The Myrtaceae family is considered one of the largest known botanical families and the genus Psidium is among the most economically interesting. Psidium genus comprises approximately 112 species, and it has been extensively studied, mainly because of Psidium guavaja species. Phytochemical investigations confirmed the presence of phenolics as the main compounds, as well as the essential oils, which were also widely investigated. Pharmacological studies report analgesic, anthelminthic, acaricidal, antihiperglicemic, among other biological activities for different species. The present review covers the relevant literature until 2019 and outlines the current data on chemical composition, preclinical and clinical studies on Psidium species, as well as the main possible mechanisms of action responsible for the described activities. Therefore, it can provide a reference for pharmaceutical research and clinical application of this genus.