Black garlic is a functional food produced from fresh garlic (Allium sativum L.) via fermentation with the whole bulbs or peeled cloves in a chamber in which temperature (60-90°C) and humidity (70-90%) are regulated for a period of time. Black garlic possesses an abundant amount of antioxidant compounds such as polyphenols, flavonoids, tetrahydro-β-carboline derivatives, and organosulfur compounds, including S-allyl-cysteine and S-allyl-mercaptocysteine, as compared with fresh garlic. Note that fermentation not only alters the nutrition components and sensory attributes but also enhances the bioactivity of black garlic. A growing body of evidences demonstrating therapeutic effects of black garlic, including anticancer, anti-obesity, immunomodulatory, hypolipidemic, antioxidant, hepatoprotective, and neuroprotective effects, have been reported in the last few decades. This book chapter provides a literature review of therapeutic effects of black garlic from fundamental to clinical studies that can be used by food and nutrition experts, researchers, and scientists to improve people's health and wellness.