Since the late 1990s, there has been rapid multiplication of data on the anti-
cancer properties of
artemisinins. This article reviews the status of progress of
artemisinin and its derivatives as anti-
cancer agents in clinical trials, case reports, and in vitro/in vivo studies. Particular attention is laid on the combinations of
artemisinins and synthetic chemodrugs to enhance the latter's efficacy. An attempt is here made to rationalize the synergistic effects of a few common anti-
cancer drugs of the
anthracycline,
taxane, anti-metabolite, and
platinum-based
drug families. The various pathways that mediate the action of
artemisinins as reported over the past decade are here summarized highlighting also the
biomarkers that could be used to better predict the efficacy of the
sesquiterpenoids. Their main action seems to be directed toward stalling
tumor cell proliferation through cell cycle arrest mediated by
reactive oxygen species (ROS). The emergence of
artemisinins' nano-based formulations in combination with chemodrugs to enhance
drug bioavailability and targeting as well as
immunotherapy is also reviewed. The enhanced efficacy of
artemisinin dimers compared to the parent molecules and standard
chemotherapy is analyzed. While these
therapies hold promises, it may be premature to conclude on their efficacy in the absence of clinical studies.