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Items: 16


Improving Prediction of Metabolic Clearance Using Quantitative Extrapolation of Results Obtained From Human Hepatic Micropatterned Cocultures Model and by Considering the Impact of Albumin Binding.

Da-Silva F, Boulenc X, Vermet H, Compigne P, Gerbal-Chaloin S, Daujat-Chavanieu M, Klieber S, Poulin P.

J Pharm Sci. 2018 Jul;107(7):1957-1972. doi: 10.1016/j.xphs.2018.03.001. Epub 2018 Mar 7.


Applicability of second-generation upcyte® human hepatocytes for use in CYP inhibition and induction studies.

Ramachandran SD, Vivarès A, Klieber S, Hewitt NJ, Muenst B, Heinz S, Walles H, Braspenning J.

Pharmacol Res Perspect. 2015 Oct;3(5):e00161. doi: 10.1002/prp2.161. Epub 2015 Aug 10.


Evaluation of Normalization Methods To Predict CYP3A4 Induction in Six Fully Characterized Cryopreserved Human Hepatocyte Preparations and HepaRG Cells.

Vermet H, Raoust N, Ngo R, Esserméant L, Klieber S, Fabre G, Boulenc X.

Drug Metab Dispos. 2016 Jan;44(1):50-60. doi: 10.1124/dmd.115.065581. Epub 2015 Oct 14.


Analysis of Glycogen Synthase Kinase Inhibitors That Regulate Cytochrome P450 Expression in Primary Human Hepatocytes by Activation of β-Catenin, Aryl Hydrocarbon Receptor and Pregnane X Receptor Signaling.

Briolotti P, Chaloin L, Balaguer P, Da Silva F, Tománková V, Pascussi JM, Duret C, Fabre JM, Ramos J, Klieber S, Maurel P, Daujat-Chavanieu M, Gerbal-Chaloin S.

Toxicol Sci. 2015 Nov;148(1):261-75. doi: 10.1093/toxsci/kfv177. Epub 2015 Aug 10.


Antibiotics. Targeting DnaN for tuberculosis therapy using novel griselimycins.

Kling A, Lukat P, Almeida DV, Bauer A, Fontaine E, Sordello S, Zaburannyi N, Herrmann J, Wenzel SC, König C, Ammerman NC, Barrio MB, Borchers K, Bordon-Pallier F, Brönstrup M, Courtemanche G, Gerlitz M, Geslin M, Hammann P, Heinz DW, Hoffmann H, Klieber S, Kohlmann M, Kurz M, Lair C, Matter H, Nuermberger E, Tyagi S, Fraisse L, Grosset JH, Lagrange S, Müller R.

Science. 2015 Jun 5;348(6239):1106-12. doi: 10.1126/science.aaa4690.


PBPK modeling of irbesartan: incorporation of hepatic uptake.

Chapy H, Klieber S, Brun P, Gerbal-Chaloin S, Boulenc X, Nicolas O.

Biopharm Drug Dispos. 2015 Nov;36(8):491-506. doi: 10.1002/bdd.1961. Epub 2015 Aug 3.


Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drug.

Klieber S, Arabeyre-Fabre C, Moliner P, Marti E, Mandray M, Ngo R, Ollier C, Brun P, Fabre G.

Pharmacol Res Perspect. 2014 Jun;2(3):e00044. doi: 10.1002/prp2.44. Epub 2014 Apr 22.


The WNT/β-catenin pathway is a transcriptional regulator of CYP2E1, CYP1A2, and aryl hydrocarbon receptor gene expression in primary human hepatocytes.

Gerbal-Chaloin S, Dumé AS, Briolotti P, Klieber S, Raulet E, Duret C, Fabre JM, Ramos J, Maurel P, Daujat-Chavanieu M.

Mol Pharmacol. 2014 Dec;86(6):624-34. doi: 10.1124/mol.114.094797. Epub 2014 Sep 16.


Morphological behaviour and metabolic capacity of cryopreserved human primary hepatocytes cultivated in a perfused multiwell device.

Vivares A, Salle-Lefort S, Arabeyre-Fabre C, Ngo R, Penarier G, Bremond M, Moliner P, Gallas JF, Fabre G, Klieber S.

Xenobiotica. 2015 Jan;45(1):29-44. doi: 10.3109/00498254.2014.944612. Epub 2014 Jul 28.


Effect of deuteration on the metabolism and clearance of some pharmacologically active compounds--synthesis and in vitro metabolism of deuterated derivatives of dronedadrone.

Schofield J, Brasseur D, de Bruin B, Vassal T, Klieber S, Arabeyre C, Bourrié M, Sadoun F, Fabre G.

J Labelled Comp Radiopharm. 2013 Jul-Aug;56(9-10):504-12. doi: 10.1002/jlcr.3090. Epub 2013 Sep 4.


5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.

Meneyrol J, Follmann M, Lassalle G, Wehner V, Barre G, Rousseaux T, Altenburger JM, Petit F, Bocskei Z, Schreuder H, Alet N, Herault JP, Millet L, Dol F, Florian P, Schaeffer P, Sadoun F, Klieber S, Briot C, Bono F, Herbert JM.

J Med Chem. 2013 Dec 12;56(23):9441-56. doi: 10.1021/jm4005835. Epub 2013 Dec 3.


Modular bioreactor for primary human hepatocyte culture: medium flow stimulates expression and activity of detoxification genes.

Vinci B, Duret C, Klieber S, Gerbal-Chaloin S, Sa-Cunha A, Laporte S, Suc B, Maurel P, Ahluwalia A, Daujat-Chavanieu M.

Biotechnol J. 2011 May;6(5):554-64. doi: 10.1002/biot.201000326. Epub 2011 Jan 21.


The use of human hepatocytes to investigate drug metabolism and CYP enzyme induction.

Klieber S, Torreilles F, Guillou F, Fabre G.

Methods Mol Biol. 2010;640:295-308. doi: 10.1007/978-1-60761-688-7_16.


Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans.

Klieber S, Hugla S, Ngo R, Arabeyre-Fabre C, Meunier V, Sadoun F, Fedeli O, Rival M, Bourrie M, Guillou F, Maurel P, Fabre G.

Drug Metab Dispos. 2008 May;36(5):851-62. doi: 10.1124/dmd.107.019539. Epub 2008 Feb 6.


In vitro metabolism of ferroquine (SSR97193) in animal and human hepatic models and antimalarial activity of major metabolites on Plasmodium falciparum.

Daher W, Pelinski L, Klieber S, Sadoun F, Meunier V, Bourrié M, Biot C, Guillou F, Fabre G, Brocard J, Fraisse L, Maffrand JP, Khalife J, Dive D.

Drug Metab Dispos. 2006 Apr;34(4):667-82. Epub 2006 Jan 13.


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