Models to predict unbound intracellular drug concentrations in the presence of transporters

Drug Metabolism and Disposition

Volumn 40, Issue 5, 2012, Pages 865-876

  Korzekwa, Ken R ^a   Nagar, Swati ^a   Tucker, Jalia ^a   Weiskircher, Erica A ^b   Bhoopathy, Siddhartha ^b   Hidalgo, Ismael J ^b  

^a TEMPLE UNIVERSITY SCHOOL OF PHARMACY   (United States)

^b Absorption Systems   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMPRENAVIR; ATORVASTATIN; CYCLOSPORIN A; DIGOXIN; LABETALOL; LOPERAMIDE; MINOXIDIL; MULTIDRUG RESISTANCE PROTEIN 1; PITAVASTATIN; REPAGLINIDE; SIMVASTATIN; VERAPAMIL;

ACTIVE TRANSPORT; ANIMAL CELL; ARTICLE; CELL STRAIN; CELLULAR DISTRIBUTION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG PENETRATION; MARKER GENE; MATHEMATICAL MODEL; MDR1 GENE; MONOLAYER CULTURE; NONHUMAN; PREDICTIVE VALUE; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN LOCALIZATION; SIMULATION; SYSTEMATIC ERROR;

ANIMALS; BIOLOGICAL TRANSPORT; CELL LINE; CELL MEMBRANE; CELL MEMBRANE PERMEABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CYCLOSPORINE; DOGS; MODELS, BIOLOGICAL; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS; PREDICTIVE VALUE OF TESTS;

EID: 84859903256     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.044289     Document Type: Article

References (25)

1. Acharya P, O'Connor MP, Polli JW, Ayrton A, Ellens H, and Bentz J (2008) Kinetic identification of membrane transporters that assist P-glycoprotein- mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells. Drug Metab Dispos 36:452-460. (Pubitemid 351185760)
2. Agarwal S, Hartz AM, Elmquist WF, and Bauer B (2011) Breast cancer resistance protein and P-glycoprotein in brain cancer: two gatekeepers team up. Curr Pharm Des 17:2793-2802.
3. Fan J, Maeng HJ, and Pang KS (2010) Interplay of transporters and enzymes in the Caco-2 cell monolayer: I. effect of altered apical secretion. Biopharm Drug Dispos 31:215-227.
4. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, et al. (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
5. Girardin F (2006) Membrane transporter proteins: a challenge for CNS drug development. Dialogues Clin Neurosci 8:311-321.
6. Gottesman MM, Hrycyna CA, Schoenlein PV, Germann UA, and Pastan I (1995) Genetic analysis of the multidrug transporter. Annu Rev Genet 29:607-649. (Pubitemid 26005354)
7. Gottesman MM, Pastan I, and Ambudkar SV (1996) P-glycoprotein and multidrug resistance. Curr Opin Genet Dev 6:610-617. (Pubitemid 26372158)
8. Hegewisch-Becker S (1996) MDR1 reversal: criteria for clinical trials designed to overcome the multidrug resistance phenotype. Leukemia 10(Suppl 3):S32-S38.
9. Hennessy M and Spiers JP (2007) A primer on the mechanics of P-glycoprotein the multidrug transporter. Pharmacol Res 55:1-15. (Pubitemid 46108588)
10. Hsiao P, Sasongko L, Link JM, Mankoff DA, Muzi M, Collier AC, and Unadkat JD (2006) Verapamil P-glycoprotein transport across the rat blood-brain barrier: cyclosporine, a concentration inhibition analysis, and comparison with human data. J Pharmacol Exp Ther 317:704-710.
11. Kalvass JC, Graff CL, and Pollack GM (2004) Use of loperamide as a phenotypic probe of mdr1a status in CF-1 mice. Pharm Res 21:1867-1870. (Pubitemid 39390099)
12. Knipp GT, Ho NF, Barsuhn CL, and Borchardt RT (1997) Paracellular diffusion in Caco-2 cell monolayers: effect of perturbation on the transport of hydrophilic compounds that vary in charge and size. J Pharm Sci 86:1105-1110. (Pubitemid 27430913)
13. Komin N and Toral R (2009) Drug absorption through a cell monolayer: a theoretical work on a non-linear three-compartment model. Eur J Pharm Sci 37:106-114.
14. Lam JL, Okochi H, Huang Y, and Benet LZ (2006) In vitro and in vivo correlation of hepatic transporter effects on erythromycin metabolism: characterizing the importance of transporterenzyme interplay. Drug Metab Dispos 34:1336-1344. (Pubitemid 44079874)
15. Lee JK, Marion TL, Abe K, Lim C, Pollock GM, and Brouwer KL (2010) Hepatobiliary disposition of troglitazone and metabolites in rat and human sandwich-cultured hepatocytes: use of Monte Carlo simulations to assess the impact of changes in biliary excretion on troglitazone sulfate accumulation. J Pharmacol Exp Ther 332:26-34.
16. Li C, Wu YL, Yang T, Zhang Y, and Huang-Fu WG (2010) Simultaneous determination of clenbuterol, salbutamol and ractopamine in milk by reversed-phase liquid chromatography tandem mass spectrometry with isotope dilution. J Chromatogr A 1217:7873-7877.
17. McEntee M, Silverman JA, Rassnick K, Zgola M, Chan AO, Tau PT, and Page RL (2003) Enhanced bioavailability of oral docetaxel by co-administration of cyclosporin A in dogs and rats. Vet Comp Oncol 1:105-112.
18. Obach RS (1999) Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes. Drug Metab Dispos 27:1350-1359.
19. Pang KS, Maeng HJ, and Fan J (2009) Interplay of transporters and enzymes in drug and metabolite processing. Mol Pharm 6:1734-1755.
20. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, and Borst P (1995) Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest 96:1698-1705.
21. Sun H, Chow EC, Liu S, Du Y, and Pang KS (2008a) The Caco-2 cell monolayer: usefulness and limitations. Expert Opin Drug Metab Toxicol 4:395-411. (Pubitemid 351728514)
22. Sun H, Zhang L, Chow EC, Lin G, Zuo Z, and Pang KS (2008b) A catenary model to study transport and conjugation of baicalein, a bioactive flavonoid, in the Caco-2 cell monolayer: demonstration of substrate inhibition. J Pharmacol Exp Ther 326:117-126. (Pubitemid 351872137)
23. Swift B, Pfeifer ND, and Brouwer KL (2010) Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metab Rev 42:446-471.
24. Urquhart BL and Kim RB (2009) Blood-brain barrier transporters and response to CNS-active drugs. Eur J Clin Pharmacol 65:1063-1070.
25. Wang Q, Strab R, Kardos P, Ferguson C, Li J, Owen A, and Hidalgo IJ (2008) Application and limitation of inhibitors in drug-transporter interactions studies. Int J Pharm 356:12-18.