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<i>Antrodia cinnamomea</i> is a precious and popular edible and medicinal mushroom. It has attracted increasing attention due to its various and excellent bioactivities, such as hepatoprotection, hypoglycemic, antioxidant, antitumor, anticancer, anti-inflammatory, immunomodulation, and gut microbiota regulation properties. To elucidate its bioactivities and develop novel functional foods or medicines, numerous studies have focused on the isolation and identification of the bioactive compounds of <i>A. cinnamomea</i>. In this review, the recent advances in bioactivity, isolation, purification, and identification methods of active compounds from <i>A. cinnamomea</i> were summarized. The present work is beneficial to the further isolation and discovery of new active compounds from <i>A. cinnamomea</i>.