Nature is an amazing source for food, shelter, clothing and medicine. An impressive number of modern drugs are isolated from many sources like plants, animals and microbes. The development of natural products from traditional medicines is of great importance to society. Modern concepts and methodologies with abundant clinical studies, unique diversity of chemical structures and biological activities aid the modern drug discovery process. Kedrostis foetidissima (Jacq.) Cogn., a traditional medicinal plant of the Cucurbitaceae family, is found in India, Sri Lanka, Ethiopia and Western Malaysia. Almost all parts of the plant are used in traditional systems of medicines and reported having medicinal properties in both in vitro and in vivo studies. In the last few years, extensive research work had been carried out using extracts and isolated phytoconstituents from Kedrostis foetidissima to confirm its pharmacology and biological activities. Many scientific reports show that crude extracts and extensive numbers of phytochemical constituents isolated from Kedrostis foetidissima have activities like antimicrobial, antioxidant, anticancer, gastroprotective, anti-inflammatory and various other important medicinal properties. The therapeutic properties of the plants are mainly attributed to the existence of phytoconstituents like phenols, alkaloids, flavonoids, tannins, terpenoids and steroids. This comprehensive review in various aspects gave a brief overview of phytoconstituents, nutritional values and medicinal property of the plant and might attract the researchers to explore its medicinal activity by discovering novel biologically active compounds that can serve as a lead compound in pharmaceutical and food industry.