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Influence of Mild Liver Impairment on the Pharmacokinetics and Metabolism of Bosentan, a Dual Endothelin Receptor Antagonist

From Department of Clinical Pharmacology, Actelion Pharmaceuticals, Ltd., Allschwil, Switzerland (P. L. M. van Giersbergen, F. Bodin, J. Dingemanse) and APEX Research, Munich, Germany (G. Popescu).

The purpose of the study was to investigate the effect of mild liver impairment on the pharmacokinetics and metabolism of bosentan. Eight patients with mild liver impairment and 8 matching healthy subjects were treated with single and multiple oral 125-mg doses of bosentan. The pharmacokinetic parameters of bosentan and its metabolites were similar in both groups: geometric means for C_max and AUC for bosentan were 2534 and 1980 ng/ml and 11,957 and 10,781 ng•h/ml after single doses and were 1831 and 1715 ng/ml and 7216 and 7838 ng•h/ml after multiple doses, respectively, in healthy subjects and patients. In both groups, the exposure to the metabolites was low when compared to that to bosentan. The decrease in exposure to bosentan after multiple dosing, indicative of autoinduction, tended to be less pronounced in patients as compared to healthy subjects. Bosentan was well tolerated in this study. In conclusion, the pharmacokinetics, metabolism, and tolerability of bosentan are similar in healthy subjects and patients with mild liver impairment.

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