Levo-praziquantel is the left isomer of racemic praziquantel. Animal experiments showed that it is an active component of schistosomicidal activity, while dextro-praziquantel is almost ineffective. Clinical trials in three endemic areas ofSchistosomiasis japonica indicated that the therapeutic efficacy of levo-praziquantel is superior to racemic praziquantel. Pharmacokinetic and pharmacodynamic activities of the stereoselectivity of praziquantel isomers (enantiomers) are discussed.