Allium sativum, is a perennial flowering bulb which has been consumed worldwide as a functional food and known from thousands of years for its medicinal and culinary properties. Therapeutic potential of garlic is attributed to presence of its vital phytoconstituents. In present review, a complete therapeutic profile of drug is summarized by discussing its potential benefits highlighting the bioactive constituents. Phytoconstituents of crude drugs are used as antiviral, antioxidant, anti-inflammatory, antibacterial, antifungal, immunomodulatory, cardioprotective, anticancer, hepatoprotective, anti-diabetic, anti-obesity, neuroprotective, etc. Thus, it could conclude that garlic is one of the superior natural sources of bioactive compounds and has promising applications in the development of functional foods and nutraceuticals to improve health, and to prevent chronic diseases in the human.