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Cancer is one of the most devastating illnesses in the world, impacting millions of individuals every year. Despite various therapies, the final effect is unsatisfactory. Chemotherapy currently dominates as the primary option of treatment. However, its severe adverse effects, limited efficacy, and resistance to drugs undermine its potential. Growing evidence suggests that ginsenoside Rg3, a natural compound obtained from the ginseng plant (Panax ginseng), holds significant promise in cancer therapy. Its proposed mechanisms primarily involve the enhancement of immunity, retardation of cancer cellular proliferation and metastasis, triggering apoptosis, angiogenesis, epigenetic modification, and Regulation of transition of epithelial mesenchyma (EMT) and miRNAs/lncRNA. Furthermore, Rg3-ginsenoside potentiates the effectiveness of conventional treatments of cancer and reduces the adverse effects through synergistic interactions. Ginsenoside Rg3's present status in cancer research is thoroughly reviewed in this article, shedding light on its intricate mechanisms and potential to revolutionize cancer therapy through combinatorial and nano-based targeted therapy., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)