Efflux and uptake transport and gut microbial reactivation of raloxifene glucuronides.

ABSTRACT: Raloxifene has low bioavailability due to extensive glucuronidation in the intestine and the liver, and its pharmacokinetics is associated with high intra- and interindividual variability. Some of this variability could be explained by the enterohepatic recycling of raloxifene, which is driven by transporter-mediated uptake and efflux and gut microbial deglucuronidation of raloxifene glucuronides. These individual processes involved in raloxifene disposition, however, have not been characterized in full detail. In this study, we evaluated the interactions of raloxifene and its three glucuronide metabolites (raloxifene 4'-glucuronide, raloxifene 6-glucuronide and raloxifene 4',6-diglucuronide) with drug transporters using Sf9 membrane vesicles and HEK293 cells. Additionally, we measured the

SUBMITTER: Uoti A 

PROVIDER: S-EPMC11659111 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature