Recent studies have shown that mushrooms are recognized as a promising source of functional and nutraceutical compounds. The species Ganoderma lucidum (also called Reishi or Lingzhi) is a mushroom used in medicine because Chinese attributes to this fungus better health and longevity. Among the numerous bioactive compounds identified in G. lucidum are polysaccharides mostly β-glucans, heteropolysaccharides or glycoproteins, terpenoids mostly ganoderic acids and derivatives, as well as many other bioactive proteinases that contribute to health and diseases prevention. The aim of this review is to report on the profile of the most bioactive compounds, particularly polysaccharides and terpenoids of G. lucidum.