Lysosomal Sequestration (Trapping) of Lipophilic Amine (Cationic Amphiphilic) Drugs in Immortalized Human Hepatocytes (Fa2N-4 Cells)

Aki, 2012, Cytoplasmic vacuolization during exposure to drugs and other substances, Cell Biol Toxicol, 28, 125, 10.1007/s10565-012-9212-3

Anderson, 2006, Drug-induced phospholipidosis, FEBS Lett, 580, 5533, 10.1016/j.febslet.2006.08.061

Angus, 2008, The potential influence of CO2, as an agent for euthanasia, on the pharmacokinetics of basic compounds in rodents, Drug Metab Dispos, 36, 375, 10.1124/dmd.107.018879

Berezhkovskiy, 2011, The corrected traditional equations for calculation of hepatic clearance that account for the difference in drug ionization in extracellular and intracellular tissue water and the corresponding corrected PBPK equation, J Pharm Sci, 100, 1167, 10.1002/jps.22324

Bowman, 1988, Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells, Proc Natl Acad Sci USA, 85, 7972, 10.1073/pnas.85.21.7972

Chadwick, 2005, Potentially hazardous drug interactions with psychotropics, Adv Psychiatr Treat, 11, 440, 10.1192/apt.11.6.440

Daniel, 1999, The role of lysosomes in the cellular distribution of thioridazine and potential drug interactions, Toxicol Appl Pharmacol, 158, 115, 10.1006/taap.1999.8688

de Duve, 1974, Commentary. Lysosomotropic agents, Biochem Pharmacol, 23, 2495, 10.1016/0006-2952(74)90174-9

Duvvuri, 2004, Weak base permeability characteristics influence the intracellular sequestration site in the multidrug-resistant human leukemic cell line HL-60, J Biol Chem, 279, 32367, 10.1074/jbc.M400735200

Duvvuri, 2005, A novel assay reveals that weakly basic model compounds concentrate in lysosomes to an extent greater than pH-partitioning theory would predict, Mol Pharm, 2, 440, 10.1021/mp050043s

Funk, 2012, Cationic amphiphilic drugs cause a marked expansion of apparent lysosomal volume: implications for an intracellular distribution-based drug interaction, Mol Pharm, 9, 1384, 10.1021/mp200641e

Goldman, 2009, Mechanisms of amine accumulation in, and egress from, lysosomes, Bioanalysis, 1, 1445, 10.4155/bio.09.128

Hallifax, 2006, Uptake and intracellular binding of lipophilic amine drugs by isolated rat hepatocytes and implications for prediction of in vivo metabolic clearance, Drug Metab Dispos, 34, 1829, 10.1124/dmd.106.010413

Hallifax, 2007, Saturable uptake of lipophilic amine drugs into isolated hepatocytes: mechanisms and consequences for quantitative clearance prediction, Drug Metab Dispos, 35, 1325, 10.1124/dmd.107.015131

Hallifax, 2012, Evaluation of hepatic clearance prediction using in vitro data: emphasis on fraction unbound in plasma and drug ionisation using a database of 107 drugs, J Pharm Sci, 101, 2645, 10.1002/jps.23202

Hanumegowda, 2010, Phospholipidosis as a function of basicity, lipophilicity, and volume of distribution of compounds, Chem Res Toxicol, 23, 749, 10.1021/tx9003825

Hariparsad, 2008, Comparison of immortalized Fa2N-4 cells and human hepatocytes as in vitro models for cytochrome P450 induction, Drug Metab Dispos, 36, 1046, 10.1124/dmd.108.020677

Hayeshi, 2008, Lysosomal trapping of amodiaquine: impact on transport across intestinal epithelia models, Biopharm Drug Dispos, 29, 324, 10.1002/bdd.616

Jigorel, 2012, Utility of drug depletion-time profiles in isolated hepatocytes for accessing hepatic uptake clearance: identifying rate-limiting steps and role of passive processes, Drug Metab Dispos, 40, 1596, 10.1124/dmd.112.045732

Kannan, 2011, Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET, Proc Natl Acad Sci USA, 108, 2593, 10.1073/pnas.1014641108

Kornhauser, 1980, Uptake of propranolol by the lung and its displacement by other drugs: involvement of the alveolar macrophage, Pharmacology, 20, 275, 10.1159/000137373

Lemieux, 2004, Quantitation of the lysosomotropic character of cationic amphiphilic drugs using the fluorescent basic amine Red DND-99, Anal Biochem, 327, 247, 10.1016/j.ab.2004.01.010

Logan, 2012, Drug-drug interactions involving lysosomes: mechanisms and potential clinical implications, Expert Opin Drug Metab Toxicol, 8, 943, 10.1517/17425255.2012.691165

MacIntyre, 1988, The potential role of lysosomes in tissue distribution of weak bases, Biopharm Drug Dispos, 9, 513, 10.1002/bod.2510090602

Muehlbacher M Tripal P Roas F Kornhuber J (2012). Identification of drugs inducing phospholipidosis by novel in vitro data. ChemMedChem. [published ahead of print].

Nadanaciva, 2011, A high content screening assay for identifying lysosomotropic compounds, Toxicol In Vitro, 25, 715, 10.1016/j.tiv.2010.12.010

Neuvonen, 2006, Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance, Clin Pharmacol Ther, 80, 565, 10.1016/j.clpt.2006.09.003

Obach, 2008, Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds, Drug Metab Dispos, 36, 1385, 10.1124/dmd.108.020479

Pappu, 1985, Inhibition of purified lysosomal phospholipase A1 by beta-adrenoceptor blockers, Biochem Pharmacol, 34, 521, 10.1016/0006-2952(85)90183-2

Paris, 2009, In vitro inhibition and induction of human liver cytochrome p450 enzymes by milnacipran, Drug Metab Dispos, 37, 2045, 10.1124/dmd.109.028274

Parkinson, 2011, An evaluation of the dilution method for identifying metabolism-dependent inhibitors of cytochrome P450 enzymes, Drug Metab Dispos, 39, 1370, 10.1124/dmd.111.038596

Poulin, 2012, In vitro-in vivo extrapolation of clearance: modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing calculation methods, J Pharm Sci, 101, 838, 10.1002/jps.22792

Shayman, 2013, Drug induced phospholipidosis: An acquired lysosomal storage disorder, Biochim Biophys Acta, 1831, 602, 10.1016/j.bbalip.2012.08.013

Siebert, 2004, Ion-trapping, microsomal binding, and unbound drug distribution in the hepatic retention of basic drugs, J Pharmacol Exp Ther, 308, 228, 10.1124/jpet.103.056770

Vestal, 1980, Active uptake of propranolol by isolated rabbit alveolar macrophages and its inhibition by other basic amines, J Pharmacol Exp Ther, 214, 106

Yoshimori, 1991, Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells, J Biol Chem, 266, 17707, 10.1016/S0021-9258(19)47429-2