Cancer is still the leading cause of death worldwide, burdening the global medical system. Rosmarinic acid (RA) is among the first secondary metabolites discovered and it is a bioactive compound identified in plants such as Boraginaceae and Nepetoideae subfamilies of the Lamiaceae family, including Thymus masticmasti chinaythia koreana, Ocimum sanctum, and Hyptis pectinate. This updated review is to highlight the chemopreventive and chemotherapeutic effects of RA and its derivatives, thus providing valuable clues for the potential development of some complementary drugs in the treatment of cancers. Relevant information about RA's chemopreventive and chemotherapeutic effects and its derivatives were collected from electronic scientific databases, such as PubMed/Medline, Scopus, TRIP database, Web of Science, and Science Direct. The results of the studies showed numerous significant biological effects such as antiviral, antibacterial, anti-inflammatory, anti-tumour, antioxidant and antiangiogenic effects. Most of the studies on the anticancer potential with the corresponding mechanisms are still in the experimental preclinical stage and are missing evidence from clinical trials to support the research. To open new anticancer therapeutic perspectives of RA and its derivatives, future clinical studies must elucidate the molecular mechanisms and targets of action in more detail, the human toxic potential and adverse effects.