Sesquiterpene lactones are the main component of many genera of the Asteraceae (Compositae) family. They include active compounds that are used in traditional medicine to treat a variety of ailments. Several sesquiterpene lactones, such as mipsagargin and artemisinin, are already available for sale and used to fight tumor growth, and malaria, respectively. In this article, we present data on prospective sources of new sesquiterpene lactones from species of the Asteraceae family over the past 10 years. The review contains information on the geographical distribution of genera, instrumental methods of analysis, as well as an explanation of the chemical structure and biological activity of sesquiterpene lactones isolated for the first time.