Artemisinin and six of its derivatives were evaluated for their in vitro gametocytocidal and erythrocytic schizontocidal properties on an Indian isolate of Plasmodium falciparum. One of the metabolic derivatives, DADF-dihydroartemisinin (NIH02), was found to possess gametocytocidal and erythrocytic schizontocidal properties similar to those of artemisinin. Gametocytes of this isolate were highly susceptible to the toxic effect of NIH02 (IC₅₀=6.6 ng/ml) and younger stages were more sensitive. This is the first report about the in vitro gametocytocidal properties of a derivative of artemisinin.