Fomitopsis pinicola is a well-known medicinal mushroom commonly used in Chinese traditional medicine and Korean folk medicine for many years, and it is believed as a non-toxic medicinal mushroom that has many clinical effects on the human body with no sub-acute toxic impacts. In recent years, the use of medicinal mushrooms is enhanced greatly. Several different principal chemical constituents are present in the fruiting bodies of F.pinicola. These principal compounds were extracted from fruiting bodies of F.pinicola, have medicinal qualities and give different pharmacological impacts in the human body. The motive of the current review paper was to intricate the principal chemical constituents that are extracted from F.pinicola fruiting bodies and demonstrate the pharmacological effects of these extracts. F.pinicola extracts have no toxic side effects on vital organs such as liver, kidney, heart, spleen, pancreas, lungs and brain. The present study describes that both low molecular weight and high molecular weight compounds that are present in the fruiting bodies of F.pinicola. This included many useful enzymes, steroids, triterpenes and triterpenes derivatives, anti-tumor active constituents, and health beneficial nutritious compounds. These principal compounds showed important medicinal effects on the human body by providing a shield effect to the internal organs against diseases and also heal the damaged tissues and organs. The pharmacological effects of F.pinicola active constituents include anti-tumor, anti-diabetic, antihyperlipidemic by controlling obesity, anti-oxidant effect, anti-microbial, anti-inflammatory and also showed an industrial waste treatment effect.