Ecuador owns many high quantity and wealthy ecosystems that contain an elevated biodiversity in flora and fauna. The use of native medicinal plants has been maintained by at least 18 different indigenous cultures; furthermore, this country has been the witness of the discovery of important medicinal plants, such as Cinchona, and is an understudied resource of new natural products. The objective of this review is to update the ethnopharmacological and phytochemical studies accomplished on the Ecuadorian flora, pointing to the 253 native families and more than 15,000 species registered at present.