Up to date,
schistosomiasis is still prevalent worldwide. It is estimated that more than 200 million individuals are infected, and 120 million suffer from clinical morbidity. Facing such huge cases of
schistosomiasis, only heavy reliance on a single
praziquantel for
schistosomiasis control does not adapt and may promote the selection and spread of
drug-resistant parasites. Therefore, it is an urgent need to develop the new antischistosomal
drug. In 2008-2009, the
antimalarial drug mefloquine, an arylaminoalcohol compound, has been found to be effective against schistosomes. According to the experimental studies, the deepest impression on the antischistosomal properties of
mefloquine can be summarized as following points: (1) single dose of
mefloquine possesses potential effect against three major species of schistosomes (Schistosoma mansoni, Schistosoma haematobium, and Schistosoma japonicum) infecting humans; (2) the
drug displays similar effects against developing stages of juvenile and adult schistosomes, which are superior to that of
artemisinins and
praziquantel; (3) in vitro
mefloquine exerts direct killing effect on juvenile and adult schistosomes, while in vivo, the efficacy of the
drug is independent to host immune response, (4)
mefloquine causes extensive and severe morphological, histopathological, and ultrastructural damage to adult and juvenile schistosomes, particularly, the worm tegument, musculature, gut, and vitelline glands of female worms are the key sites attacked by the
drug; (5) combined treatment with
mefloquine and
praziquantel, or
artemisinins shows synergistic effect against schistosome in
experimental therapy,while in initially clinical trial,
mefloquine in combination with
artesunate also exhibits higher cure rates against
schistosomiasis hematobia and
schistosomiasis mansoni, and (6) several
mefloquine-related arylmethanols exhibit potential effect against schistosomes in vivo, which is a useful clue helpful for development of new antischistosomal compound. In the present review, we have summarized the major results published in recent years, and the significance as well as the prospect for the future study of
mefloquine have been discussed briefly.