Artesunate as an emerging anticancer modality: Insights and advances

Artesunate is an antimalarial agent widely recognized for its high efficacy, low toxicity, and favorable tolerability profile. Beyond its primary activity, artesunate has demonstrated promising anti-tumor properties with a well-established safety record. Emerging scientific evidence indicates that its anticancer effects are mediated by multiple mechanisms, including the inhibition of tumor cell proliferation, migration, invasion, and angiogenesis, induction of apoptosis and autophagy in tumor cells, modulation of the tumor microenvironment, regulation of immune responses and circumvention of drug resistance. Collectively, these findings underscore the considerable potential of artesunate as a therapeutic candidate in cancer treatment. In this review, we highlight the effects of artesunate on various types of cancer and explore its mechanisms of action, aiming to suggest potential research directions and support the expansion of its clinical use. In addition, we have compiled the latest in vitro, preclinical and clinical trials and we summarize the positive effects of its combination with other chemotherapies, especially in cases where tumors develop resistance. We also explore strategies to enhance its anticancer efficacy through novel drug delivery methods, and finally, we emphasize recent findings on pharmacology, toxicity, and the emerging issue of artesunate resistance in cancer treatment, and provide a critical perspective.