Background: Ganoderma lucidum, a double-walled basidiospore produced by porous basidiomycete fungi, has been used as a traditional medicine for thousands of years. It is considered a valuable Chinese medicine for strengthening body resistance, invigorating the spleen, and replenishing Qi. G. lucidum contains a variety of active ingredients, such as polysaccharides, triterpenoids, nucleosides, sterols, alkaloids, polypeptides, fatty acids, steroids, and inorganic elements, and has anticancer, anti-inflammatory, hepatoprotection, hypoglycemic, anti-melanogenesis, anti-aging, and skin barrier-repairing activity. Conclusions: The review summarizes the traditional usages, distribution, active constituents, structure, and biological effects of G. lucidum, with an aim to offer directions for further research and better usage of G. lucidum as a medicinal raw material.