Abstract Prostate cancer (PCa) is the most common cancer and a leading cause of cancer-related deaths among men globally, including in Singapore. The incidence of PCa has been increasing worldwide due to lifestyle changes, though there is a significant disparity in the incidence-to-mortality ratio between developed and developing countries, largely because of the advanced theragnostic approaches utilized in developed regions. While conventional treatments are effective for localized and metastatic PCa, treatment outcomes for metastatic castration-resistant prostate cancer (mCRPC), a more aggressive form of the disease, remain poor with current therapies failing to significantly extend survival. Hence, in the current study we investigated the potential role of artesunate (ART), a semisynthetic derivative of the malaria drug artemisinin in PCa cell lines. Interestingly, the ART found to inhibit the cell growth, invasion, migration, stemness and trigger the expression of apoptosis and autophagy-related proteins in PCa cell lines. In particular, ART inhibited the expression of Wnt/β-catenin pathway proteins responsible for the progression of prostate cancer to mCRPC. Moreover, inhibiting the ART induced autophagy resulted in the survival of the PCa cells to a greater extent. Furthermore, the ART treatment in a preclinical model of prostate cancer exhibited a significant reduction of prostate tumor growth along with the inhibition of lung and liver metastasis. Overall, our findings suggest that ART may activate a powerful antitumor mechanism, offering a new therapeutic approach for treating mCRPC. Citation Format: Chandra Sekhar Bhol, Muthu Kumaraswamy Shanmugam, Grace Chew, Goh Si Rui Eva, Sujit Kumar Bhutia, Gautam Sethi. Harnessing Antineoplastic Properties of Artesunate for Prostate Cancer Therapy abstract. In: Proceedings of Frontiers in Cancer Science 2024; 2024 Nov 13-15; Singapore. Philadelphia (PA): AACR; Cancer Res 2025;85 (15Suppl): Abstract nr P47.
Bhol et al. (Fri,) studied this question.