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It has been shown that isoprinosine, an antiviral drug, possesses immunoregulatory properties. To complement such studies, the effects of increasing concentrations of isoprinosine on several functions of polymorphonuclear leukocytes (PMN) [chemotaxis, adhesiveness, particle ingestion, quantitative reduction of nitroblue tetrazolium dye (NBT), candidacidal activity] were investigated. At higher concentrations (greater than 10/gmg/ml) this drug produced a dose-related depressive effect, more pronounced on chemotaxis than on NBT reduction. A significant decrease of adhesiveness was observed only with the highest concentration (1000 μg/ml) of isoprinosine; the other tests were not affected. Thus, these in vitro experiments could not demonstrate any stimulatory effect of isoprinosine on normal human PMN. However, these results do not exclude the possibility of a beneficial effect of the drug on functionally altered PMN.