Fungal-derived bioactive compounds are emerging as key components in functional food development, offering new opportunities for health-promoting formulations. The Polyporaceae family, particularly Cerrena unicolor, has demonstrated significant potential due to its rich biochemical profile and diverse health benefits. Despite its extensive bioactive properties, its application in food science and biotechnology remains underutilized. This review explores the bioactive composition, technological potential, and functional applications of C. unicolor in innovative food systems. We analyze its antioxidant, antimicrobial, and anticancer effects, focusing on its interactions with dairy-based matrices to enhance bioavailability and therapeutic potential. C. unicolor is a valuable source of polysaccharides, phenolics, and enzymatic compounds with antioxidant and anti-inflammatory properties. Its anticancer potential, especially when incorporated into dairy fermentations, opens new avenues for oncology-focused functional foods. Strong antimicrobial activity suggests its potential as a natural biopreservative or bioactive food additive. Bioactive fractions contribute to metabolic health improvements (diabetes management) and tissue regeneration, highlighting their role in next-generation nutraceuticals. Incorporating C. unicolor into functional food systems represents a cutting-edge approach to biotechnology-driven health solutions. Further research is required to optimize its formulation, improve bioavailability, and explore regulatory pathways for market implementation.