This review provides a comprehensive overview of the botany, traditional uses, phytochemistry, pharmacology, and toxicity of the genusTripleurospermum.Tripleurospermum, a prominent genus within the family Asteraceae, is recognized for its therapeutic potential in treating various ailments, including skin, digestive, and respiratory diseases; cancer; muscular pain; and stress and as a sedative. Through extensive phytochemical studies regarding theTripleurospermumspecies, numerous chemical compounds have been identified and classified into distinct classes, predominantly encompassing terpenes, hydrocarbons, steroids, hydrocarbons, oxygenated compounds, flavonoids, tannins, alcohols, acids, melatonin, and fragrant compounds. The findings from this review highlight the presence of bioactive compounds within theTripleurospermumspecies that possess significant medicinal properties.