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It is widely known that mushrooms present several properties with applications in the medicinal and pharmaceutical sectors, including antimicrobial, immunomodulatory, antioxidant, hypotensive, neuroprotective, and anti-inflammatory activities. This article aims to review examples of the bioactive metabolites responsible for those activities, such as polysaccharides, phenols and polyphenols, terpenes, peptides, alkaloids, and steroids, which are produced by several relevant mushroom species. It also discusses their production through solid-state fermentation and submerged fermentation, as well as the processes of obtention of mushroom bioactive extracts and considerations on their stability aiming industrial applications. In addition, the article examines the patent landscape surrounding mushroom-derived bioactives, shedding light on the intellectual property history and innovations driving this field forward. Examples of recently deposited patents in the field are highlighted, as well as the main depositors. China and the United States are the major depositor countries in this field (52% and 35% of patents, respectively), and the principal compounds on the patents are polysaccharides and alkaloids. The article also provides insights into the current market landscape, showcasing mushroom-derived products in the pharmaceutical field available to consumers. From dietary supplements to skincare formulations, the market offerings reflect the growing interest in harnessing the health benefits of mushroom bioactives.