This article presents a comprehensive overview of tiger milk mushroom (TMM), covering its nutritional composition, phytochemicals, health benefits, and related scientific advancements. It describes various potential positive health benefits of TMM, including anticancer, anti-inflammatory, respiratory function enhancement, antioxidant, anti-aging, neuroprotective, photoprotective, antidiabetic, wound-healing, and anti-HIV, among others. This article also underlines the importance of further research into the phytochemicals present in TMM for additional discoveries. It underscores the importance of further research into phytochemicals content of TMM for additional discoveries and emphasizes the potential applications of TMM in nutrition, health, and well-being. Sophisticated techniques, such as chemometrics and multi-omics technologies revealed latest scientific advancements of TMM. This comprehensive overview provides a foundation for future research and development in harnessing TMM’s potential for human health.