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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptor.

Recent clinical studies have shown that bosentan, a dual endothelin receptor antagonist, decreases the exposure to various substrates of cytochrome P450 ( CYP) isoenzymes 2C9 and 3A4. The aim of the study was to investigate the effect of bosentan, its metabolites and glibenclamide on the activity of the pregnane X receptor, a nuclear receptor that regulates the transcription of CYP3A4. CV-1 monkey kidney cells were transiently transfected with a luciferase reporter plasmid containing three copies of the ER6 response element of CYP3A4 and the human or mouse pregnane X receptor. Subsequently, the cells were incubated with the test compounds and the activity of luciferase determined. Bosentan activated the human pregnane X receptor with an EC(50) of 19.9 microM, whereas rifampicin had an EC(50) value of 1.9 microM. Ro 47-8634 (4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-hydroxy-phenoxy)-2,2'-bipyrimidin-4-yl]-benzenesulfonamide), a metabolite of bosentan, and glibenclamide also activated the pregnane X receptor. The findings provide a molecular mechanism for the interactions observed between bosentan and several drugs.[1]

References

  1. Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptor. van Giersbergen, P.L., Gnerre, C., Treiber, A., Dingemanse, J., Meyer, U.A. Eur. J. Pharmacol. (2002) [Pubmed]
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