Researchers have unraveled the nutritive value and other beneficial effects of coffee on human health, especially prevention of lifestyle diseases of the modern world. Therefore, it is being considered as a nutraceutical to prevent and combat diseases of modern society. This chapter describes historical perspectives of green coffee bean, its source, processing, global production scenario, major phytoconstituents, pharmacokinetic attributes, major pharmacological activities, promising potential as a nutraceutical, and some of the possible adverse effects. Its promising antioxidant and weight-reducing potential, ability to check type 2 diabetes and hypertension, ability to prevent cardiovascular and other diseases like cancer and hepatic and neurodegenerative disorders, along with their possible mechanism(s) of action, strongly favor its consideration as a promising nutraceutical and food supplement. However, detailed research work following long-term exposure is warranted to assess the efficacy and safety of coffee.