<p>The treatment of malignant tumors is plagued by intricate challenges of pathogenesis and drug resistance, which continuously drive the scientific community to explore novel therapeutic strategies. Natural products, with their inherent chemical diversity and multi-targeted effects, have emerged as a crucial direction in anticancer research. <i>Commiphora myrrha</i>, commonly referred to as myrrh, is a traditional medicinal resin with a long-standing history in therapeutic use, and its preclinical anticancer properties have gradually garnered increasing attention. Studies have identified that the primary bioactive constituents of myrrh include sesquiterpenes, triterpenoid compounds, steroids, and phenolic derivatives. These bioactive components exert their antitumor effects through multiple mechanisms, such as inhibiting cancer cell proliferation, regulating the cell cycle, inducing apoptosis, and remodeling the tumor microenvironment. However, current research on myrrh’s anticancer effects still faces challenges, including the complexity of its constituents, unclear mechanisms of action, and insufficient validation of its efficacy in physiologically relevant models. Future research is expected to overcome these obstacles through multi-omics integration and the design of targeted delivery systems. This review aims to summarize the research progress on myrrh and its active components in the field of anticancer therapy, with a focus on their potential mechanisms of action and the key knowledge gaps that remain to be addressed.</p>