In this paper, the chemical structures and pharmacological activities of diterpenoids from isodon japonica var.glaucocalyx were reviewed, and the research on modification of chemical structure and dosage form of the diterpenoids to improve the antitumor activity was also reviewed. Meanwhile, the deficiencies in the current research on diterpenoids from isodon japonica var.glaucocalyx were analyzed, and the future research direction of the development of clinical drug use of the diterpenoids from isodon japonica var.glaucocalyx was prospected. It provides a reference for the material basis research and resource development of the plant, which is safe and widely distributed in China. Meanwhile, it has accumulated data for the research and development of the diterpenoids as antitumor drugs.