Elephantopus scaber Linn., family Asteraceae, is a small herb found in the Neotropics, Europe, Asia, Africa and Australia. The parts of this plant have been used traditionally for the treatment of number of diseases in many countries. The plant has been extensively screened for anticancer activity. Sesquiterpene lactones such as deoxyelephantopin, isodeoxyelephantopin, scabertopin and isoscabertopin. have been found to be prominent anticancer constituents. Many other biological activities such as antimicrobial, hepatoprotective, antioxidant, antidiabetic, anti-inflammatory, analgesic, antiasthamatic, antiplatelet and wound healing ability have been reported in various research articles. This review has been envisaged with an intention to provide the scientific information about the pharmacological and toxicological profile of E. scaber.