With just one drug used for individual patient management and community-based morbidity control, the treatment, control, and eventual elimination of schistosomiasis is vulnerable should resistance to praziquantel emerge and spread. The discovery and development of novel chemical entities that exhibit antischistosomal properties, and the repurposing of existing drugs for schistosomiasis is thus of central importance as long as praziquantel remains effective. Here, we discuss the public health relevance of schistosomiasis, which is currently considered a neglected tropical disease. We recapitulate the past and current drug armamentarium against schistosomiasis, including shortcomings and a target product profile of an antischistosomal drug. The central piece of our review is the discovery of the antischistosomal properties of various antimalarial drugs, notably the artemisinins, synthetic trioxolanes, and mefloquine. We summarize findings from preclinical investigations and experiences made thus far from clinical studies. We conclude that a closer collaboration between the malaria and schistosomiasis communities might facilitate the discovery and development of novel antischistosomal drugs, and will foster monitoring and evaluation of the ancillary benefits of antimalarial prophylaxis and treatment against schistosomiasis.