SPECIES- AND DISPOSITION MODEL-DEPENDENT METABOLISM OF RALOXIFENE IN GUT AND LIVER: ROLE OF UGT1A10

@article{Jeong2005SPECIESAD,
  title={SPECIES- AND DISPOSITION MODEL-DEPENDENT METABOLISM OF RALOXIFENE IN GUT AND LIVER: ROLE OF UGT1A10},
  author={Eun Ju Jeong and Yong Liu and Huimin Lin and Ming Hu},
  journal={Drug Metabolism and Disposition},
  year={2005},
  volume={33},
  pages={785 - 794}
}
Caco-2 cell lysate, and intestinal and liver microsomes derived from female humans and rats were used to compare and contrast the metabolism and disposition of raloxifene. In Caco-2 cell lysate, raloxifene 6-β-glucuronide (M1) was the main metabolite, although raloxifene 4′-β-glucuronide (M2) was formed in comparable abundance (58% versus 42%). In rat liver and intestinal microsomes, M1 represented about 76 to 86% of glucuronidated metabolites. In contrast, raloxifene 4′-β-glucuronide (M2) was… 

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