India is perhaps the most unique country in the world, with the richest tradition of indigenous and health care medical practices. Most of these practices are unique and known to very few individuals or communities. Leonotis nepetifolia Family (Lamiaceae) commonly known as ‘Klip dagga’ which has a long history of several traditional medicinal uses in many countries in the world. A huge number of phytoconstituents have been reported from the plant are allenic acid, iridoids, glycosides, terpenoids, and many more. This plant exhibited various biological activities and has been attributed to a variety of physiological effects like antifungal, antidiabetic, anxiolytic, arthritic, and many more activities. This literature review presents important species covering phytochemistry and pharmacological activities aspects systematically.