Biophytum sensitivum (L.) DC (Family: Oxalidaceae) is a medicinal plant widely used in the treatment of various health aliments throughout the world. The plant extract showed the presence of flavonoids, saponins, tannins, terpenes, steroids, amino acids, essential oil, polysaccharides and pectin. The plant has been extensively studied by various researchers for its biological activities and therapeutic potentials such as analgesic, anti-pyretic, anti-inflammatory, immunomodulatory, antitumor, antidiabetic, antioxidant, antibacterial, antihypertensive, chemoprotective, radioprotective and antifertility. The present review is an effort to provide detailed information on folkloric uses, chemical compositions, pharmacological activities of the extracts and isolated compounds and safety profile of Biophytum sensitivum for further research studies.