Praziquantel: The enigmatic antiparasitic

Praziquantel (PZQ), a pyrazinoisoquinoline, was introduced as a novel anthelmintic in 1975. PZQ is currently the drug of choice for the treatment of a wide range of both veterinary and human trematode and cestode infections, including human schistosomiasis. Current estimates suggest that 150 million humans are infected with schistosomes, and it is expected that PZQ will play the lead role in chemotherapeutic control of those infections. Despite the time that has passed since its introduction and its obvious importance in global health care, it is not yet understood why PZQ is so selective and effective. The target molecules for PZQ have not been defined, nor are the sites of its effects within the parasites known. Here, Tim Day, James Bennett and Ralph Pax summarize some of the progress that has been made toward reaching these objectives in recent years.