Low systemic exposure of oral docetaxel in mice resulting from extensive first-pass metabolism is boosted by ritonavir
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HA Bardelmeijer, M Ouwehand, T Buckle…
Cancer …, 2002
aacrjournals.org
P-glycoprotein seems to be the most important factor limiting the oral absorption of paclitaxel. We have now explored the mechanisms responsible for the low oral bioavailability of docetaxel, a structurally related taxane drug. The recovery of 33% of oxidative metabolites and only 39% of unchanged drug in the feces of FVB wild-type mice receiving 10 mg/kg of oral docetaxel indicates that the major part of the oral dose has been absorbed. The feces and bile of mice receiving 10 mg/kg of iv docetaxel contained large …