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={E. Jeong and Y. Liu and H. Lin and M. 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… Expand
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References
SHOWING 1-10 OF 40 REFERENCES
Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance.
- Chemistry, Medicine
- Drug metabolism and disposition: the biological fate of chemicals
- 2002
- 166
- Highly Influential
- PDF
Disposition Mechanisms of Raloxifene in the Human Intestinal Caco-2 Model
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2004
- 65
- PDF
Absorption and metabolism of genistein and its five isoflavone analogs in the human intestinal Caco-2 model
- Chemistry, Medicine
- Cancer Chemotherapy and Pharmacology
- 2004
- 100
- PDF
Metabolism of Flavonoids via Enteric Recycling: Role of Intestinal Disposition
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2003
- 213
- PDF
Disposition of Flavonoids via Enteric Recycling: Enzyme-Transporter Coupling Affects Metabolism of Biochanin A and Formononetin and Excretion of Their Phase II Conjugates
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2004
- 82
- PDF
Metabolism of Flavonoids via Enteric Recycling: Mechanistic Studies of Disposition of Apigenin in the Caco-2 Cell Culture Model
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2003
- 122
- PDF
Absorption and metabolism of flavonoids in the caco-2 cell culture model and a perused rat intestinal model.
- Chemistry, Medicine
- Drug metabolism and disposition: the biological fate of chemicals
- 2002
- 220
- PDF
UDP-glucuronosyltransferase activity in human liver and colon.
- Biology, Medicine
- Gastroenterology
- 1999
- 179
Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms.
- Chemistry, Medicine
- The Journal of pharmacology and experimental therapeutics
- 2001
- 269
Expression of the UDP-glucuronosyltransferase 1A Locus in Human Colon
- Biology, Medicine
- The Journal of Biological Chemistry
- 1998
- 269
- PDF