Nutraceuticals comprise special foods, supplements, or products that offer benefits beyond basic nutrition. These are also referred to as superfoods or health supplements, as they provide medicinal advantages along with regular dietary supplements. Nutraceuticals are composed of vitamins sourced naturally, plant-based compounds, and nutrient-dense foods such as fortified cereals. These also include herbal pills or even genetically modified foods engineered to provide additional health benefits. Higher vascular plants, animals, fungi, algae, and bacteria are the sources of natural nutraceuticals. This chapter focuses on fungal-derived biomolecules that can be used in the production of nutraceuticals while highlighting their impact on the consumer’s health with perceptions of their economic value. Numerous bioactive molecules found in cultured mycelia, broths, and fungal fruiting bodies are enzymes, lectins, phenolics, folates, carotenoids, tocopherols, flavonoids, glycosides, terpenoids, volatile oil, alkaloids, polysaccharides, lipids, minerals, proteins, and ascorbic and organic acids. Fungi are rich in various types of bioactive compounds with properties such as antioxidants, antibiotics, anti-cancer compounds, anti-inflammatory, anti-diabetic, cardiovascular health-promoting effects, immunomodulators, hypoglycaemics, and hypocholesterolaemic, consequently upholding significant therapeutic potential and clinical applications. This chapter deliberates on the important nutraceutical bioactive compounds of various fungi and their functions, the scope of fungal nutraceuticals in the food and medical field, the economic importance of fungal nutraceuticals, and the role of fungal elicitors in nutraceutical production. This chapter also discusses the drawbacks in nutraceutical efficacy and the future perspectives of nutraceuticals development.