Myrtle (Myrtus communis L., Myrtaceae) is a medicinal herb used worldwide in traditional medicine. A large number of components have been isolated from this herb. Polyphenols, myrtucommulone (MC), semimyrtucommulone (S-MC), 1,8-cineole, α-pinene, myrtenyl acetate, limonene, linalool and α-terpinolene are among the compounds considered to be the main biologically active components. Various parts of this herb such as its berries, leaves and fruits have been used extensively as a folk medicine for several centuries. The herb is used traditionally for the treatment of disorders such as diarrhea, peptic ulcer, hemorrhoid, inflammation, pulmonary and skin diseases, although clinical and experimental studies suggest that it possesses a broader spectrum of pharmacological and therapeutic effects such as antioxidative, anticancer, anti-diabetic, antiviral, antibacterial, antifungal, hepatoprotective and neuroprotective activity. The present review attempts to give an overview on the phytochemical, pharmacological, toxicological and clinical studies of total extracts and the most relevant active ingredients of M. communis.