Eleven healthy volunteers (six men, five women) and twelve cancer patients (six men, six women) were given single oral doses (2.5 mg/kg body weight) of levarnisole, an immunostimulant agent. In a second experiment eleven healthy et volunteers (six men, five women) and twelve cancer patients (six men, six women) were given single oral doses (5 rug/kg body weight) of levamisole. The levamisole concentrations in plasma (24 h blood sampling) were measured by gas chromatography after extraction. A mono-compartment open model was proposed, and some parameters were calculated. The main results from these two experiments are: the drug was absorbed well, the peak levels of levamisole in the plasma were reached after 1.0 -2.0 hrs and ranged between 0,8 l!g and 1.6 ug/ml with the 2.5 mg and 5 mg/kg body weight doses respectively (concentrations required in vitro to produce an immunological effect); the plasma half-life of levamisole calculated from the decline in the concentration curves varied between 3.3 hand 5.1 h; the absorbed fractions were 0.7 and clearance 310 ml/min; twenty-four hours after medication, the levamisole concentrations in plasma were only 6 % of the peak levels.The interindividual variability in the parameters seemed to be very important; and it may be concluded that the immunostimulant effect critically depends on the dose of the drug. A minimum effective plasma concentration is necessary to trigger its effects, on the other hand high concentrations may produce an immunosuppressive effect.

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Intratumoral platinum concentrations were measured in three tumor sites (head and neck, uterine cervix, and breast) 48 h after cisplatin administration according to the same protocol. The platinum levels were in the same order of magnitude in all tumors, but the concentration in breast tumors was found to be higher than that in tumors of the head and neck and of the uterine cervix.

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