Ursolic acid (UA), a natural pentacyclic triterpenoid carboxylic acid, exhibits diverse biological activities and notable antitumor properties. Lung cancer (LC), a leading malignancy of the respiratory system, is predominantly classified into small cell LC and non‑small cell LC. The increasing incidence and mortality rates of LC have spurred considerable interest in the chemo‑preventive potential of UA. Accumulating evidence demonstrates that UA markedly inhibits LC cell proliferation and induces apoptosis. Mechanistically, UA induces cell cycle arrest at the G0/G1 phase, thereby suppressing LC cell invasion, migration and tumor growth. Furthermore, UA has shown synergistic effects when combined with other therapeutic agents, including mitotic kinase inhibitors and multifunctional nanomedicines, effectively overcoming drug resistance in LC cells. These multifaceted mechanisms collectively contribute to the chemo‑preventive efficacy of UA against LC. Consequently, UA represents a promising candidate for LC prevention and therapy. The present review comprehensively summarizes the anticancer effects and molecular mechanisms of UA in LC, offering insights to guide future research and facilitate the development of innovative therapeutic strategies.

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