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Oltipraz Concentrations in Plasma, Buccal Mucosa Cells,and Lipids

Pharmacological Studies¹

Departments of Medicine [N. V. D., C. M. L., E. R. T., M. N.], Food Sciences and Human Nutrition [E. S., M. B.], Epidemiology and Statistics [J. G.], and Pharmacology and Toxicology [J. L. B.], Michigan State University, East Lansing, Michigan 48824; and National Cancer Institute, Division of Cancer Prevention [J. C., E. H.] and Gastrointestinal and Other Cancers Research Group [E. H.], Bethesda, Maryland 20892

Oltipraz is considered one of the most potent cancer chemoprevention agents, as shown in preclinical studies. Its pharmacological effects in humans have been associated with unusual toxicity affecting the fingers and toes. This study was designed to test intermittent dosing schedules using two dosage levels: 500 mg as a single weekly dose and 200 mg as a biweekly dose, each for 30 days. Fifteen men and women were studied in each dosing group. All were heavy smokers considered to be at high risk for developing lung cancer. Plasma, buccal mucosa cell, and lipoprotein concentrations were measured at different intervals corresponding to the time period when most of the adverse effects occur. No serious toxicities were observed using these doses and schedules. The plasma and buccal mucosa cell concentrations of Oltipraz showed substantial interindividual variations at each sampling. Some subjects had no detectable plasma or buccal mucosal cell Oltipraz concentrations. The distribution of Oltipraz incorporation into the lipid fractions and albumin was changed by the administration of different schedules of Oltipraz. The results of this study suggest that the intermittent dosing is well tolerated and does not result in steady state in plasma or buccal mucosa cells. The variation and lack of detectable Oltipraz concentration in plasma, buccal mucosa cells, and lipids may affect both the toxicity and the pharmacological effects when these doses and schedules are used.

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