitive and specific instrumental methods, chromatographic techniques (TLC, HPLC, GC) as well as other methods (immunoaffinity chromatography).