The growing public awareness of health care substantiates the importance of nutraceuticals and their health beneficial properties. Little millet (Panicum sumatrense), a minor cereal, is known for several health benefits due to the presence of bioactive nutraceuticals such as phenolic compounds, gamma-aminobutyric acid (GABA), carotenoids, and tocopherols. In this chapter, the literature on the nutraceuticals of the little millet and also the influence of processing on their stability has been reviewed. During the milling process, the physical separation of different morphological parts takes place and this has the greatest impact on the nutrient and nutraceutical content of the millet. Processing of little millet enhances its phenolic content and antioxidant properties. Soaking and germination increases its GABA content significantly. These nutraceuticals may offer protection to the consumer against diseases. This information will be useful for utilization of processed little millet as an ingredient in functional foods with health promoting functions.