Macrofungi production and economic value have been increasing globally. The demand for macrofungi has expanded rapidly owing to their popularity among consumers, pleasant taste, and unique flavors. The presence of high quality proteins, polysaccharides, unsaturated fatty acids, minerals, triterpene sterols, and secondary metabolites makes macrofungi an important commodity. Macrofungi are well known for their ability to protect from or cure various health problems, such as immunodeficiency, cancer, inflammation, hypertension, hyperlipidemia, hypercholesterolemia, and obesity. Many studies have demonstrated their medicinal properties, supported by both in vivo and in vitro experimental studies, as well as clinical trials. Numerous bioactive compounds isolated from mushrooms, such as polysaccharides, proteins, fats, phenolic compounds, and vitamins, possess strong bioactivities. Consequently, they can be considered as an important source of nutraceuticals. Numerous edible mushrooms have been studied for their bioactivities, but only a few species have made it to the market. Many species remain to be explored. The converging trends and popularity of eastern herbal medicines, natural/organic food product preference, gut-healthy products, and positive outlook towards sports nutrition are supporting the growth in the medicinal mushroom market. The consumption of medicinal mushrooms as functional food or dietary supplement is expected to markedly increase in the future. The global medicinal mushroom market size is projected to increase by USD 13.88 billion from 2018 to 2022. The global market values of promising bioactive compounds, such as lentinan and lovastatin, are also expected to rise. With such a market growth, mushroom nutraceuticals hold to be very promising in the years to come.