Glaucocalyxin A （GLA） is a natural diterpenoid extracted from Isodon amethystoides belonging to Labiatae. Modern pharmacological research has shown that GLA has anti-inflammatory， anti-tumor， anti-fibrotic， osteoporosis-ameliorating， and cardiovascular system-protecting activities and good biosafety. However， the low content in plants， poor solubility， high metabolic rate， and low bioavailability limit the application of GLA. To address these issues， researchers have studied the total synthesis， structural modification， and nanomedicine development of GLA. By reviewing the available studies about GLA in the past five years， we summarize the research progress in the total synthesis， pharmacological activities and mechanisms， and in vivo metabolic transformation， aiming to provide a theoretical basis for clarifying the specific mechanisms underlying the pharmacological activities of GLA and for further research， development， and clinical applications of GLA.