Citrullus lanatus Thunb (Family: Cucurbitaceae) is a medicinal plant widely used traditionally in the treatment of various disorders in world. The phytochemical evaluation of plant showed presence of carbohydrate, alkaloids, steroids, saponins, glycoside, flavonoids, tannins and phenolic compounds. The plant also showed presence of vitamins, amino acids, proteins, minerals and fat. The plant has been extensively studied by various scientist and researchers for its pharmacological activities and therapeutic approaches such as antibacterial, antifungal, antimicrobial, antiulcer, antioxidant, anti-inflammatory, gastroprotective, analgesic, laxative, antigiardial, hepatoprotective, against prostetic hyperplasia and atherosclerosis. The present review is an effort to provide detailed information of its uses, chemical composition, pharmacological activities of extract and its isolated compounds and safety profile of Citrullus lanatus for further research.