Agrimonia eupatoria L. is an herb of the Rosaceae family, widely used in traditional (folk) medicine for its beneficial effects. Its water extracts (infusions and decoctions) are used in the treatment of airway and urinary system diseases, digestive tract diseases, and chronic wounds. Phytochemical analyses of Agrimonia eupatoria L. identified a variety of bioactive compounds including tannins, flavonoids, phenolic acids, triterpenoids and volatile oils possessing antioxidant, immunomodulatory and antimicrobial activities. The authors review the available literature sources examining and discussing the therapeutic and pharmacological effects of Agrimonia eupatoria L. at the molecular level in vitro and in vivo.