Today schistosomiasis, caused mainly by the three major schistosome species (S.
mansoni, S. haematobium and S. japonicum), has for many decades and still continues to be on a
rapid and swift rise globally, claiming thousands of lives every year and leaving 800 million people
at the risk of infection. Due to the high prevalence of this disease and the steady increase in the
infection rates, praziquantel (PZQ) remains the only effective drug against this acute disease although
it has no effect on the juvenile schistosome parasite. However, no significant approaches
have been made in recent years in the discovery of new or alternative drugs and unfortunately, resistance
to this drug has been reported in some parts of the world. Therefore, it is imperative to
develop a new drug for this debilitating disease. In this review, a brief history of past, present, and
new promising anti-schistosomal drugs is presented.