Achyranthes aspera L., commonly known as the “prickly chaff flower”, belongs to the family “Amaranthaceae”. It is widely used in ancient medicinal practices because of its diverse therapeutic features. The plant has been employed in traditional medicine across Asia and Africa for the treatment of inflammation, diabetes, infections, and liver disorders. This chapter provides a brief description of the phytochemical composition and medicinal uses of A. aspera. Phytochemical analysis has revealed the existence of different bioactive molecules in A. aspera, including alkaloids, flavonoids, saponins, tannins, terpenoids, steroids, and phenolics. Important components found in it include achyranthine, oleanolic acid, ecdysterone, and rutin, which are identified to show antioxidant and anti-inflammatory effects. Multiple studies have been conducted on this species due to its medicinal uses. The studies have suggested that the species has potent anti-inflammatory, antidiabetic, antioxidant, antimicrobial, hepatoprotective, and anticancer properties. Some new studies have also suggested its immunomodulatory and wound healing activities. There have been many explorations done regarding its biological activity. Due to inconsistency in extraction procedures and lack of standardized formulations, its pharmaceutical significance is less explored. Further study is required to elucidate its biological mechanism and increase its efficacy. Therefore, it is evident that Achyranthes aspera is a promising medicinal plant with a lot of biomedical significance.