TABLE 1

Bosentan clinical data included in the PBPK modeling exercise

Dosed Compound(s)Dosing RouteDosing AmountReference
mg
BosentanIntravenous infusion (5 min)10, 50, 250, 500, or 750 Weber et al. (1996)
BosentanIntravenous infusion (15 min)250Weber et al. (1999b)
BosentanTablet after high-fat meal500U.S. Food and Drug Administration (2001)
BosentanTablet after high-fat meal125Dingemanse et al. (2002)
BosentanTablet500Weber et al. (1999c)
BosentanTablet62.5van Giersbergen et al. (2002b)
Bosentan (twice daily) and tadalafil (once daily)TabletBosentan: 125; tadalafil: 40Wrishko et al. (2008)
Bosentan (twice daily) and warfarin (once on day 6)TabletBosentan: 500; racemic mixture of warfarin: 26 Weber et al. (1999a)