Urtica dioica (stinging nettle), a flowering plant with the herbaceous perennial habit, belonging to the 'Urticaceae' family, native to temperate Asia, Europe, and North Africa, shows now worldwide distribution. The plant has a long history of being utilized as a medicinal herb. Traditionally, it is being used widely by many medical practitioners to treat many diseases like haematuria, arthritis, nephritis, menorrhagia, and rheumatism. Although this plant's phytochemistry is complex, studies on phytochemical constituents showed the occurrence of compounds like flavonoids, tannins, saponins, proteins, amino acids, and phytosterols. Likewise, Urtica dioica is being used as food, fibre, manure, and cosmetics. The plant also possesses diverse pharmacological activities, including antioxidant, antibacterial, analgesic, antiviral, anti-inflammatory, hepatoprotective, anticancer, and immune-regulatory effects. This review briefs about biological activities, phytochemistry, toxicology, and pharmacology of Urtica dioica.