Title : Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism.

Pub. Date : 2010 Dec

PMID : 21175442






3 Functional Relationships(s)
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1 Finally, a panel of human liver microsomes (genotyped for UGT1A1*28 allele status) was used to determine the importance of UGT1A1 in the direct glucuronidation of repaglinide. repaglinide UDP glucuronosyltransferase family 1 member A1 Homo sapiens
2 UGT1A1 plays a significant role in the glucuronidation of repaglinide. repaglinide UDP glucuronosyltransferase family 1 member A1 Homo sapiens
3 CONCLUSIONS: Inhibition of UGT enzymes, especially UGT1A1, by gemfibrozil and its glucuronide is an additional mechanism to consider when rationalizing the interaction between repaglinide and gemfibrozil. repaglinide UDP glucuronosyltransferase family 1 member A1 Homo sapiens