Abstract: In the genus Orthosiphon (Lamiaceae), Orthosiphon aristatus, Orthosiphon pallidus, Orthosiphon thymiflorus, Orthosiphon stamineus are widely used in traditional medicine to prevent different diseases such as diabetes, kidney stone, edema, rheumatism, hepatitis, hypertensive and jaundice. A different variety of phytoconstituents has been isolated from the Orthosiphon species which include monoterpenes, diterpenes, triterpenes, saponins, organic acid and flavonoids compound. Antidiabetic, anti-inflammatory, antioxidant, hepatoprotective, analgesic and nephroprotective activities have been reported in the plant extract and phytoconstituents. Hence, the purpose of this review is to provide a comprehensive report about the Orthosiphon genus based on its toxicity in order to identify its therapeutic potential and future prospects for betterment of research.