Covering: up to February 2020Antrodia camphorata is a medicinal mushroom endemic to Taiwan for the treatment of intoxication, liver injury, cancer, and inflammation. Owing to its rare occurrence and potent pharmacological activities, efforts have been devoted to identify its bioactive constituents, especially terpenoids. Since 1995, a total of 162 terpenoids including triterpenoids, meroterpenoids, sesquiterpenoids, diterpenoids, and steroids have been characterized. The ergostane-type triterpenoids (antcins) and meroterpenoids (antroquinonols) are characteristic constituents of A. camphorata. The terpenoids show anti-cancer, hepatoprotective, anti-inflammatory, anti-diabetic, and neuroprotective activities. This review summarizes the research progress on terpenoids in A. camphorata during 1995-2020, including structural diversity, resources, biosynthesis, pharmacological activities, metabolism, and toxicity. The medicinal potential of the terpenoids is also discussed.