Pfeifer ND, Hardwick RN, Brouwer KL. Role of hepatic efflux transporters in regulating systemic and hepatocyte exposure to xenobiotics. Annu Rev Pharmacol Toxicol. 2014;54:509–35. https://doi.org/10.1146/annurev-pharmtox-011613-140021.

Article  CAS  PubMed  Google Scholar 

Miners JO, Yang X, Knights KM, Zhang L. The role of the kidney in drug elimination: Transport, metabolism, and the impact of kidney disease on drug clearance. Clin Pharmacol Ther. 2017;102:436–49. https://doi.org/10.1002/cpt.757.

Article  CAS  PubMed  Google Scholar 

Shen S, Zhang W. ABC transporters and drug efflux at the blood-brain barrier. Rev Neurosci. 2010;21:29–53. https://doi.org/10.1515/revneuro.2010.21.1.29.

Article  CAS  PubMed  Google Scholar 

Volpe DA, Qosa H. Challenges with the precise prediction of ABC-transporter interactions for improved drug discovery. Expert Opin Drug Discov. 2018;13:697–707. https://doi.org/10.1080/17460441.2018.1493454.

Article  CAS  PubMed  Google Scholar 

Lee CA, Cook JA, Reyner EL, Smith DA. P-glycoprotein related drug interactions: Clinical importance and a consideration of disease states. Expert Opin Drug Metab Toxicol. 2010;6:603–19. https://doi.org/10.1517/17425251003610640.

Article  CAS  PubMed  Google Scholar 

Lin JH. Transporter-mediated drug interactions: clinical implications and in vitro assessment. Expert Opin Drug Metab Toxicol. 2007;3:81–92. https://doi.org/10.1517/17425255.3.1.81.

Article  CAS  PubMed  Google Scholar 

Balimane PV, Marino A, Chong S. P-gp inhibition potential in cell-based models: which “calculation” method is the most accurate? AAPS J. 2008;10:577–86. https://doi.org/10.1208/s12248-008-9068-x.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Balimane PV, Han YH, Chong S. Current industrial practices of assessing permeability and P-glycoprotein interaction. AAPS J. 2006;8:E1-13. https://doi.org/10.1208/aapsj080101.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Elsby R, Atkinson H, Butler P, Riley RJ. Studying the right transporter at the right time: an in vitro strategy for assessing drug-drug interaction risk during drug discovery and development. Expert Opinion Drug Metab Toxicol. 2022;18:619–55. https://doi.org/10.1080/17425255.2022.2132932.

Article  CAS  Google Scholar 

Keogh JP, Kunta JR. Development, validation and utility of an in vitro technique for assessment of potential clinical drug-drug interactions involving P-glycoprotein. Eur J Pharm Sci. 2006;27:543–54. https://doi.org/10.1016/j.ejps.2005.11.011.

Article  CAS  PubMed  Google Scholar 

Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, et al. Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001;299:620–8.

CAS  PubMed  Google Scholar 

Seithel A, Karlsson J, Hilgendorf C, Björquist A, Ungell AL. Variability in mRNA expression of ABC- and SLC-transporters in human intestinal cells: comparison between human segments and Caco-2 cells. Eur J Pharm Sci. 2006;28:291–9. https://doi.org/10.1016/j.ejps.2006.03.003.

Article  CAS  PubMed  Google Scholar 

Hilgendorf C, Ahlin G, Seithel A, Artursson P, Ungell AL, Karlsson J. Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines. Drug Metab Dispos. 2007;35:1333–40. https://doi.org/10.1124/dmd.107.014902.

Article  CAS  PubMed  Google Scholar 

Wang Q, Strab R, Kardos P, Ferguson C, Li J, Owen A, et al. Application and limitation of inhibitors in drug-transporter interactions studies. Int J Pharm. 2008;356:12–8. https://doi.org/10.1016/j.ijpharm.2007.12.024.

Article  CAS  PubMed  Google Scholar 

Maubon N, Le Vee M, Fossati L, Audry M, Le Ferrec E, Bolze S, Fardel O. Analysis of drug transporter expression in human intestinal Caco-2 cells by real-time PCR. Fundam Clin Pharmacol. 2007;21(6):659–63. https://doi.org/10.1111/j.1472-8206.2007.00550.x.

Article  CAS  PubMed  Google Scholar 

Vaessen SF, van Lipzig MM, Pieters RH, Krul CA, Wortelboer HM, van de Steeg E. Regional expression levels of drug transporters and metabolizing enzymes along the pig and human intestinal tract and comparison with Caco-2 cells. Drug Metab Dispos. 2017;45:353–60. https://doi.org/10.1124/dmd.116.072231.

Article  CAS  PubMed  Google Scholar 

Chen EC, Broccatelli F, Plise E, Chen B, Liu L, Cheong J, et al. Evaluating the utility of canine Mdr1 knockout Madin-Darby canine kidney I cells in permeability screening and efflux substrate determination. Mol Pharm. 2018;15:5103–13. https://doi.org/10.1021/acs.molpharmaceut.8b00688.

Article  CAS  PubMed  Google Scholar 

Gartzke D, Delzer J, Laplanche L, Uchida Y, Hoshi Y, Tachikawa M, et al. Genomic knockout of endogenous canine P-glycoprotein in wild-type, human P-glycoprotein and human BCRP transfected MDCKII cell lines by zinc finger nucleases. Pharm Res. 2015;32:2060–71. https://doi.org/10.1007/s11095-014-1599-5.

Article  CAS  PubMed  Google Scholar 

Li J, Wang Y, Hidalgo IJ. Kinetic analysis of human and canine P-glycoprotein-mediated drug transport in MDR1-MDCK cell model: approaches to reduce false-negative substrate classification. J Pharm Sci. 2013;102:3436–46. https://doi.org/10.1002/jps.23523.

Article  CAS  PubMed  Google Scholar 

Simoff I, Karlgren M, Backlund M, Lindström AC, Gaugaz F`Z, Matsson P, et al. Complete knockout of endogenous Mdr1 (Abcb1) in MDCK cells by CRISPR-Cas9. J Pharm Sci. 2016; 105:1017–1021. https://doi.org/10.1016/S0022-3549(15)00171-9

Mease K, Sane R, Podila L, Taub ME. Differential selectivity of efflux transporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: a strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2. J Pharm Sci. 2012;101:1888–97. https://doi.org/10.1002/jps.23069.

Article  CAS  PubMed  Google Scholar 

Graber-Maier A, Gutmann H, Drewe J. A new intestinal cell culture model to discriminate the relative contribution of P-gp and BCRP on transport of substrates such as imatinib. Mol Pharm. 2010;7:1618–28. https://doi.org/10.1021/mp100040f.

Article  CAS  PubMed  Google Scholar 

Litman T, Druley TE, Stein WD, Bates SE. From MDR to MXR: new understanding of multidrug resistance systems, their properties and clinical significance. Cell Mol Life Sci. 2001;58:931–59. https://doi.org/10.1007/PL00000912.

Article  CAS  PubMed  Google Scholar 

Matsson P, Pedersen JM, Norinder U, Bergström CAS, Artursson P. Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs. Pharm Res. 2009;26:1816–31. https://doi.org/10.1007/s11095-009-9896-0.

Article  CAS  PubMed  Google Scholar 

Tang F, Horie K, Borchardt RT. Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm Res. 2002;19:765–72. https://doi.org/10.1023/a:1016140429238.

Article  CAS  PubMed  Google Scholar 

Tang F, Horie K, Borchardt RT. Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002;19(6):773–9. https://doi.org/10.1023/a:1016192413308.

Article  CAS  PubMed  Google Scholar 

Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B. Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000;57(4):760–8. https://doi.org/10.1124/mol.57.4.760.

Article  CAS  PubMed  Google Scholar 

Xia CQ, Liu N, Yang D, Miwa G, Gan LS. Expression, localization, and functional characteristics of breast cancer resistance protein in Caco-2 cells. Drug Metab Dispos. 2005;33(5):637–43. https://doi.org/10.1124/dmd.104.003442.

Article