<i>Justicia gendarussa</i> Burm f., a member of Acanthaceae family, is indigenous to China and is widely dispersed throughout India, including the Andaman and Nicobar Islands. <i>J. gendarussa</i> is one of the most important plant species utilised in Ayurveda and Chinese medicine. Typically the plants are employed for different medicinal purposes. The plant possesses diverse biological activities like antiangiogenic, antibacterial, hepatoprotection, antifungal, antidepressant, sedative-hypnotic, anxiolytic, immunosuppressant, cytotoxicity, antioxidant and anthelmintic activities. Various chemical elements such as carbohydrates, alkaloids, polyphenolic chemicals, steroids, terpenoids, and saponins have been identified to contribute to these functions. The leaves were found to own most of the constituents like lupeol, friedelin, ß-sitosterol and aromatic amines. The current review emphases on Justicia gendarussa Burm's ethnobotanical significance, bioactive ingredients, and pharmacological profile.