A comprehensive 60-year review of antischistosomal
drug discovery and development research in the People's Republic of China (P.R. China) is presented. In the 1950s, three antimonials were developed, which, compared to
potassium antimony tartrate-the treatment of choice against
schistosomiasis at the time-showed equal efficacy but lower toxicity when administered orally or intramuscularly. Activity of
furapromidum against Schistosoma japonicum was reported in the early 1960s, and this
drug became the first non-antimonial used in clinical treatment of
schistosomiasis japonica. Subsequently, two additional nitrofuran derivatives (furadiamine and
fuvinazole) were investigated in the laboratory and clinically. In the late 1960s,
niridazole and
amoscanate were developed by western scientists, which encouraged Chinese researchers to synthesise and further modify the chemical structures of these compounds. However, the modified compounds were less efficacious but similarly toxic, which impeded their further development. The advent of the safe, highly efficacious broad-spectrum antischistosomal
drug praziquantel, in the mid-1970s, eventually resulted in a change of the global
schistosomiasis control strategy from a multi-pronged transmission control approach to
drug-based morbidity control. Numerous studies were carried out in P.R. China to further the understanding of efficacy, mechanism of action and safety of
praziquantel against S. japonicum. Efforts have also been made to develop antischistosomal drugs from
Chinese traditional medicine, and research with cucurbitin (an
amino acid isolated from pumpkin seeds), among other products, showed interesting in vitro and in vivo activities against S. japonicum. In the 1990s, the
artemisinins-originally reserved for
malaria treatment-were developed as 'chemoprophylactic' agents against S. japonicum, which in turn led to a series of new developments of
artemisinins and related compounds as broad-spectrum antischistosomal and anthelminthic
therapies.