Schistosomiasis still represents a major health problem in many tropical and subtropical countries despite continuing control efforts. Due to the unavailability of a vaccine that is practically applicable to humans, the use of chemotherapy is the mainstay of schistosomiasis-associated morbidity control. This paper attempts to review the antischistosomal drugs currently used in the treatment of intestinal schistosomiasis caused by Schistosoma mansoni. Their antischistosomal properties, advantages, and disadvantages as well as issues regarding the evidence for drug resistance and combination studies are reviewed in a simple manner. The recent trends towards the identification of specific chemotherapeutic targets for the treatment of schistosomes are also discussed briefly.