There has been tremendous growth in field of herbal medicine as therapeutic agents. Dennettia tripetala, is known to possess ethnomedicinal properties and has been used for centuries in the Ayurvedic system of medicine for the treatments of various diseases. The present review provides detailed description on the distribution, ethno-medicinal use, phyto-constituents, and biological properties of the plant that justifies its use as a potential therapeutic agent in management of different diseases. The phyto chemical composition of Dennettia tripetala include alkaloids, tannins, saponins, flavonoids, terpenoids, steroids and cardiac glycosides while it biological activities include antioxidant, antidiabetic, antibacterial, antihypertensive, anticonvulsant, antitrypanosomal, antimalarial, anti-inflammatory and cytotoxic properties among others. In conclusion, Dennettia tripetala contains various nutritional and phytochemicals compositions that make it valuable for pharmacological purposes.