Introduction. – Artesunate and other artemisinin derivatives are used in various infectious and non-infectious diseases. We aimed to analyze available data on artesunate and artemisinin derivatives activity in humans and their potential clinical benefits in non-malarial indications. Material and methods. – Literature review performed on PubMed and the Cochrane Library databases using the PRISMA method. We analyzed studies published in English from January 2008 to August 2017 using the same indicators of drug efficacy. Results. – We included 19 studies performed in humans (1 meta-analysis, 1 literature review, 4 randomized controlled trials, 3 prospective controlled trials, 3 prospective uncontrolled trials, 2 exploratory phase 1 or 2 trials, 1 case series, and 4 case reports). Artesunate and artemisinin derivatives demonstrated efficacy in the treatment of schistosomiasis in combination with praziquantel (P = 0.003). Artesunate monotherapy was less effective than praziquantel alone (P < 0.001) probably because its activity only affects the early stages of Schistosoma parasites. Artesunate monotherapy could be interesting as a chemoprophylactic drug against schistosomiasis (P < 0.001). Findings seem promising but are still controversial in the treatment of multidrug-resistant CMV infections. Studies do not conclude on artesunate and artemisinin derivatives efficacy in the treatment of cervix, breast, colorectal, and lung cancers. Conclusion. – Artesunate and artemisinin derivatives in combination with praziquantel were effective against schistosomiasis, and could be used as a chemoprophylactic drug alone. They could be interesting as anti-CMV and anti-tumor treatment. Additional trials in humans are required to assess the efficacy of artesunate and artemisinin derivatives in diseases other than malaria.