Garlic (Allium sativum L.) is one of the greatest gifts of natural medicine and the oldest medicinal herbs that is cultivated all over the world. It is a widely used spice plant with well-known medicinal properties. Garlic is an important raw material of plant origin with observed and proven positive effects on the human body. A. sativum L. belongs to the most extensively studied medicinal herbs from genus Allium. In the past few decades, its biologically active compounds have been analyzed for their therapeutical properties. The most essential biologically active compound discovered in A. sativum is allicin, working synergistically with other phytochemicals in the prevention of many diseases. Preparation of garlic extractions can be done in liquid form and solid form. The composition and bioactivity of the extraction depend on the strain, age, method of preparation, and consumption method. When extracted and isolated, the bioactive compounds of garlic show a wide range of beneficial health effects: platelets inhibitory and antithrombic activities, hepatoprotective, antimicrobial, antihyperglycemic, antidiabetic, and antitumor. The present chapter describes botanical characterization of garlic, its chemical composition regarding bioactive compounds, and its health benefits.