Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of 3-hydroxydesloratadine

Biopharmaceutics and Drug Disposition

Volumn 25, Issue 6, 2004, Pages 243-252

  Ghosal, Anima ^a   Yuan, Yuan ^a   Hapangama, Neil ^a   Su, Ai Duen ^a   Alvarez, Narciso ^a   Chowdhury, Swapan K ^a   Alton, Kevin B ^a   Patrick, James E ^a   Zbaida, Shmuel ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Desloratadine; Glucuronides; UGT; UGT1A1; UGT1A3; UGT2B15

Indexed keywords

3 HYDROXYDESLORATADINE; ANTIHISTAMINIC AGENT; BILIRUBIN; DESLORATADINE; DICLOFENAC; DRUG METABOLITE; FLUNITRAZEPAM; GLUCURONIDE; GLUCURONOSYLTRANSFERASE; RECOMBINANT ENZYME; UNCLASSIFIED DRUG; URIDINE DIPHOSPHATE GLUCURONIC ACID;

ALLERGIC RHINITIS; ARTICLE; CONTROLLED STUDY; DRUG APPROVAL; DRUG GLUCURONIDATION; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; INCUBATION TIME; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; MASS SPECTROMETRY;

BILIRUBIN; DICLOFENAC; ENZYME INHIBITORS; FLUNITRAZEPAM; GLUCURONIDES; GLUCURONOSYLTRANSFERASE; HISTAMINE H1 ANTAGONISTS, NON-SEDATING; HUMANS; LORATADINE; MICROSOMES, LIVER; TIME FACTORS;

EID: 4644327579     PISSN: 01422782     EISSN: None     Source Type: Journal    
DOI: 10.1002/bdd.405     Document Type: Article

References (15)

1. Tukey RH, Strassburg CP. Human UDP-glucuronosyltransferases: Metabolism, expression and disease. Ann Rev Pharmacol Toxicol 2000; 40: 581-616.
2. Ramanathan R, Su A-D, Alvarez N, et al. Liquid chromatography/mass spectrometry methods for distinguishing N-oxides from hydroxylated compounds. Anal Chem 2000; 72: 1352-1359.
3. Fisher MB, Campanale K, Ackermann BL, Vandenbranden M, Wrighton SA. In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin. Drug Metab Dispos 2000; 28: 560-566.
4. Pless D, Gouze JN, Senay C, et al. Characterization of the UDP-glucuronosyltransferases involved in the glucuronidation of an antithrombotic thioxyloside in rat and humans. Drug Metab Dispos 1999; 27: 588-595.
5. Dehal SS, Gagne PV, Crespi CL, Patten CJ. Characterization of a probe substrate and an inhibitor of UDP glucuronosyltransferase (UGT) 1A4 activity in human liver microsomes (HLM) and cDNA-expressed UGT-enzymes. In 6th International ISSX Meeting at Munich, Germany, 2001. Drug Metabolism Reviews, Volume 33, 2001, Page 162 Abstract No. 321, Marcel Dekker Inc.
6. Cheng Z, Radominska-Pandya A, Tephly TR. Studies on the substrate specificity of human intestinal UDP-glucuronosyltransferases 1A8 and 1A10. Drug Metab Dispos 1999; 27: 1165-1170.
7. Strassburg CP, Manns MP, Tukey RH. Expression of the UDP-glucuronosyltransferase 1A locus in human colon. Identification and characterization of the novel extrahepatic UGT1A8. J Biol Chem 1998; 273: 8719-8726.
8. Strassburg CP, Nguyen N, Manns MP, Tukey RH. Polymorphic expression of the UDP-glucuronosyltransferase UGT1A gene locus in human gastric epithelium. Mol Pharm 1998; 54: 647-654.
9. Miners JO, Valente L, Lillywhite KJ, et al. Preclinical prediction of factors influencing the elimination of 5,6-dimethylxanthenone-4-acetic acid, a new anticancer drug. Cancer Res 1997; 57: 284-289.
10. Kirkwood LC, Nation RL, Somogyi AA. Glucuronidation of dihydrocodeine by human liver microsomes and the effect of inhibitors. Clin Exp Pharmacol Physiol 1998; 25: 266-270.
11. King C, Finley B, Franklin R. The glucuronidation of morphine by dog liver microsomes: Identification of morphine-6-O-glucuronide. Drug Metab Dispos 2000; 28: 661-663.
12. Cheng Z, Rios GR, King CD, et al. Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3 and 2B7. Toxicol Sci 1998; 45: 52-57.
13. Hagenauer B, Salamon A, Thalhammer T, et al. In vitro glucuronidation of the cyclin-dependent kinase inhibitor flavopiridol by rat and human liver microsomes: Involvement of UDP-glucuronosyltransferases 1A1 and 1A9. Drug Metab Dispos 2001; 29: 407-414.
14. Williams JA, Ring BJ, Cantrell VE, et al. Differential modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1)-catalysed estradiol-3-glucuronidation by the addition of UGT1A1 substrates and other compounds to human liver microsomes. Drug Metab Dispos 2002; 30: 1266-1273.
15. Soars MG, Ring BJ, Wrighton SA. The effect of incubation conditions on the enzyme kinetics of UDP-glucuronosyltransferases. Drug Metab Dispos 2003; 31: 762-767.