PHARMACOLOGY

Olivier FARDEL

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Olivier Fardel received his PharmD in 1986 and his PhD on the “Expression and regulation of P-glycoprotein in normal and cancerous hepatocytes” in 1993 at the University of Rennes (France). He is currently full professor at the Faculty of Pharmaceutical and Biological Sciences of Rennes (University of Rennes 1). He leads a research team at the Research Institute for Environmental and Occupational Health (IRSET), a joint project between the French national agency for medical research (INSERM), Rennes 1 University and EHESP School of Public Health. His research activities notably concern cellular and molecular regulation of drug transporter expression and activity in hepatocytes and functional consequences for hepatobiliary disposition of drugs and environmental chemical contaminants. He published more than 150 original and review articles in peer-refereed scientific journals and scientific books.

Int J Mol Sci. 2021 Nov 29;22:12926. Substrate-dependent trans-stimulation of Organic Cation Transporter 2 activity. Lefèvre CR, Le Vée M, Gaubert S, Jouan E, Bruyere A, Moreau C, Fardel O. PubMed 

Eur J Drug Metab Pharmacokinet. 2021;46:625-635. Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) activity by Tyrosine Kinase Inhibitors. Jouan E, Moreau A, Bruyere A, Alim K, Denizot C, Parmentier Y, Fardel O. PubMed

Biopharm Drug Dispos. 2021;42:393-398. Comparative in silico prediction of P-glycoprotein-mediated transport for 2010-2020 US FDA-approved drugs using six Web-tools. Guéniche N, Huguet A, Bruyere A, Habauzit D, Le Hégarat L, Fardel O. PubMed

Fundam Clin Pharmacol2021;35:919-929. Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. Alim K, Moreau A, Bruyère A, Jouan E, Denizot C, Nies AT, Parmentier Y, Fardel O. PubMed

Xenobiotica. 2021;51:467-478. Differential in vitro interactions of the Janus kinase inhibitor ruxolitinib with human SLC drug transporters. Bruyère A, Le Vée M, Jouan E, Molez S, Nies AT, Fardel O. PubMed

Expert Opin Drug Metab Toxicol. 2021;17:259-271. Interactions of janus kinase inhibitors with drug transporters and consequences for pharmacokinetics and toxicity. Alim K, Bruyère A, Lescoat A, Jouan E, Lecureur V, Le Vée M, Fardel O. PubMed

Xenobiotica. 2020 Jun 4:1-13. Differential interactions of carbamate pesticides with drug transporters. Guéniche N, Bruyere A, Ringeval M, Jouan E, Huguet A, Le Hégarat L, Fardel O. PubMed

Int Immunopharmacol. 2020 Jun;83:106439. Janus kinase-dependent regulation of drug detoxifying protein expression by interleukin-22 in human hepatic cells. Le Vée M, Bruyère A, Jouan E, Fardel O. Int Immunopharmacol. 2020;83:106439. PubMed

Fundam Clin Pharmacol. 2020;In press. Differential interactions of the β-lactam cloxacillin with human renal organic anion transporters (OATs). Lalanne S, Le Vée M, Lemaitre F, Le Corre P, Verdier MC, Fardel O. PubMed

Inflamm Res. 2020;69:51-62. Potent repression of C-reactive protein (CRP) expression by the JAK1/2 inhibitor ruxolitinib in inflammatory human hepatocytes. Febvre-James M, Lecureur V, Fardel O. PubMed

Pest Manag Sci. 2020;76:18-25. Implication of human drug transporters to toxicokinetics and toxicity of pesticides. Guéniche N, Bruyere A, Le Vée M, Fardel O. PubMed

J Biochem Mol Toxicol. 2019;33:e22379. Neonicotinoid pesticides poorly interact with human drug transporters. Le Vée M, Bacle A, Bruyere A, Fardel O. PubMed

Toxicol In Vitro. 2019;58:60-68. Induction of multidrug resistance-associated protein 3 expression by diesel exhaust particle extract in human bronchial epithelial BEAS-2B cells. Le Vée M, Bacle A, Jouan E, Lecureur V, Potin S, Fardel O. PubMed

Environ Int. 2019;126:659-671. Membrane transporter data to support kinetically-informed chemical risk assessment using non-animal methods: Scientific and regulatory perspectives. Clerbaux LA, Paini A, Lumen A, Osman-Ponchet H, Worth AP, Fardel O. PubMed

Pharmaceutics. 2018;10. pii: E246. mRNA expression and activity of Nucleoside Transporters in human hepatoma HepaRG cells. Mayati A, Moreau A, Jouan E, Febvre-James M, Denizot C, Parmentier Y, Fardel O. PubMed

Sci Rep. 2018;8:16115. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Mayati A, Moreau A, Le Vée M, Bruyère A, Jouan E, Denizot C, Parmentier Y, Fardel O. PubMed

Toxicol In Vitro. 2019;54:10-22. Inhibition of organic cation transporter (OCT) activities by carcinogenic heterocyclic aromatic amines. Sayyed K, Camillerapp C, Le Vée M, Bruyère A, Nies AT, Abdel-Razzak Z, Fardel O. PubMed

Eur J Drug Metab Pharmacokinet. 2019;44:13-30. Evaluation of drug biliary excretion using sandwich-cultured human hepatocytes. Fardel O, Moreau A, Le Vée M, Denizot C, Parmentier Y. PubMed

Expert Opin Drug Metab Toxicol. 2018;14:739-752. Interactions of pesticides with membrane drug transporters: implications for toxicokinetics and toxicity. Chedik L, Bruyere A, Bacle A, Potin S, Le Vée M, Fardel O. PubMed

Eur J Pharm Sci. 2018;121:85-94. New insights in the in vitro characterisation and molecular modelling of the P-glycoprotein inhibitory promiscuity. Bocci G, Moreau A, Vayer P, Denizot C, Fardel O, Parmentier Y. PubMed

Xenobiotica. 2018;6:1-12. Interactions of organophosphorus pesticides with solute carrier (SLC) drug transporters. Chedik L, Bruyere A, Fardel O. PubMed

Drug Metab Dispos. 2018;46:131-140. The JAK1/2 inhibitor Ruxolitinib reverses interleukin-6-mediated suppression of drug-detoxifying proteins in cultured human hepatocytes. Febvre-James M, Bruyère A, Le Vée M, Fardel O. PubMed

Toxicol In Vitro. 2017;44:27-35. Inhibition of organic anion transporter (OAT) activity by cigarette smoke condensate. Sayyed K, Le Vee M, Abdel-Razzak Z, Fardel O. PubMed

Eur J Pharm Sci. 2017;106:302-312. β2-adrenergic receptor-mediated in vitro regulation of human hepatic drug transporter expression by epinephrine. Mayati A, Moreau A, Denizot C, Stieger B, Parmentier Y, Fardel O. PubMed

Int J Mol Sci. 2017;18. pii: E764. Protein Kinases C-mediated regulations of drug transporter activity, localization and expression. Mayati A, Moreau A, Le Vée M, Stieger B, Denizot C, Parmentier Y, Fardel O. PubMed

Eur J Drug Metab Pharmacokinet. 2017; in press. Effect of Gevokizumab on Interleukin-1β-mediated cytochrome P450 3A4 and drug transporter repression in cultured human hepatocytes. Moreau A, Le Vée M, Jouan E, Denizot C, Parmentier Y, Fardel O. PubMed

PLoS One. 2017;12:e0169480. Inhibition of human drug transporter activities by the pyrethroid pesticides Allethrin and Tetramethrin. Chedik L, Bruyere A, Le Vee M, Stieger B, Denizot C, Parmentier Y, Potin S, Fardel O. PubMed

Toxicol In Vitro. 2017;40:34-44. Inhibition of SLC drug transporter activities by environmental bisphenols. Bruyere A, Hubert C, Le Vee M, Chedik L, Sayyed K, Stieger B, Denizot C, Parmentier Y, Fardel O. PubMed

Pharmaceutics. 2016;9: E3. Drug transporter expression and activity in human hepatoma HuH-7 cells. Jouan E, Le Vée M, Denizot C, Parmentier Y, Fardel O. PubMed

Pharmaceutics. 2016;8: E12.  Evaluation of P-Glycoprotein inhibitory potential using a Rhodamine 123 accumulation assay. Jouan E, Le Vée M, Mayati A, Denizot C, Parmentier Y, Fardel O. PubMed

Toxicology. 2016;363-364:58-71. Alteration of human hepatic drug transporter activity and expression by cigarette smoke condensate. Sayyed K, Vee ML, Abdel-Razzak Z, Jouan E, Stieger B, Denizot C, Parmentier Y, Fardel O. In the present study, the authors demonstrate that cigarette smoke condensate (CSC) alters the activity and expression of hepatic drug transporters, which are recognized as major actors of hepatobiliary elimination of drugs. PubMed

PLoS One. 2015;10:e0144667. Protein kinase C-independent inhibition of Organic Cation Transporter 1 activity by the bisindolylmaleimide Ro 31-8220. Mayati A, Bruyere A, Moreau A, Jouan E, Denizot C, Parmentier Y, Fardel O. PubMed

Biochem Pharmacol. 2015;98:703-17. Protein kinase C-dependent regulation of human hepatic drug transporter expression. Mayati A, Le Vee M, Moreau A, Jouan E, Bucher S, Stieger B, Denizot C, Parmentier Y, Fardel O. PubMed

Methods Mol Biol. 2015;1250:287-302. Analysis of sinusoidal drug uptake transporter activities in primary human hepatocytes. Le Vée M, Jouan E, Denizot C, Parmentier Y, Fardel O. PubMed

Expert Opin Drug Metab Toxicol. 2015;11:1233-51. Nature and uses of fluorescent dyes for drug transporter studies. Fardel O, Le Vee M, Jouan E, Denizot C, Parmentier Y. PubMed

Toxicol In Vitro. 2015;29:938-46. Polarized location of SLC and ABC drug transporters in monolayer-cultured human hepatocytes. Le Vee M, Jouan E, Noel G, Stieger B, Fardel O. PubMed

PLoS One. 2015;10:e0121232. Regulation of human hepatic drug transporter activity and expression by diesel exhaust particle extract. Le Vee M, Jouan E, Stieger B, Lecureur V, Fardel O. PubMed

Virology. 2015;481:34-42. Interleukin 6 inhibits HBV entry through NTCP down regulation. Bouezzedine F, Fardel O, Gripon P. PubMed

J Biochem Mol Toxicol. 2014;28:119-28. Regulation of hepatic drug transporter activity and expression by organochlorine pesticides. Bucher S, Le Vee M, Jouan E, Fardel O. PubMed

Toxicol In Vitro. 2013;27:1979-86. Polarized expression of drug transporters in differentiated human hepatoma HepaRG cells. Le Vee M, Noel G, Jouan E, Stieger B, Fardel O. PubMed

Eur J Pharm Sci. 2013;49:39-50. Functional expression and regulation of drug transporters in monolayer- and sandwich-cultured mouse hepatocytes. Noel G, Le Vee M, Moreau A, Stieger B, Parmentier Y, Fardel O. PubMed

Eur J Pharm Sci. 2013;48:767-74. Differential regulation of drug transporter expression by all-trans retinoic acid in hepatoma HepaRG cells and human hepatocytes. Le Vee M, Jouan E, Stieger B, Fardel O. PubMed

Fundam Clin Pharmacol. 2014;28:65-77. The mitochondrial fluorescent dye rhodamine 123 is a high-affinity substrate for organic cation transporters (OCTs) 1 and 2. Jouan E, Le Vee M, Denizot C, Da Violante G, Fardel O. PubMed

Expert Opin Drug Metab Toxicol. 2012;8:29-46. Environmental chemicals as substrates, inhibitors or inducers of drug transporters: implication for toxicokinetics, toxicity and pharmacokinetics. Fardel O, Kolasa E, Le Vee M. PubMed

Biochem Pharmacol. 2011;82:304-11. Regulation of drug transporter expression by oncostatin M in human hepatocytes. Le Vee M, Jouan E, Stieger B, Lecureur V, Fardel O. PubMed

Fundam Clin Pharmacol. 2011;25:99-103. Regulation of drug transporter mRNA expression by interferon-γ in primary human hepatocytes. Le Vee M, Jouan E, Moreau A, Fardel O. PubMed

Expert Opin Drug Metab Toxicol. 2009;5:1469-81. Regulation of human hepatic drug transporter expression by pro-inflammatory cytokines. Fardel O, Le Vée M. PubMed

Drug Metab Dispos. 2009;37:2228-35. Differential regulation of drug transporter expression by hepatocyte growth factor in primary human hepatocytes. Le Vee M, Lecureur V, Moreau A, Stieger B, Fardel O. PubMed

Drug Metab Dispos. 2009;37:685-93. Regulation of drug transporter expression in human hepatocytes exposed to the proinflammatory cytokines tumor necrosis factor-alpha or interleukin-6. Le Vee M, Lecureur V, Stieger B, Fardel O. PubMed

Drug Metab Dispos. 2008;36:217-22. Down-regulation of organic anion transporter expression in human hepatocytes exposed to the proinflammatory cytokine interleukin 1beta. Le Vee M, Gripon P, Stieger B, Fardel O. PubMed

Drug Metab Dispos. 2006;34:1756-63. Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Jigorel E, Le Vee M, Boursier-Neyret C, Parmentier Y, Fardel O. PubMed