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Abbreviation : ER
Long Form : efflux ratio
No. Year Title Co-occurring Abbreviation
2020 Investigation of MDR1-overexpressing cell lines to derive a quantitative prediction approach for brain disposition using in vitro efflux activities. BCRP, CFR, WT
2020 Permeability and transport mechanism of trihexyphenidyl hydrochloride in Caco-2 cell monolayer model with a validated UPLC-MS/MS method. IS, LLOQ, TH
2019 Potential P-glycoprotein-mediated herb-drug interaction of phyllanthin at the intestinal absorptive barrier. LY, P-gp, TEER
2019 Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors. ASK1
2019 Simplified Method to Determine the Efflux Ratio on P-Glycoprotein Substrates Using Three-Compartment Model Analysis for Caco-2 Cell Assay Data. P-gp
2019 The Impact of Endogenous Breast Cancer Resistance Protein on Human P-Glycoprotein-Mediated Transport Assays Using LLC-PK1 Cells Transfected With Human P-Glycoprotein. BCRP, LLC-PK1, WT
2019 Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells. 7,8-DHF, AP, BCRP, BDNF, BL, MRPs, OATPs, OCTs, P-gp
2018 ABCC10 Plays a Significant Role in the Transport of Gefitinib and Contributes to Acquired Resistance to Gefitinib in NSCLC. ABC, EGFR, MDR, NSCLC, RNA-Seq
2018 Effect of five novel 5-substituted tetrandrine derivatives on P-glycoprotein-mediated inhibition and transport in Caco-2 cells. MDR, Rho-123, Tet, TF
10  2018 Evaluating the Utility of Canine Mdr1 Knockout Madin-Darby Canine Kidney I Cells in Permeability Screening and Efflux Substrate Determination. A-to-B, MDCK, WT
11  2018 Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. BTK, SAP
12  2017 Abcb1a (P-glycoprotein) limits brain exposure of the anticancer drug candidate seliciclib in vivo in adult mice. AUCbrain, BBB
13  2017 Drug-transporter mediated interactions between anthelminthic and antiretroviral drugs across the Caco-2 cell monolayers. ARVs, IVM, PZQ, TEER
14  2017 Elucidation of Compatibility Interactions of Traditional Chinese Medicines: In Vitro Absorptions Across Caco-2 Monolayer of Coptidis Rhizoma and Euodiae Fructus in Zuojin and Fanzuojin Formulas as A Case. CR, EF, FZJF, Papp
15  2017 In Silico and in Vitro Screening for P-Glycoprotein Interaction with Tenofovir, Darunavir, and Dapivirine: An Antiretroviral Drug Combination for Topical Prevention of Colorectal HIV Transmission. P-gp
16  2017 Transport of curcumin derivatives in Caco-2 cell monolayers. AP-BL, CUR
17  2016 In vitro blood-brain barrier permeability predictions for GABAA receptor modulating piperine analogs. BBB, BLEC, GABAA
18  2016 Integrating in Silico and in Vitro Approaches To Predict Drug Accessibility to the Central Nervous System. BBB, CNS, neuroPK, P-gp, QSAR
19  2016 Intestinal permeability and P-glycoprotein-mediated efflux transport of ticagrelor in Caco-2 monolayer cells. P-gp, Papp
20  2016 Intracellular Retention of Three Quinuclidine Derivatives in Caco-2 Permeation Experiments: Mechanisms and Impact on Estimating Permeability and Active Efflux Ratio. ---
21  2015 Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor. P-gp, PDE10A, SBDD
22  2015 Effects of herbal drugs in Mahuang decoction and their main components on intestinal transport characteristics of Ephedra alkaloids evaluated by a Caco-2 cell monolayer model. DPEP, LEP, LMEP, PAB, TCM
23  2015 Multidrug resistance-associated protein 2 is involved in the efflux of Aconitum alkaloids determined by MRP2-MDCKII cells. AC, BAC, BCRP, BHA, BMA, HA, MA, MRP2, P-gp
24  2015 Transport and uptake of clausenamide enantiomers in CYP3A4-transfected Caco-2 cells: An insight into the efflux-metabolism alliance. CLA
25  2014 Calibration of in vitro multidrug resistance protein 1 substrate and inhibition assays as a basis to support the prediction of clinically relevant interactions in vivo. CNS, DDIs, L-MDR1, MDR1
26  2014 Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: an assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers. ---
27  2014 Development and validation of a LC-MS/MS method for assessment of an anti-inflammatory indolinone derivative by in vitro blood-brain barrier models. BBB, P-gp, PBCECs, RHB, RT
28  2014 Digoxin net secretory transport in bronchial epithelial cell layers is not exclusively mediated by P-glycoprotein/MDR1. ALI, MDCKII, NHBE
29  2013 Effects of Borneol on Pharmacokinetics and Tissue Distribution of Notoginsenoside R1 and Ginsenosides Rg1 and Re in Panax notoginseng in Rabbits. GRg1, NGR1
30  2013 In vitro P-glycoprotein efflux ratio can predict the in vivo brain penetration regardless of biopharmaceutics drug disposition classification system class. BBB, BDDCS, CNS, P-gp
31  2013 Physicochemical characterization and in vitro permeation of an indirubin derivative. CML
32  2013 PK/PD assessment in CNS drug discovery: Prediction of CSF concentration in rodents for P-glycoprotein substrates and application to in vivo potency estimation. BBB, CNS, Cu_p
33  2013 The role of efflux transporters on the transport of highly toxic aconitine, mesaconitine, hypaconitine, and their hydrolysates, as determined in cultured Caco-2 and transfected MDCKII cells. AC, BAC, BCRP, BHA, BMA, HA, MA, MRP2, P-gp
34  2012 A transcellular assay to assess the P-gp inhibition in early stage of drug development. NSF
35  2012 [Drug delivery systems of baicalin, baicalin-phospholipid complex and self-microemulsifying drug across Caco-2 cell model]. BA, BA-PC, SMEDDS
36  2011 Establishment of in vitro P-glycoprotein inhibition assay and its exclusion criteria to assess the risk of drug-drug interaction at the drug discovery stage. DDI, MDR1, P-gp
37  2008 Application and limitation of inhibitors in drug-transporter interactions studies. E3S
38  2007 Kinetic considerations for the quantitative assessment of efflux activity and inhibition: implications for understanding and predicting the effects of efflux inhibition. PS
39  2005 Functional role of P-glycoprotein in limiting intestinal absorption of drugs: contribution of passive permeability to P-glycoprotein mediated efflux transport. AQ, BCS, HIA, NS, P-gp-mediated, P-gpS
40  2001 Transport of peptidomimetic thrombin inhibitors with a 3-amidino-phenylalanine structure: permeability and efflux mechanism in monolayers of a human intestinal cell line (Caco-2). TEER