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Meeting the challenge of predicting hepatic clearance of compounds slowly metabolized by cytochrome P450 using a novel hepatocyte model, HepatoPac.

Chan TS, Yu H, Moore A, Khetani SR, Tweedie D.

Drug Metab Dispos. 2013 Dec;41(12):2024-32. doi: 10.1124/dmd.113.053397. Epub 2013 Aug 19. Erratum in: Drug Metab Dispos. 2014 Jan;42(1):200. Kehtani, Salman R [corrected to Khetani, Salman R].


Generating an in vitro-in vivo correlation for metabolism and liver enrichment of a hepatitis C virus drug, faldaprevir, using a rat hepatocyte model (HepatoPac).

Ramsden D, Tweedie DJ, St George R, Chen LZ, Li Y.

Drug Metab Dispos. 2014 Mar;42(3):407-14. doi: 10.1124/dmd.113.055947. Epub 2013 Dec 23.


Bridging in vitro and in vivo metabolism and transport of faldaprevir in human using a novel cocultured human hepatocyte system, HepatoPac.

Ramsden D, Tweedie DJ, Chan TS, Taub ME, Li Y.

Drug Metab Dispos. 2014 Mar;42(3):394-406. doi: 10.1124/dmd.113.055897. Epub 2013 Dec 23.


Metabolite formation kinetics and intrinsic clearance of phenacetin, tolbutamide, alprazolam, and midazolam in adenoviral cytochrome P450-transfected HepG2 cells and comparison with hepatocytes and in vivo.

Donato MT, Hallifax D, Picazo L, Castell JV, Houston JB, Gomez-Lechón MJ, Lahoz A.

Drug Metab Dispos. 2010 Sep;38(9):1449-55. doi: 10.1124/dmd.110.033605. Epub 2010 May 25.


Modeling the in vitro intrinsic clearance of the slowly metabolized compound tolbutamide determined in sandwich-cultured rat hepatocytes.

Treijtel N, Barendregt A, Freidig AP, Blaauboer BJ, van Eijkeren JC.

Drug Metab Dispos. 2004 Aug;32(8):884-91.


A novel relay method for determining low-clearance values.

Di L, Trapa P, Obach RS, Atkinson K, Bi YA, Wolford AC, Tan B, McDonald TS, Lai Y, Tremaine LM.

Drug Metab Dispos. 2012 Sep;40(9):1860-5. doi: 10.1124/dmd.112.046425. Epub 2012 May 29.


Prediction of in vivo rat biliary drug clearance from an in vitro hepatocyte efflux model.

Lundquist P, Lööf J, Fagerholm U, Sjögren I, Johansson J, Briem S, Hoogstraate J, Afzelius L, Andersson TB.

Drug Metab Dispos. 2014 Mar;42(3):459-68. doi: 10.1124/dmd.113.054155. Epub 2014 Jan 6.


Prediction of metabolic clearance using cryopreserved human hepatocytes: kinetic characteristics for five benzodiazepines.

Hallifax D, Rawden HC, Hakooz N, Houston JB.

Drug Metab Dispos. 2005 Dec;33(12):1852-8. Epub 2005 Sep 20.


Prediction of hepatic clearance using cryopreserved human hepatocytes: a comparison of serum and serum-free incubations.

Blanchard N, Hewitt NJ, Silber P, Jones H, Coassolo P, Lavé T.

J Pharm Pharmacol. 2006 May;58(5):633-41.


Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.

Sanoh S, Horiguchi A, Sugihara K, Kotake Y, Tayama Y, Ohshita H, Tateno C, Horie T, Kitamura S, Ohta S.

Drug Metab Dispos. 2012 Feb;40(2):322-8. doi: 10.1124/dmd.111.040923. Epub 2011 Nov 2.


A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes.

Riley RJ, McGinnity DF, Austin RP.

Drug Metab Dispos. 2005 Sep;33(9):1304-11. Epub 2005 Jun 2.


Prediction of human hepatic clearance using an in vitro plated hepatocyte clearance model.

Chao P, Barminko J, Novik E, Han Y, Maguire T, Cheng KC.

Drug Metab Lett. 2009 Dec;3(4):296-307.


Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.

Zanelli U, Caradonna NP, Hallifax D, Turlizzi E, Houston JB.

Drug Metab Dispos. 2012 Jan;40(1):104-10. doi: 10.1124/dmd.111.042309. Epub 2011 Oct 13.


Substrate depletion approach for determining in vitro metabolic clearance: time dependencies in hepatocyte and microsomal incubations.

Jones HM, Houston JB.

Drug Metab Dispos. 2004 Sep;32(9):973-82. Erratum in: Drug Metab Dispos. 2004 Nov;32(11):1331.


A comprehensive evaluation of metabolic activity and intrinsic clearance in suspensions and monolayer cultures of cryopreserved primary human hepatocytes.

Smith CM, Nolan CK, Edwards MA, Hatfield JB, Stewart TW, Ferguson SS, Lecluyse EL, Sahi J.

J Pharm Sci. 2012 Oct;101(10):3989-4002. doi: 10.1002/jps.23262. Epub 2012 Jul 17.

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