Ganoderic acids (GAs) isolated from Ganoderma lucidum, which have shown remarkable pharmacological activities and a variety of therapeutic effects on a number of human diseases, have provided an important resource for the development of new medicines. The yield of GAs in field cultivation is still limited, which is mainly due to a scarcity of information regarding its biosynthesis pathway and its regulation. Here, we review the recent publication that has been made in the biosynthesis and regulation of GAs. From these studies, researchers have identified part of the biosynthesis pathway of GAs named mevalonate pathway. They have cloned and characterized the genes involved in the biosynthesis pathway. Additionally, they found that expression of the genes involved in GA biosynthesis is closely related to the impact of environmental factors through transcriptional profiling analysis. Moreover, this review focuses on suggesting new directions for studying GAs and attempts to gain some insights for better understanding of the biosynthesis and regulation of GAs.