Ganoderma lucidum (Lingzhi or Reishi) is known as a bitter mushroom with remarkable health benefits. The active constituents found in mushrooms include polysaccharides, dietary fibers, oligosaccharides, triterpenoids, peptides and proteins, alcohols and phenols, mineral elements (such as zinc, copper, iodine, selenium, and iron), vitamins, and amino acids. The bioactive components found in the G. lucidum mushroom have numerous health properties to treat diseased conditions such as hepatopathy, chronic hepatitis, nephritis, hypertension, hyperlipemia, arthritis, neurasthenia, insomnia, bronchitis, asthma, gastric ulcers, atherosclerosis, leukopenia, diabetes, anorexia, and cancer. In spite of the voluminous literature available, G. lucidum is used mostly as an immune enhancer and a health supplement, not therapeutically. This review discusses the therapeutic potential of G. luidum to attract the scientific community to consider its therapeutic application where it can be worth pursuing.