8, GW4064 treatment caused a significant increase in the mRNA level of phase II conjugation enzymes and phase III transporters, including glutathione S-transferases (GSTs) (Gst[alpha]3 and Gst[alpha]4) as well as GSH metabolism-related genes (Gclm, GpxJ), glucuronosyltransferase
(Ugtlal), sulfotransferases (SultJal) (phase II), and efflux transporters (Mrp2 and Bsep) (phase III).
Raltegravir is primarily metabolised by glucuronidation via uridine diphosphate glucuronosyltransferase
Coadministration of ISENTRESS with drugs that are strong inducers of uridine diphosphate glucuronosyltransferase
(UGT) 1A1 may result in reduced plasma concentrations of raltegravir.
Findings on the roles of genetic polymorphisms in the UGT1A9 (UDP glucuronosyltransferase
1 family, polypeptide A9) gene for mycophenolate mofetil (16), the UGT2B7 (UDP glucuronosyltransferase
2 family, polypeptide B7) gene for acyl-glucuronide mycophenolic acid (17), and CYP3A5/ABCB1 for Tac exposure and acute rejection (18) in the FDCC study have previously been published.
One of these isoforms, encoded by the UGT1A1 (UDP glucuronosyltransferase
1 family, polypeptide A1) gene, is an enzyme that conjugates bilirubin with glucuronic acid in the liver, making bilirubin more water soluble (3).
1) Drug Interactions -- Caution should be used when coadministering ISENTRESS with strong inducers of uridine diphosphate glucuronosyltransferase
(UGT) 1A1 (e.
Pharmacogenetics: Many different single-nucleotide polymorphisms (SNPs) and their associations with individual responses to drugs and clinical outcomes have been tested [IMPDH (8) (inosine 5'-monophosphate dehydrogenase 1), CYP3A5 (cytochrome P450, family 3, subfamily A, polypeptide 5), UGT1A9 (UDP glucuronosyltransferase
1 family, polypeptide A9), ABCB1 (ATP-binding cassette, sub-family B (MDR/TAP), member 1; formerly MDR1), IL10 (interleukin 10), TGFB1 (transforming growth factor, beta 1)].
We have previously reported a positive association between PCBs grouped according to their potential to induce uridine diphosphate glucuronosyltransferase
(UDP-GT) in rodents and neonatal TSH (Chevrier et al.
Co administration with strong inducers of uridine diphosphate glucuronosyltransferase
(UGT) 1A1 may reduce plasma concentrations of ISENTRESS.
Discrimination between Crigler-Najjar type I and II by expression of mutant bilirubin uridine diphosphate glucuronosyltransferase
The identified chromosomal region harbors the gene for the uridine diphosphate glucuronosyltransferase
(UGT1A1,  UDP glucuronosyltransferase
1 family, polypeptide A1), the major enzyme of bilirubin glucuronidation, which mainly determines bilirubin elimination in humans.
The dose of ISENTRESS should be increased during coadministration with rifampin, a strong uridine diphosphate glucuronosyltransferase
(UGT) 1A1, due to reduced plasma concentrations of ISENTRESS.