Toddalia aculeata is an important medicinal plant widely used for treatment of several diseases and disorders. Root bark of the plant is antimalarial, antiperiodic, antipyretic, tonic and carminative. Plant leaves and stem have bitter taste, minty and warming-nature and, considered antiphlogistic and analgesic in nature. Leaf essential oil is used in relieving rheumatic arthritis, sprains, contusions, intercostal neuralgia, cough, malaria, dysentery and gastralgia. The also plant shows antimicrobial, antiplasmodial, analgesic, antihyperipidemic, larvicidal, spasmolytic, anti-inflmmatory, antidiarrhetic and dynamogenic activities and is traditionally utilized for the cure of diabetes. The plant roots contain coumarins that show antiplasmodial activity while Toddalin isolated from this plant inhibits osteoclastigenesis and enhances the osteoblastigenesis. Bio-organic components of T. aculeata show anti-viral, anti-tubercular and cytotoxicity against tumor cells. Present review explains therapeutic and pharmaceutical potential of Toddalia aculeata. Moreover, this review also summarizes the traditional uses of the plant for treatment of various ailments.