The worldwide human health system is threatened by the spread of numerous diseases and microbial contamination, further increased by climate change and its environmental consequences. Scientists are actively researching innovative medication sources, such as plants, animals, microorganisms, and fungi. Fungi, particularly medicinal mushrooms, are gaining popularity because of their high potential to produce different bioactive metabolites for drug discovery. Different medicinal mushrooms produce compounds that are both medicinal and beneficial to human nutrition. These metabolites can potentially treat various health issues, including antibacterial, immunomodulatory, anticancer, and anti-inflammatory properties. This chapter thoroughly examines medicinal mushrooms, their beneficial bioactive metabolites, and their applications in the treatment of human health disorders. It also discusses the mechanics and applications of these metabolites, highlighting their significance in establishing novel therapeutic techniques to enhance global health outcomes.