The Journal of Steroid Biochemistry and Molecular Biology
Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity
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Sulfonation of raloxifene in HEK293 cells overexpressing SULT1A3: Involvement of breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated protein 4 (MRP4/ABCC4) in excretion of sulfate metabolites
2015, Drug Metabolism and PharmacokineticsCitation Excerpt :Since raloxifene glucuronides are found in blood in an old report, previous metabolism studies have mainly focused on glucuronidation, giving less attention to other metabolic pathways such as sulfonation [21]. However, there is accumulating evidence that sulfonation plays an important role in disposition of raloxifene in human tissues [20,22,23]. Analysis of sulfonation pathway will help to understand the mechanisms of raloxifene [20].
Effect of UDP-glucuronosyltransferase 1A8 polymorphism on raloxifene glucuronidation
2013, European Journal of Pharmaceutical SciencesCitation Excerpt :In addition, these clinical studies have reported that the products of in vivo metabolism are glucuronides at 6- and/or 4′-positions of raloxifene, and that the plasma concentration of 4′-glucuronide is about 8-fold higher than that of 6-glucuronide. The glucuronides exhibit minimal binding to estrogen receptor but they should not be overlooked as they can be readily reconverted to active raloxifene in various organs (Dodge et al., 1997). Raloxifene glucuronidation has been identified to be catalyzed by UGT1A1, UGT1A8, UGT1A9 and UGT1A10 in humans (Fig. 1) (Kemp et al., 2002).
Synthesis of estradiol backbone mimics via the Stille reaction using copper(II) oxide as co-reagent
2011, Tetrahedron LettersIn vitro evaluation, biodistribution in rats of radiolabeled raloxifene
2010, Applied Radiation and IsotopesPharmacokinetics of raloxifene in male Wistar-Hannover rats: Influence of complexation with hydroxybutenyl-beta-cyclodextrin
2008, International Journal of Pharmaceutics