Affiliation: CHU Dupuytren
- Involvement of UDP-glucuronosyltransferases UGT1A9 and UGT2B7 in ethanol glucuronidation, and interactions with common drugs of abuseAlaa Al Saabi
EA4483, Faculty of Medicine, Universite Lille Nord de France, Lille, France
Drug Metab Dispos 41:568-74. 2013..17 mg/l; inhibition constant (K(i)) = 3.1 mg/l). UGT1A9 and 2B7 are the main enzymes involved in ethanol glucuronidation. In addition, our results suggest that cannabinol and cannabidiol could significantly alter ethanol glucuronidation...
- The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokineticsN Picard
INSERM U850, Limoges, France
Clin Pharmacol Ther 87:100-8. 2010..Further studies demonstrated that this variant of OATP1B3 exhibited a reduced maximal velocity (V(max)) in transfected HEK cells, thereby providing functional evidence to support our clinical findings...
- Metabolism of sirolimus in the presence or absence of cyclosporine by genotyped human liver microsomes and recombinant cytochromes P450 3A4 and 3A5Nicolas Picard
Laboratoire de Pharmacologie Medicale, EA 3838 DEXO, Facultéde Médecine, 2 rue du Dr Marcland, 87025 Limoges, France
Drug Metab Dispos 35:350-5. 2007..In the absence of cyclosporine, the CYP 3A5*3 polymorphism may not influence significantly sirolimus metabolism at the hepatic level. However, strong CYP 3A4 inhibition by cyclosporine could unveil the influence of this polymorphism...
- CYP3A5 genotype does not influence everolimus in vitro metabolism and clinical pharmacokinetics in renal transplant recipientsNicolas Picard
INSERM, UMR S 850, Limoges, France
Transplantation 91:652-6. 2011..CYP3A5 genotyping might be useful to guide tacrolimus and sirolimus dosing. The aim of this study was to assess the influence of CYP3A5 polymorphism on everolimus metabolism and pharmacokinetics...
- Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transportersNicolas Picard
INSERM, UMR S850, Limoges, France
Xenobiotica 41:752-7. 2011..In conclusion, our data suggest that the major OATP transporters expressed in the liver and the intestine do not contribute to the pharmacokinetics of sirolimus and everolimus. However, ImTORs are inhibitors of these transporters...
- Donor P-gp polymorphisms strongly influence renal function and graft loss in a cohort of renal transplant recipients on cyclosporine therapy in a long-term follow-upJ B Woillard
INSERM, UMR S 850, Limoges, France
Clin Pharmacol Ther 88:95-100. 2010..186 mlxmin(-1)/year; P = 0.0240). The study showed that the presence of ABCB1 polymorphisms in donors influences long-term graft outcome adversely with decrease in renal function and graft loss in transplant recipients receiving CsA...
- Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant alleleJean Baptiste Woillard
INSERM, UMR S 850, Limoges, France
Br J Clin Pharmacol 69:675-83. 2010....
- Tacrolimus population pharmacokinetic-pharmacogenetic analysis and Bayesian estimation in renal transplant recipientsKhaled Benkali
INSERM U850, University of Limoges, Limoges, France
Clin Pharmacokinet 48:805-16. 2009....
- [Pharmacogenetics and immunosuppressor drugs: impact and clinical interest in transplantation]P Marquet
Service de pharmacologie toxicologie, CHU Dupuytren, Limoges Cedex, France
Ann Pharm Fr 65:382-9. 2007..The pharmacogenetics of immunosuppressants is thus still an open field for investigations and potential therapeutic progress...
- Contribution of the different UDP-glucuronosyltransferase (UGT) isoforms to buprenorphine and norbuprenorphine metabolism and relationship with the main UGT polymorphisms in a bank of human liver microsomesKoukeb Rouguieg
INSERM, Unité Mixte de Recherche S 850, Limoges, France
Drug Metab Dispos 38:40-5. 2010..0352). This study represents a functional basis for further clinical pharmacogenetic studies...
- Determination of mycophenolic acid plasma levels in renal transplant recipients co-administered sirolimus: comparison of an enzyme multiplied immunoassay technique (EMIT) and liquid chromatography-tandem mass spectrometryAurélie Prémaud
Department of Pharmacology and Toxicology, Limoges University Hospital, Limoges, France
Ther Drug Monit 28:274-7. 2006..7 +/- 2 6.8% with EMIT, with variations depending on the time elapsed since transplantation. An EMIT overestimation of 16.7 +/- 22.5% also was obtained for the MPA areas under the curve calculated using the trapezoidal rule...
- Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenaseOlivier Gensburger
INSERM UMR S850, Limoges, France
Clin Chem 55:986-93. 2009..We investigated the action of the MPA metabolites MPA-phenyl-glucuronide (MPAG) and MPA-acyl-glucuronide (AcMPAG) on recombinant human IMPDH II (rhIMPDH II), as well as their passage into lymphocytes in vitro...
- General unknown screening procedure for the characterization of human drug metabolites: Application to loratadine phase I metabolismNicolas Picard
INSERM, UMR S850, Limoges Cedex, France
J Sep Sci 32:2209-17. 2009..The GUS procedure used in this study may be applicable as a generic technique for the characterization of drug metabolites after in vitro incubation, as well as probably in vivo experiments...
- Influence of the UGT2B7 promoter region and exon 2 polymorphisms and comedications on Acyl-MPAG production in vitro and in adult renal transplant patientsNassim Djebli
Laboratory of Pharmacology, Faculty of Medicine, Limoges University, Limoges University Hospital, 2 Avenue Martin Luther King, 87042 Limoges, France
Pharmacogenet Genomics 17:321-30. 2007....
- A comparison of the effect of ciclosporin and sirolimus on the pharmokinetics of mycophenolate in renal transplant patientsNicolas Picard
Laboratory of Pharmacology, Faculty of Medicine, University of Limoges, France
Br J Clin Pharmacol 62:477-84. 2006..This interaction is probably not caused by inhibition of mycophenolic acid glucuronidation or glycosylation, but is more likely to be due to the influence of ciclosporin on the excretion of mycophenolic acid metabolites into bile...
- In vitro metabolism study of buprenorphine: evidence for new metabolic pathwaysNicolas Picard
Department of Medical Pharmacology, University of Limoges, France
Drug Metab Dispos 33:689-95. 2005..Incubation of BUP or Nor-BUP with HLM led to the formation of new metabolites, identified by tandem mass spectrometry as being hydroxy-BUP and hydroxy-Nor-BUP. Hydroxy-BUP was produced by the CYP 3A, but not the 2C isoforms...
- Characterization of a phase 1 metabolite of mycophenolic acid produced by CYP3A4/5Nicolas Picard
Department of Pharmacology and Toxicology, University Hospital, 87042 Limoges, France
Ther Drug Monit 26:600-8. 2004..MPA might compete with other drugs on CYP3A because of its high therapeutic concentrations, although this was not the case for cyclosporin and to only a small extent for tacrolimus...
- Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolismNicolas Picard
Department of Pharmacology-Toxicology, University Hospital, 87042 Limoges, France
Drug Metab Dispos 33:139-46. 2005..In conclusion, UGT 1A9 and 2B7 were clearly identified as the main UGT isoforms involved in mycophenolic acid glucuronidation, presumably due to their high hepatic and renal expression...