Summary:
Artemesia annua is a medicinal plant with a long history of use in Traditional Chinese Medicine. Artemisinin is an extract from Artemisia annua, and several semisynthetic derivatives have been developed including artesunate and dihydroartemisinin. Artemisinin and artesunate are approved for use for the treatment of malaria. Interest in the use of artemisinin and its derivatives in cancer has grown due to observed inhibitory and cytotoxic effects on cancer cells lines in vitro. Although several anti-cancer mechanisms of action have been studied, the proposed main mechanism is the intracellular iron-facilitated production of hydroxyl radicals leading to cellular oxidative stress. Oral and intravenous (IV) artesunate are the most common forms and routes used in cancer care. The structured literature search yielded two RCTs, four single-arm trials, and eight case reports evaluating artemisinin or its derivatives for cancer. Treatment was administered orally (n=10), IV (n=3), and by vaginal suppository (n=1). Most studies have used artemisinin as monotherapy, and thus little is known regarding possible interactions with cancer treatments. Although several case reports describe positive outcomes for response and survival, clinical trials have mostly focused on safety, dose, and feasibility. The only randomized controlled trial to assess survival found no difference in overall survival compared to controls in patients with lung cancer. Due to significant heterogeneity and limited research, no overarching statement can be made regarding artemisinin’s efficacy as an anticancer agent. Most studies have found artemisinin and its derivates to be safe; however, side effects including anemia, neutropenia, and gastrointestinal disturbances are common. Monitoring at baseline and throughout treatment is recommended for safety. More research is needed to assess the usefulness as artemisinin and its derivatives as a cancer treatment.