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Artenibenzoate is a new schistosomacide. This paper reports the pharmacokinetics of artenibenzoate in rats after oral administration. The concentrations in biological samples were detected by spectrophotometry. The concentration-time curve of the drug in plasma showed a double-peak after 150, 300 and 600 mg.kg-1 ig. Artenibenzoate absorption was fast and peak plasma level was found 1 h after administration. Then, the drug level declined to the lowest in 8 h. A second absorption peak appeared in 12 h. Two hours after oral administration to normal rats, the highest level of artenibenzoate was present in the stomach wall, while appreciable level was found in testicle, liver, spleen, heart, kidney and lung. Artenibenzoate in fat and intestine was lower, almost no drug was detected in brain and muscle. Six hours after oral administration, the drug concentration in various tissues decreased rapidly, but that in testicle, heart, kidney and fat decreased slowly. Urinary excretion was an important route of excretion. Artenibenzoate excreted in urine was about 45.6% of the administered dosage and that in feces 24.8% within a 48 hours period. The excreted amount in bile was 0.54% within 36 hours. Plasma protein binding of artenibenzoate was about 70%. Major unchanged artenibenzoate was detected in the extract from plasma, major reduced-arteannuin from feces, and both unchanged artenibenzoate and reduced-arteannuin from urine after oral administration in rats.