Hyptis Jacq. (Lamiaceae) has been used in traditional medicine for the treatment of many diseases around the world. However, Harley and Pastore in 2012 proposed a new circumscription for this large genus, reducing its number of species, but supporting its monophyly. Hyptis and Peltodon were used as keywords, and triage of articles was performed using genus delimitation sensu Harley and Pastore. Only 29 species have some type of record in the literature for their medicinal use and chemical description, corresponding to 20% of the 148 species. Most cited biological activities were the antioxidant activity, reported for 9% of the species, and the antifungal activity reported for 5% of the species. For 11% of the species was described the essential oil composition, while non-volatile compounds were reported for only 6% of them. Terpenes, flavonoids, and caffeic acid derivatives are the most reported compounds for this genus. Only 8% of the species are reported as medicinal, with potential as antibacterial and antiparasitic, pointing to relevance of Hyptis to bioprospecting studies, especially in South America and Africa. However, there is a lack of studies regarding isolated compounds concerning their toxicology and efficacy, important information to achieve the production and the effective use of Hyptis as a herbal medicine.