Euphorbia lunulata Bunge (ELB) is a traditional Chinese medicine possessing the functions of expectoration, cough relief, asthma relief, detoxification, and itching relief. Modern pharmacological studies have showed that ELB exhibits a variety of activities, such as antitumor, antibacterial, and antioxidant activities. In particular, the anticancer activities of ELB have attracted much attention. In this review, we summarize the recent research progress on the chemical constituents and anticancer activities of ELB by searching the PubMed, Web of Science, and China National Knowledge Infrastructure databases. The results show that more than 151 components have been identified from extracts of ELB, including 73 terpenoids, 28 flavonoids, 8 phenylpropanoids, 7 steroids, 19 phenols, and 5 alkaloids. ELB has been shown to exhibit significant inhibitory effects on lung, cervical, gastric, breast, and liver cancers, and its anticancer effects are mainly manifested in the 3 aspects, including cell cycle arrest, cell apoptosis, and inhibition of the migration of cancer cells.