In Vitro–In Vivo Extrapolation of Clearance: Modeling Hepatic Metabolic Clearance of Highly Bound Drugs and Comparative Assessment with Existing Calculation Methods

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

Obach, R. S. (1999) · Drug Metabolism and Disposition · doi:10.1016/s0090-9556(24)14938-0 · Cited by 1,232 · see citing works

Practical Aspects of the Ligand-Binding and Enzymatic Properties of Human Serum Albumin.

Kragh‐Hansen, U., Chuang, V. T. G., & Otagiri, M. (2002) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.25.695 · Cited by 896 · see citing works

Physiologically Based Pharmacokinetic Modeling 1: Predicting the Tissue Distribution of Moderate-to-Strong Bases

Rodgers, T., Leahy, D., & Rowland, M. (2005) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20322 · Cited by 776 · see citing works

Effects of Charge on Antibody Tissue Distribution and Pharmacokinetics

Boswell, C. A., Tesar, D. B., Mukhyala, K., Theil, F.-P., Fielder, P. J., & Khawli, L. A. (2010) · Bioconjugate Chemistry · doi:10.1021/bc100261d · Cited by 398 · see citing works

Prediction of Human Pharmacokinetics from Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches

Hosea, N. A., Collard, W. T., Cole, S., Maurer, T. S., Fang, R. X., Jones, H., Kakar, S. M., Nakai, Y., Smith, B. J., Webster, R., et al. (2009) · The Journal of Clinical Pharmacology · doi:10.1177/0091270009333209 · Cited by 300 · see citing works

The pharmacokinetics of midazolam in man

Smith, M. T., Eadie, M. J., & Brophy, T. (1981) · European Journal of Clinical Pharmacology · doi:10.1007/bf00562804 · Cited by 278 · see citing works

Reduced elimination of IgG antibodies by engineering the variable region

Igawa, T., Tsunoda, H., Tachibana, T., Maeda, A., Mimoto, F., Moriyama, C., Nanami, M., Sekimori, Y., Nabuchi, Y., Aso, Y., et al. (2010) · Protein Engineering Design and Selection · doi:10.1093/protein/gzq009 · Cited by 265 · see citing works

Plasma protein binding of basic drugs

Piafsky, K. M., & Borga, O. (1977) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt1977225part1545 · Cited by 232 · see citing works

PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: Comparative assessement of prediction methods of human clearance

Ring, B. J., Chien, J. Y., Adkison, K. K., Jones, H. M., Rowland, M., Jones, R. D., Yates, J. W. T., Ku, M. S., Gibson, C. R., He, H., et al. (2011) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22552 · Cited by 206 · see citing works

The plasma protein binding of basic drugs.

Routledge, P. (1986) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.1986.tb02927.x · Cited by 181 · see citing works

Plasma protein binding of basic drugs. I. Selective displacement from alpha 1-acid glycoprotein by tris(2-butoxyethyl) phosphate.

Borgå, O., Piafsky, K. M., & Nilsen, O. G. (1977) · PubMed · Cited by 160 · see citing works

A unified algorithm for predicting partition coefficients for PBPK modeling of drugs and environmental chemicals

Peyret, T., Poulin, P., & Krishnan, K. (2010) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2010.09.010 · Cited by 136 · see citing works

In vitro–in vivoextrapolation of hepatic clearance: Biological tools, scaling factors, model assumptions and correct concentrations

Pelkonen, O., & Turpeinen, M. (2007) · Xenobiotica · doi:10.1080/00498250701620726 · Cited by 118 · see citing works

Influence of Non-Steroidal Anti-Inflammatory Drugs on Organic Anion Transporting Polypeptide (OATP) 1B1- and OATP1B3-Mediated Drug Transport

Kindla, J., Müller, F., Mieth, M., Fromm, M. F., & König, J. (2011) · Drug Metabolism and Disposition · doi:10.1124/dmd.110.037622 · Cited by 106 · see citing works

Effect of age and sex on the plasma binding of acidic and basic drugs

Verbeeck, R. K., Cardinal, J.-A., & Wallace, S. M. (1984) · European Journal of Clinical Pharmacology · doi:10.1007/bf00553161 · Cited by 104 · see citing works

Alpha 1‐acid glycoprotein (orosomucoid) and plasma protein binding of quinine in falciparum malaria.

Silamut, K., Molunto, P., Ho, M., Davis, T. M. E., & White, N. J. (1991) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.1991.tb03904.x · Cited by 86 · see citing works

Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease

Bilello, J. A., Bilello, P., Stellrecht, K. A., Leonard, J. M., Norbeck, D. W., Kempf, D. J., Robins, T., & Drusano, G. L. (1996) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.40.6.1491 · Cited by 78 · see citing works

Orosomucoid (α1-acid glycoprotein) plasma concentration and genetic variants: Effects on human immunodeficiency virus protease inhibitor clearance and cellular accumulation

Colombo, S. F., Buclin, T., Decosterd, L. A., Telenti, A., Furrer, H., LEE, B., Biollaz, J., & Eap, C. B. (2006) · Clinical Pharmacology & Therapeutics · doi:10.1016/j.clpt.2006.06.006 · Cited by 77 · see citing works

Prediction of human pharmacokinetics—evaluation of methods for prediction of hepatic metabolic clearance

Fagerholm, U. (2007) · Journal of Pharmacy and Pharmacology · doi:10.1211/jpp.59.6.0007 · Cited by 76 · see citing works

Role of Site-Specific Binding to Plasma Albumin in Drug Availability to Brain

Mandula, H., Parepally, J. M. R., Feng, R., & Smith, Q. R. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.097402 · Cited by 66 · see citing works

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

Blanchard, N., Hewitt, N. J., Silber, P. M., Jones, H. M., Coassolo, P., & Lavé, T. (2006) · Journal of Pharmacy and Pharmacology · doi:10.1211/jpp.58.5.0008 · Cited by 63 · see citing works

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

Berezhkovskiy, L. M. (2011) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22324 · Cited by 63 · see citing works

Use of intrinsic clearance for prediction of human hepatic clearance

Chao, P., Uss, A. S., & Cheng, K. (2010) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1517/17425250903405622 · Cited by 62 · see citing works

In Vitro Protein Binding of Diclofenac Sodium in Plasma and Synovial Fluid

Chan, K. K. H., Vyas, K. H., & Brandt, K. D. (1987) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600760204 · Cited by 59 · see citing works

Cationic Drug Pharmacokinetics in Diseased Livers Determined by Fibrosis Index, Hepatic Protein Content, Microsomal Activity, and Nature of Drug

Hung, D. Y., Chang, P., Cheung, K., McWhinney, B. C., Masci, P. P., Weiß, M., & Roberts, M. S. (2002) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.301.3.1079 · Cited by 57 · see citing works

Verapamil plasma binding: Relationship to α1-acid glycoprotein and drug efficacy

McGowan, F. X. J., Reiter, M. J., Pritchett, E. L. C., & Shand, D. G. (1983) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1983.66 · Cited by 57 · see citing works

Effect of Albumin on Phenytoin and Tolbutamide Metabolism in Human Liver Microsomes: An Impact More Than Protein Binding

Tang, C., Lin, Y. J., Rodrigues, A. D., & Lin, J. H. (2002) · Drug Metabolism and Disposition · doi:10.1124/dmd.30.6.648 · Cited by 56 · see citing works

Impact of serum on clearance predictions obtained from suspensions and primary cultures of rat hepatocytes

Blanchard, N., Richert, L., Notter, B., Delobel, F., David, P., Coassolo, P., & Lavé, T. (2004) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2004.07.007 · Cited by 55 · see citing works

Biosynthesis of Rat serum albumin

Judah, J. D., & Nicholls, M. R. (1971) · Biochemical Journal · doi:10.1042/bj1230649 · Cited by 52 · see citing works

Microsome composition-based model as a mechanistic tool to predict nonspecific binding of drugs in liver microsomes

Poulin, P., & Haddad, S. (2011) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22619 · Cited by 50 · see citing works

Comparison of intrinsic clearances in human liver microsomes and suspended hepatocytes from the same donor livers: clearance-dependent relationship and implications for prediction ofin vivoclearance

Foster, J. A., Houston, J. B., & Hallifax, D. (2010) · Xenobiotica · doi:10.3109/00498254.2010.530700 · Cited by 49 · see citing works

Comparison of clearance predictions using primary cultures and suspensions of human hepatocytes

Blanchard, N., Alexandre, E., Viollon‐Abadie, C., Lavé, T., Heyd, B., Mantion, G., Jaeck, D., Richert, L., & Coassolo, P. (2005) · Xenobiotica · doi:10.1080/00498250400021820 · Cited by 48 · see citing works

Pharmacokinetics of tenoxicam in healthy human volunteers.

Heintz, R., Guentert, T. W., Enrico, J. F., Dubach, U. C., Brandt, R. D., & Jeunet, F. (1984) · PubMed · Cited by 44 · see citing works

Measurement of intracellular albumin in rat liver

Gordon, A. H., & Humphrey, J. (1961) · Biochemical Journal · doi:10.1042/bj0780551 · Cited by 43 · see citing works

Interaction of albumin with the endothelial cell surface

Osterloh, K. R. S., Ewert, U., & Pries, A. R. (2002) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.00558.2001 · Cited by 42 · see citing works

A hybrid approach to advancing quantitative prediction of tissue distribution of basic drugs in human

Poulin, P., Ekins, S., & Theil, F. (2010) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2010.10.014 · Cited by 38 · see citing works

Are tolfenamic acid and tenidap dual inhibitors of 5-lipoxygenase and cyclo-oxygenase?

Proudman, K. E., & McMillan, R. M. (1991) · Inflammation Research · doi:10.1007/bf01993255 · Cited by 35 · see citing works

Palmitate uptake by cultured hepatocytes: albumin binding and stagnant layer phenomena

Burczynski, F. J., Cai, Z., Moran, J. B., & Forker, E. L. (1989) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1989.257.4.g584 · Cited by 33 · see citing works

Protein binding of drugs in plasma, interstitial fluid and tissues: Effect on pharmacokinetics

Faed, E. M. (1981) · European Journal of Clinical Pharmacology · doi:10.1007/bf00609592 · Cited by 32 · see citing works

Hepatocyte [3H]-palmitate uptake: effect of albumin surface charge modification

Burczynski, F. J., Wang, G.-Q., Elmadhoun, B., She, Y., Roberts, M. S., & Standing, K. G. (2001) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/cjpp-79-10-868 · Cited by 31 · see citing works

Hepatocyte [³H]-palmitate uptake: effect of albumin surface charge modification

Burczynski, F. J., Wang, G. Q., Elmadhoun, B., She, Y. M., Roberts, M. S., & Standing, K. G. (2001) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/y01-072 · Cited by 28 · see citing works

Extrapolating In vitro Metabolic Interactions to Isolated Perfused Liver: Predictions of Metabolic Interactions between R-Bufuralol, Bunitrolol, and Debrisoquine

Haddad, S., Poulin, P., & Funk, C. (2010) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22136 · Cited by 26 · see citing works

Membrane lipids of hepatocytes, Kupffer cells and endothelial cells

Gabellec, M., Steffan, A., Dodeur, M., Durand, G., Kirn, A., & Rebel, G. (1983) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(83)91076-8 · Cited by 26 · see citing works

Toward an integrated human clearance prediction strategy that minimizes animal use

Beaumont, K. C., Gardner, I. B., Chapman, K. L., Hall, M., & Rowland, M. (2011) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22635 · Cited by 21 · see citing works

Enantioselective plasma protein binding of propafenone: Mechanism, drug interaction, and species difference

Hong, Y., Tang, Y., & Zeng, S. (2008) · Chirality · doi:10.1002/chir.20666 · Cited by 21 · see citing works

Protein binding study of clozapine by capillary electrophoresis in the frontal analysis mode

Zhou, D., & Li, F. (2004) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2004.02.019 · Cited by 21 · see citing works

Effects of Serum Albumin and Liver Cytosol on CYP2C9- and CYP3A4-mediated Drug Metabolism

Baba, T., Touchi, A., Ito, K., Yamaguchi, Y., Yamazoe, Y., Ohno, Y., & Sugiyama, Y. (2002) · Drug Metabolism and Pharmacokinetics · doi:10.2133/dmpk.17.522 · Cited by 21 · see citing works

On the prediction of hepatic clearance using the diluted plasma in metabolic stability assay.

Berezhkovskiy, L. M., Khojasteh, S. C., Halladay, J. S., & Hop, C. (2009) · Journal of Pharmacy and Science · doi:10.1002/jps.21582 · Cited by 20 · see citing works

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

Chao, P., Barminko, J., Novik, E. I., Han, Y., Maguire, T., & Cheng, K.-C. (2009) · Drug Metabolism Letters · doi:10.2174/187231209790218073 · Cited by 18 · see citing works

Triazolam protein binding and correlation with alpha-1 acid glycoprotein concentration

Kroboth, P. D., Smith, R. B., Sorkin, M. I., Silver, M. R., Rault, R., Garry, M. R., & Juhl, R. P. (1984) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1984.191 · Cited by 18 · see citing works

Plasma protein binding of zolpidem in liver and renal insufficiency.

Gm, P., Viani, A., Rizzo, G. E., Carrai, M., Ganansia, J., Bianchetti, G., & Morselli, P. L. (1988) · PubMed · Cited by 18 · see citing works

Propranolol Disposition in the Rat: Variation in Hepatic Extraction with Unbound Drug Fraction

Gariépy, L., Fenyves, D., & Villeneuve, J. (1992) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600810314 · Cited by 17 · see citing works

Decreased elimination of drug in the presence of alpha-1-acid glycoprotein is related to a reduced hepatocyte uptake.

Qin, M., Nilsson, M., & Oie, S. (1994) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)38855-5 · Cited by 16 · see citing works

Binding of diazepam and desmethyldiazepam to plasma protein: Concentration-dependence and interactions

Divoll, M., & Greenblatt, D. J. (1981) · Psychopharmacology · doi:10.1007/bf00435857 · Cited by 14 · see citing works

Influence of midazolam on the protein binding of ketorolac

Reed, M. D., Myers, C. M., & Blumer, J. L. (2001) · Current Therapeutic Research · doi:10.1016/s0011-393x(01)80061-8 · Cited by 14 · see citing works

Binding of 5-Methoxypsoralen to Blood Fractions

Muret, P., Makki, S., Urien, S., Agache, P. G., Bechtel, P. R., & Tillement, J. P. (2009) · Skin Pharmacology · doi:10.1159/000211084 · Cited by 8 · see citing works

Binding of 5-methoxypsoralen to blood fractions. Influence of albumin and free fatty acids: an in vitro study.

Muret, P., Makki, S., Urien, S., Agache, P. G., Bechtel, P. R., & Tillement, J. P. (1993) · PubMed · Cited by 3 · see citing works

Triazolam protein binding and correlation with alpha-1 acid glycoprotein

Kroboth, P. D., Smith, R. B., Sorkin, M. I., Mr, S., Rault, R., Garry, M., & Juhl, R. P. (1985) · Journal of Clinical Psychopharmacology · doi:10.1097/00004714-198502000-00016 · Cited by 2 · see citing works

A Pharmacokinetic Model for Tenidap in Normal Volunteers and Rheumatoid Arthritis Patients

Evans, L., Aarons, L. J., & Coates, P. E. (1999) · Pharmaceutical Research · doi:10.1023/a:1018969024101 · Cited by 2 · see citing works

Effect of β-CD on the Electrochemical Behavior of Tenoxicam

Guzmán‐Hernández, D. S., Ramírez-Silva, M. T., Alarcón-Ángeles, G., & Rojas-Hernándéz, A. (2008) · ECS Transactions · doi:10.1149/1.3046652 · Cited by 1 · see citing works

Recent advances in 2D and 3D in vitro systems using primary hepatocytes, alternative hepatocyte sources and non-parenchymal liver cells and their use in investigating mechanisms of hepatotoxicity, cell signaling and ADME

Godoy, P., Hewitt, N. J., Albrecht, U., Andersen, M. E., Ansari, N., Bhattacharya, S., Bode, J. G., Bolleyn, J., Borner, C., Böttger, J., et al. (2013) · Archives of Toxicology · doi:10.1007/s00204-013-1078-5 · Cited by 1,280 · see citing works

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

Kazmi, F., Hensley, T. N., Pope, C. A., Funk, R. S., Loewen, G. J., Buckley, D. B., & Parkinson, A. (2013) · Drug Metabolism and Disposition · doi:10.1124/dmd.112.050054 · Cited by 259 · see citing works

Applications of minimal physiologically-based pharmacokinetic models

Cao, Y.-G., & Jusko, W. (2012) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-012-9280-2 · Cited by 200 · see citing works

Clearance Prediction Methodology Needs Fundamental Improvement: Trends Common to Rat and Human Hepatocytes/Microsomes and Implications for Experimental Methodology

Wood, F. L., Houston, J. B., & Hallifax, D. (2017) · Drug Metabolism and Disposition · doi:10.1124/dmd.117.077040 · Cited by 158 · see citing works

Meeting the Challenge of Predicting Hepatic Clearance of Compounds Slowly Metabolized by Cytochrome P450 Using a Novel Hepatocyte Model, HepatoPac

Chan, T. S., Yu, H., Moore, A., Khetani, S. R., & Tweedie, D. (2013) · Drug Metabolism and Disposition · doi:10.1124/dmd.113.053397 · Cited by 150 · see citing works

Metabolic stability and its role in the discovery of new chemical entities

Słoczyńska, K., Gunia-Krzyżak, A., Koczurkiewicz, P., Wójcik-Pszczoła, K., Żelaszczyk, D., Popiół, J., & Pękala, E. (2019) · Acta Pharmaceutica · doi:10.2478/acph-2019-0024 · Cited by 130 · see citing works

Special Section on Pharmacokinetic and Drug Metabolism Properties of Novel Therapeutic Modalities–Minireview

Zhang, D., Hop, C. E. C. A., Patilea-Vrana, G., Gampa, G., Seneviratne, H. K., Unadkat, J. D., Kenny, J. R., Nagapudi, K., Di, L., Zhou, L., et al. (2019) · Drug Metabolism and Disposition · doi:10.1124/dmd.119.086744 · Cited by 121 · see citing works

Metabolic Profiling of Human Long-Term Liver Models and Hepatic Clearance Predictions from In Vitro Data Using Nonlinear Mixed-Effects Modeling

Kratochwil, N. A., Meille, C., Fowler, S. M., Klammers, F., Ekiciler, A., Molitor, B., Simon, S., Walter, I., McGinnis, C., Walther, J., et al. (2017) · The AAPS Journal · doi:10.1208/s12248-016-0019-7 · Cited by 111 · see citing works

Content and activity of human liver microsomal protein and prediction of individual hepatic clearance in vivo

Zhang, H.-F., Gao, N., Tian, X., Liu, T., Fang, Y., Zhou, J., Wen, Q., Xu, B., Qi, B., Gao, J., et al. (2015) · Scientific Reports · doi:10.1038/srep17671 · Cited by 110 · see citing works

In vitro to in vivo extrapolation and species response comparisons for drug-induced liver injury (DILI) using DILIsym™: a mechanistic, mathematical model of DILI

Howell, B. A., Yang, Y., Kumar, R., Woodhead, J. L., Harrill, A. H., M.A., H. J. C. I., Andersen, M. E., Siler, S. Q., & Watkins, P. B. (2012) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-012-9266-0 · Cited by 105 · see citing works

Comprehensive Assessment of Human Pharmacokinetic Prediction Based on In Vivo Animal Pharmacokinetic Data, Part 2: Clearance

Lombardo, F., Waters, N. J., Argikar, U. A., Dennehy, M. K., Zhan, J., Gunduz, M., Harriman, S. P., Berellini, G., Liric Rajlic, I., & Obach, R. S. (2013) · The Journal of Clinical Pharmacology · doi:10.1177/0091270012440282 · Cited by 106 · see citing works

An examination of protein binding and protein-facilitated uptake relating to in vitro-in vivo extrapolation

Bowman, C. M., & Benet, L. Z. (2018) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2018.08.008 · Cited by 95 · see citing works

Microengineered cell and tissue systems for drug screening and toxicology applications: Evolution ofin-vitroliver technologies

Usta, O. B., McCarty, W. J., Bale, S. S., Hegde, M., Jindal, R., Bhushan, A., Golberg, I., & Yarmush, M. L. (2015) · TECHNOLOGY · doi:10.1142/s2339547815300012 · Cited by 85 · see citing works

When is Protein Binding Important?*

Heuberger, J. A. A. C., Schmidt, S., & Derendorf, H. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23559 · Cited by 83 · see citing works

Application of In Silico, In Vitro and Preclinical Pharmacokinetic Data for the Effective and Efficient Prediction of Human Pharmacokinetics

Grime, K., Barton, P., & McGinnity, D. F. (2012) · Molecular Pharmaceutics · doi:10.1021/mp300476z · Cited by 78 · see citing works

Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling

Choi, G.-W., Lee, Y.-B., & Cho, H.-Y. (2019) · Pharmaceutics · doi:10.3390/pharmaceutics11040168 · Cited by 76 · see citing works

Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: Influence of time between substrate and inducer administration

Baneyx, G., Parrott, N. J., Meille, C., Iliadis, A., & Lavé, T. (2014) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2014.02.002 · Cited by 77 · see citing works

Profiling antimicrobial peptides from the medical maggot Lucilia sericata as potential antibiotics for MDR Gram-negative bacteria

Hirsch, R., Wiesner, J., Marker, A., Pfeifer, Y., Bauer, A., Hammann, P., & Vilcinskas, A. (2018) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dky386 · Cited by 75 · see citing works

The Role of Extracellular Binding Proteins in the Cellular Uptake of Drugs: Impact on Quantitative In Vitro -to- In Vivo Extrapolations of Toxicity and Efficacy in Physiologically Based Pharmacokinetic-Pharmacodynamic Research

Poulin, P., Burczynski, F. J., & Haddad, S. (2015) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.24571 · Cited by 74 · see citing works

Comparative Assessment of In Vitro–In Vivo Extrapolation Methods used for Predicting Hepatic Metabolic Clearance of Drugs

Poulin, P., Hop, C. E. C. A., Ho, Q., Halladay, J. S., Haddad, S., & Kenny, J. R. (2012) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23288 · Cited by 64 · see citing works

Evaluation of the Success of High-Throughput Physiologically Based Pharmacokinetic (HT-PBPK) Modeling Predictions to Inform Early Drug Discovery

Naga, D., Parrott, N. J., Ecker, G. F., & Olivares‐Morales, A. (2022) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.2c00040 · Cited by 62 · see citing works

Evaluation of Hepatic Clearance Prediction Using In Vitro Data: Emphasis on Fraction Unbound in Plasma and Drug Ionisation Using a Database of 107 Drugs

Hallifax, D., & Houston, J. B. (2012) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23202 · Cited by 60 · see citing works

Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data

Yadav, J., Hassani, M. E., Sodhi, J. K., Lauschke, V. M., Hartman, J. H., & Russell, L. E. (2021) · Drug Metabolism Reviews · doi:10.1080/03602532.2021.1922435 · Cited by 57 · see citing works

Organic Anion Transporter 2–Mediated Hepatic Uptake Contributes to the Clearance of High-Permeability–Low-Molecular-Weight Acid and Zwitterion Drugs: Evaluation Using 25 Drugs

Kimoto, E., Mathialagan, S., Tylaska, L. A., Niosi, M., Lin, J., Carlo, A. A., Tess, D. A., & Varma, M. V. S. (2018) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.118.252049 · Cited by 56 · see citing works

A physiologically based pharmacokinetic model to predict the pharmacokinetics of highly protein‐bound drugs and the impact of errors in plasma protein binding

Ye, M., Nagar, S., & Korzekwa, K. (2015) · Biopharmaceutics & Drug Disposition · doi:10.1002/bdd.1996 · Cited by 54 · see citing works

Toward a new paradigm for the efficient in vitro–in vivo extrapolation of metabolic clearance in humans from hepatocyte data

Poulin, P., & Haddad, S. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23502 · Cited by 54 · see citing works

Predicting Human Clearance of Organic Anion Transporting Polypeptide Substrates Using Cynomolgus Monkey: In Vitro–In Vivo Scaling of Hepatic Uptake Clearance

De Bruyn, T., Ufuk, A., Cantrill, C., Kosa, R. E., Bi, Y.-A., Niosi, M., Modi, S., Rodrigues, A. D., Tremaine, L. M., Varma, M. V. S., et al. (2018) · Drug Metabolism and Disposition · doi:10.1124/dmd.118.081315 · Cited by 53 · see citing works

Cutting Edge PBPK Models and Analyses: Providing the Basis for Future Modeling Efforts and Bridges to Emerging Toxicology Paradigms

Caldwell, J. C., Evans, M. V., & Krishnan, K. (2012) · Journal of Toxicology · doi:10.1155/2012/852384 · Cited by 51 · see citing works

Quantitation of Lysosomal Trapping of Basic Lipophilic Compounds Using In Vitro Assays and In Silico Predictions Based on the Determination of the Full pH Profile of the Endo-/Lysosomal System in Rat Hepatocytes

Schmitt, M. V., Lienau, P., Fricker, G., & Reichel, A. (2018) · Drug Metabolism and Disposition · doi:10.1124/dmd.118.084541 · Cited by 46 · see citing works

Albumin and Uptake of Drugs in Cells: Additional Validation Exercises of a Recently Published Equation that Quantifies the Albumin-Facilitated Uptake Mechanism(s) in Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling Research

Poulin, P., & Haddad, S. (2015) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.24676 · Cited by 45 · see citing works

PredMS: a random forest model for predicting metabolic stability of drug candidates in human liver microsomes

Ryu, J. Y., Lee, J. H., Lee, B. H., Song, J. S., Ahn, S., & Oh, K. (2021) · Bioinformatics · doi:10.1093/bioinformatics/btab547 · Cited by 45 · see citing works

A critical assessment of in vitro tissue models for ADME and drug delivery

Vellonen, K., Malinen, M. M., Mannermaa, E., Subrizi, A., Toropainen, E., Lou, Y., Kidron, H., Yliperttula, M. L., & Urtti, A. O. (2014) · Journal of Controlled Release · doi:10.1016/j.jconrel.2014.06.044 · Cited by 42 · see citing works

An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis

Vugler, A., O’Connell, J. P., Nguyễn, M. Á., Weitz, D., Leeuw, T., Hickford, E. S., Verbitsky, A., Ying, X., Rehberg, M., Carrington, B., et al. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.1037983 · Cited by 41 · see citing works

Meeting the Challenge of Predicting Hepatic Clearance of Compounds Slowly Metabolized by Cytochrome P450 Using a Novel Hepatocyte Model, HepatoPac

Chan, T. S., Yu, H., Moore, A., Khetani, S. R., & Tweedie, D. (2018) · Drug Metabolism and Disposition · doi:10.1124/dmd.113.053397fullarticlecorrection · Cited by 41 · see citing works

Analysis of the impact of controlled release formulations on oral drug absorption, gut wall metabolism and relative bioavailability of CYP3A substrates using a physiologically-based pharmacokinetic model

Olivares‐Morales, A., Kamiyama, Y., Darwich, A. S., Aarons, L. J., & Rostami‐Hodjegan, A. (2014) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2014.10.018 · Cited by 40 · see citing works

Comparison of methods for the prediction of human clearance from hepatocyte intrinsic clearance for a set of reference compounds and an external evaluation set

Yamagata, T., Zanelli, U., Gallemann, D., Perrin, D., Dolgos, H., & Petersson, C. (2016) · Xenobiotica · doi:10.1080/00498254.2016.1222639 · Cited by 37 · see citing works

The potential protein-mediated hepatic uptake: discussion on the molecular interactions between albumin and the hepatocyte cell surface and their implications for the in vitro-to-in vivo extrapolations of hepatic clearance of drugs

Bteich, M., Poulin, P., & Haddad, S. (2019) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2019.1640679 · Cited by 37 · see citing works

Prediction of Total Hepatic Clearance by Combining Metabolism, Transport, and Permeability Data in the In Vitro–In Vivo Extrapolation Methods: Emphasis on an Apparent Fraction Unbound in Liver for Drugs

Poulin, P. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23562 · Cited by 37 · see citing works

A quantitative approach to hepatic clearance prediction of metabolism by aldehyde oxidase using custom pooled hepatocytes

Akabane, T., Gerst, N., Masters, J. N., & Tamura, K. (2012) · Xenobiotica · doi:10.3109/00498254.2012.670736 · Cited by 36 · see citing works

Improving Prediction of Metabolic Clearance Using Quantitative Extrapolation of Results Obtained From Human Hepatic Micropatterned Cocultures Model and by Considering the Impact of Albumin Binding

Da-silva, F., Boulenc, X., Vermet, H., Compigne, P., Gerbal‐Chaloin, S., Daujat‐Chavanieu, M., Klieber, S., & Poulin, P. (2018) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2018.03.001 · Cited by 36 · see citing works

Upcyte Human Hepatocytes: a Potent In Vitro Tool for the Prediction of Hepatic Clearance of Metabolically Stable Compounds

Schaefer, M., Schänzle, G., Bischoff, D., & Süßmuth, R. D. (2015) · Drug Metabolism and Disposition · doi:10.1124/dmd.115.067348 · Cited by 34 · see citing works

A human life-stage physiologically based pharmacokinetic and pharmacodynamic model for chlorpyrifos: Development and validation

Smith, J. N., Hinderliter, P. M., Timchalk, C. A., Bartels, M. J., & Poet, T. S. (2013) · Regulatory Toxicology and Pharmacology · doi:10.1016/j.yrtph.2013.10.005 · Cited by 34 · see citing works

Prediction of Drug Disposition on the Basis of its Chemical Structure

Stepensky, D. (2013) · Clinical Pharmacokinetics · doi:10.1007/s40262-013-0042-0 · Cited by 33 · see citing works

Enzyme-Transporter Interplay in the Formation and Clearance of Abundant Metabolites of Faldaprevir Found in Excreta but not in Circulation

Li, Y., Zhou, J., Ramsden, D., Taub, M., O'Brien, D., Xu, J., Busacca, C. A., Gonnella, N., & Tweedie, D. (2014) · Drug Metabolism And Disposition · doi:10.1124/dmd.113.055863 · Cited by 31 · see citing works

Effect of Human Plasma on Hepatic Uptake of Organic Anion–Transporting Polypeptide 1B Substrates: Studies Using Transfected Cells and Primary Human Hepatocytes

Bi, Y., Ryu, S., Tess, D. A., Rodrigues, A. D., & Varma, M. V. S. (2020) · Drug Metabolism and Disposition · doi:10.1124/dmd.120.000134 · Cited by 30 · see citing works

Consideration of albumin-mediated hepatic uptake for highly protein-bound anionic drugs: Bridging the gap of hepatic uptake clearance between in vitro and in vivo.

Miyauchi, S., Kim, S., Lee, W., & Sugiyama, Y. (2021) · Pharmacology and Therapeutics · doi:10.1016/j.pharmthera.2021.107938 · Cited by 26 · see citing works

In Vitro- in Vivo Extrapolation of Hepatic Metabolism for Different Scenarios - a Toolbox.

Krause, S., & Goss, K. (2018) · Chemical Research in Toxicology · doi:10.1021/acs.chemrestox.8b00187 · Cited by 29 · see citing works

Plasma protein-mediated uptake and contradictions to the free drug hypothesis: a critical review

Schulz, J., Stresser, D. M., & Kalvass, J. C. (2023) · Drug Metabolism Reviews · doi:10.1080/03602532.2023.2195133 · Cited by 31 · see citing works

Can We Predict Clinical Pharmacokinetics of Highly Lipophilic Compounds by Integration of Machine Learning or In Vitro Data into Physiologically Based Models? A Feasibility Study Based on 12 Development Compounds

Parrott, N. J., Manevski, N., & Olivares‐Morales, A. (2022) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.2c00350 · Cited by 29 · see citing works

In Silico Prediction of Human Clinical Pharmacokinetics with ANDROMEDA by Prosilico: Predictions for an Established Benchmarking Data Set, a Modern Small Drug Data Set, and a Comparison with Laboratory Methods

Fagerholm, U., Hellberg, S., Alvarsson, J., & Spjuth, O. (2022) · Alternatives to Laboratory Animals · doi:10.1177/02611929221148447 · Cited by 29 · see citing works

In vitro biotransformation rates in fish liver S9: Effect of dosing techniques

Lee, Y., Lee, D. H. Y., Delafoulhouze, M., Otton, S. V., Moore, M. M., Kennedy, C. J., & Gobas, F. A. P. C. (2014) · Environmental Toxicology and Chemistry · doi:10.1002/etc.2636 · Cited by 29 · see citing works

Extrapolation of the Hepatic Clearance of Drugs in the Absence of Albumin In Vitro to That in the Presence of Albumin In Vivo : Comparative Assessement of 2 Extrapolation Models Based on the Albumin-Mediated Hepatic Uptake Theory and Limitations and Mechanistic Insights

Poulin, P., & Haddad, S. (2018) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2018.03.012 · Cited by 29 · see citing works

Current Approaches for Predicting Human PK for Small Molecule Development Candidates: Findings from the IQ Human PK Prediction Working Group Survey

Petersson, C., Zhou, X., Berghausen, J., Cebrián, D. Á., Davies, M., DeMent, K., Eddershaw, P. J., Riedmaier, A. E., Leblanc, A. F., Manveski, N., et al. (2022) · The AAPS Journal · doi:10.1208/s12248-022-00735-9 · Cited by 28 · see citing works

Hepatocyte Composition-Based Model as a Mechanistic Tool for Predicting the Cell Suspension: Aqueous Phase Partition Coefficient of Drugs in In Vitro Metabolic Studies

Poulin, P., & Haddad, S. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23602 · Cited by 26 · see citing works

A 20-Year Research Overview: Quantitative Prediction of Hepatic Clearance Using the In Vitro-In Vivo Extrapolation Approach Based on Physiologically Based Pharmacokinetic Modeling and Extended Clearance Concept

Sugiyama, Y., & Aoki, Y. (2023) · Drug Metabolism and Disposition · doi:10.1124/dmd.123.001344 · Cited by 25 · see citing works

The Impact of the Hepatocyte-to-Plasma pH Gradient on the Prediction of Hepatic Clearance and Drug-Drug Interactions for CYP2D6 Substrates

Rougée, L. R. A., Mohutsky, M. A., Bedwell, D. W., Ruterbories, K. J., & Hall, S. D. (2016) · Drug Metabolism and Disposition · doi:10.1124/dmd.116.071761 · Cited by 24 · see citing works

Rosuvastatin Liver Partitioning in Cynomolgus Monkeys: Measurement In Vivo and Prediction Using In Vitro Monkey Hepatocyte Uptake

Morse, B. L., Cai, H., MacGuire, J. G., Fox, M., Zhang, L., Zhang, Y., Gu, X., Shen, H., Dierks, E. A., Su, H. L., et al. (2015) · Drug Metabolism and Disposition · doi:10.1124/dmd.115.065946 · Cited by 23 · see citing works

From Genotype to Phenotype: Cytochrome P450 2D6-Mediated Drug Clearance in Humans

Gao, J., Tian, X., Zhou, J., Cui, M., Zhang, H., Gao, N., Wen, Q., & Qiao, H. (2017) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.6b00920 · Cited by 22 · see citing works

Utility of Chimeric Mice with Humanized Liver for Predicting Human Pharmacokinetics in Drug Discovery: Comparison with in Vitro–in Vivo Extrapolation and Allometric Scaling

Naritomi, Y., Sanoh, S., & Ohta, S. (2019) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.b18-00754 · Cited by 22 · see citing works

Use of Segregated Hepatocyte Scaling Factors and Cross-Species Relationships to Resolve Clearance Dependence in the Prediction of Human Hepatic Clearance

Hallifax, D., & Houston, J. B. (2019) · Drug Metabolism and Disposition · doi:10.1124/dmd.118.085191 · Cited by 18 · see citing works

Supplemental Analysis of the Prediction of Hepatic Clearance of Binary Mixtures of Bisphenol A and Naproxen Determined in an Isolated Perfused Rat Liver Model to Promote the Understanding of Potential Albumin-Facilitated Hepatic Uptake Mechanism

Poulin, P., Bteich, M., & Haddad, S. (2017) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2017.07.004 · Cited by 18 · see citing works

In vitro Metabolic Stability of Drugs and Applications of LC-MS in Metabolite Profiling

Krishna, M. V., Padmalatha, K., & Gorrepati, M. (2021) · IntechOpen eBooks · doi:10.5772/intechopen.99762 · Cited by 17 · see citing works

The Impact of the Hepatocyte-to-Plasma pH Gradient on the Prediction of Hepatic Clearance and Drug-Drug Interactions for CYP2C9 and CYP3A4 Substrates

Rougée, L. R. A., Mohutsky, M. A., Bedwell, D. W., Ruterbories, K. J., & Hall, S. D. (2017) · Drug Metabolism and Disposition · doi:10.1124/dmd.117.076331 · Cited by 17 · see citing works

In SilicoModeling for the Prediction of Dose and Pathway-Related Adverse Effects in Humans FromIn VitroRepeated-Dose Studies

Klein, S. G., Maggioni, S., Bucher, J., Mueller, D., Niklas, J., Shevchenko, V., Mauch, K., Heinzle, E., & Noor, F. (2015) · Toxicological Sciences · doi:10.1093/toxsci/kfv218 · Cited by 17 · see citing works

The Influence of Old Age and Poloxamer-407 on the Hepatic Disposition of Diazepam in the Isolated Perfused Rat Liver

Mitchell, S. J., Huizer‐Pajkos, A., Cogger, V. C., McLachlan, A. J., Couteur, D. G. L., Jones, B., de Cabo, R., & Hilmer, S. N. (2012) · Pharmacology · doi:10.1159/000341724 · Cited by 15 · see citing works

Specific Inhibition of the Distribution of Lobeglitazone to the Liver by Atorvastatin in Rats: Evidence for a Rat Organic Anion Transporting Polypeptide 1B2–Mediated Interaction in Hepatic Transport

Yim, C.-S., Jeong, Y., Lee, S.-Y., Pyeon, W., Ryu, H.-M., Lee, J., Lee, K., Maeng, H., & Chung, S. (2017) · Drug Metabolism and Disposition · doi:10.1124/dmd.116.074120 · Cited by 15 · see citing works

In vitro metabolism of the lignan (−)‐grandisin, an anticancer drug candidate, by human liver microsomes

Barth, T., Habenschus, M. D., Moreira, F. D. L., Ferreira, L. D. S., Lopes, N. P., & de Oliveira, A. R. M. (2015) · Drug Testing and Analysis · doi:10.1002/dta.1743 · Cited by 13 · see citing works

Comparative Assessment of Extrapolation Methods Based on the Conventional Free Drug Hypothesis and Plasma Protein-Mediated Hepatic Uptake Theory for the Hepatic Clearance Predictions of Two Drugs Extensively Bound to Both the Albumin And Alpha-1-Acid Glycoprotein

Bteich, M., Poulin, P., & Haddad, S. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.11.009 · Cited by 13 · see citing works

In Vitro–In Vivo Extrapolation of Hepatic Biotransformation Data for Fish. III. An In-depth Case Study with Pyrene

Nichols, J. W., Fitzsimmons, P. N., Hoffman, A. D., & Wong, K. (2023) · Environmental Toxicology and Chemistry · doi:10.1002/etc.5626 · Cited by 12 · see citing works

Successful Prediction of Human Pharmacokinetics After Oral Administration by Optimized Physiologically Based Pharmacokinetics Approach and Permeation Assay Using Human Induced Pluripotent Stem Cell–Derived Intestinal Epithelial Cells

Mayumi, K., Akazawa, T., Kanazu, T., Ohnishi, S., & Hasegawa, H. (2019) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2019.12.019 · Cited by 12 · see citing works

Successful Prediction of Human Pharmacokinetics by Improving Calculation Processes of Physiologically Based Pharmacokinetic Approach.

Mayumi, K., Ohnishi, S., & Hasegawa, H. (2019) · Journal of Pharmacy and Science · doi:10.1016/j.xphs.2019.03.002 · Cited by 10 · see citing works

Studies on Diketopiperazine and Dipeptide Analogs as Opioid Receptor Ligands

Nia, S. S., Hossain, M. A., Ji, G., Jonnalagadda, S. K., Obeng, S., Rahman, M. A., Sifat, A. E., Nozohouri, S., Blackwell, C., Patel, D., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115309 · Cited by 10 · see citing works

Suitable albumin concentrations for enhanced drug oxidation activities mediated by human liver microsomal cytochrome P450 2C9 and other forms predicted with unbound fractions and partition/distribution coefficients of model substrates

Shimura, K., Murayama, N., Tanaka, S., Onozeki, S., & Yamazaki, H. (2018) · Xenobiotica · doi:10.1080/00498254.2018.1482576 · Cited by 9 · see citing works

Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-incubation, and Continuous Fluorometric Kinetic Analyses

Caldwell, G. W., & Yan, Z. (2013) · Methods in pharmacology and toxicology · doi:10.1007/978-1-62703-742-6_17 · Cited by 8 · see citing works

Prediction of the effect of voriconazole on the pharmacokinetics of non-steroidal anti-inflammatory drugs

Li, N., Zhu, L., Qi, F., Li, M., Xu, G., & Ge, T. (2018) · Journal of Chemotherapy · doi:10.1080/1120009x.2018.1500197 · Cited by 8 · see citing works

Drug Design and Success of Prospective Mouse In Vitro–In Vivo Extrapolation (IVIVE) for Predictions of Plasma Clearance (CLp) from Hepatocyte Intrinsic Clearance (CLint)

Manevski, N., Umehara, K., & Parrott, N. J. (2023) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.2c01001 · Cited by 7 · see citing works

Hepatic transporter‐mediated pharmacokinetic drug–drug interactions: Recent studies and regulatory recommendations

Izat, N., & Şahin, S. (2021) · Biopharmaceutics & Drug Disposition · doi:10.1002/bdd.2262 · Cited by 7 · see citing works

Impact of Extensive Plasma Protein Binding on the In Situ Hepatic Uptake and Clearance of Perampanel and Fluoxetine in Sprague Dawley Rats

Bteich, M., Poulin, P., Piette, S., & Haddad, S. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.07.003 · Cited by 7 · see citing works

Translational PK/PD Modeling of Tumor Growth Inhibition and Target Inhibition to Support Dose Range Selection of the LMP7 Inhibitor M3258 in Relapsed/Refractory Multiple Myeloma

Lignet, F., Esdar, C., Walter-Bausch, G., Friese‐Hamim, M., Stinchi, S., Drouin, E. E., Bawab, S. E., Becker, A. D., Gimmi, C. D., Sanderson, M. P., et al. (2022) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.122.001355 · Cited by 6 · see citing works

Stereoselectivity in Pharmacokinetics of Rivoglitazone, A Novel Peroxisome Proliferator-Activated Receptor γ Agonist, in Rats and Monkeys: Model-Based Pharmacokinetic Analysis and In Vitro-In Vivo Extrapolation Approach

Izumi, T., Tsuruta, F., Ishizuka, T., Nakamura, K., Kothuma, M., & Makoto, T. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23586 · Cited by 6 · see citing works

Improved Human Pharmacokinetic Prediction of Hepatically Metabolized Drugs With Species-Specific Systemic Clearance

Horiuchi, K., Ohnishi, S., Matsuzaki, T., Funaki, S., Watanabe, A., Mizutare, T., Matsumoto, S., Nezasa, K., & Hasegawa, H. (2018) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2017.12.027 · Cited by 6 · see citing works

Biological Profiling of Coleoptericins and Coleoptericin-Like Antimicrobial Peptides from the Invasive Harlequin Ladybird Harmonia axyridis

Hirsch, R., Wiesner, J., Marker, A., Bauer, A., Hammann, P., & Vilcinskas, A. (2018) · Advances in experimental medicine and biology · doi:10.1007/5584_2018_276 · Cited by 6 · see citing works

Evidence of the Need for Modified Well-stirred Model in In Vitro to In Vivo Extrapolation.

Chang, T.-Y., Wang, H.-J., Hsu, S.-H., Chang, M., Kao, L., & Pao, L.-H. (2022) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2022.106268 · Cited by 5 · see citing works

Assumptions Underlying Hepatic Clearance Models: Recognizing the Influence of Saturable Protein Binding on Driving Force Concentration and Discrimination Between Models of Hepatic Clearance

Pauly, J. A. S., Wang, J., Phipps, C. J., & Kalvass, J. (2023) · Drug Metabolism And Disposition · doi:10.1124/dmd.123.001326 · Cited by 4 · see citing works

Predicting Transport of 3,5,6-Trichloro-2-Pyridinol Into Saliva Using a Combination Experimental and Computational Approach

Smith, J. N., Carver, Z. A., Weber, T. J., & Timchalk, C. A. (2017) · Toxicological Sciences · doi:10.1093/toxsci/kfx055 · Cited by 5 · see citing works

Physiologically Based Pharmacokinetic Modeling of Chemical Mixtures

Haddad, S. (2018) · Springer eBooks · doi:10.1007/978-3-319-56234-6_12 · Cited by 4 · see citing works

A myth of the well-stirred model: Is the well-stirred model good for high clearance drugs?

Dong, J., & Park, M. S. (2022) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2022.106134 · Cited by 4 · see citing works

A Novel Experimental and Theoretical Method for Estimating Albumin-Mediated Hepatic Uptake Based on the Albumin Binding Fraction in Plasma and Human PK Prediction Using a Physiologically-Based Pharmacokinetic Approach

Egashira, Y., Shimada, T., & Mayumi, K. (2021) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2021.01.015 · Cited by 4 · see citing works

Determination of Intrinsic Clearance and Fraction Unbound in Human Liver Microsomes and In Vitro-In Vivo Extrapolation of Human Hepatic Clearance for Marketed Central Nervous System Drugs

Palacharla, V. R. C., Nirogi, R., Kumar, N., & Nandakumar, K. (2024) · European journal of drug metabolism and pharmacokinetics · doi:10.1007/s13318-024-00931-2 · Cited by 3 · see citing works

The role of drug metabolism in drug discovery and development : case ospemifene

Uusitalo, J. (2015) · Cited by 2 · see citing works

Toward improved clearance predictions and distribution profiles employing the isolated perfused rat liver model: Experimental optimization

Heylen, S., Nicolaï, J., Asten, S. V., Tuytelaars, A., Wagter, K. D., Snoeys, J., Evers, R., Kourula, S., & Annaert, P. (2025) · Drug Metabolism and Disposition · doi:10.1016/j.dmd.2025.100045 · Cited by 2 · see citing works

Prediction of hepatic plasma clearance in vivo from gel-entrapped rat and human hepatocytes

Yin, J. B., Qiu, H., Dai, J., Lü, Y., Zhao, R., Chen, L., & Meng, Q. (2012) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/cjpp-2012-0334 · Cited by 2 · see citing works

SYSTEM-DEPENDENT METABOLISM OF DRUGS BY CYTOCHROME P450: THE MECHANISTIC BASIS FOR WHY HUMAN LIVER MICROSOMES ARE SUPERIOR TO HUMAN HEPATOCYTES AT METABOLIZING MIDAZOLAM BUT INFERIOR AT METABOLIZING DESLORATADINE

Kazmi, F. (2015) · KU ScholarWorks (University of Kansas) · Cited by 2 · see citing works

3D Hepatocyte Model with Composite Nanofibers That Reproduced Human In Vivo Drug Clearance Profiles

Park, R., & Chen, C. (2025) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.5c00149 · Cited by 1 · see citing works

Lipid-Based Drug Delivery Systems: Formulation and Applications

Yadav, P. (2025) · Methods in pharmacology and toxicology · doi:10.1007/978-1-0716-4554-3_5 · Cited by 1 · see citing works

Special Section on Prediction of Human Pharmacokinetic Parameters from In Vitro Systems Meeting the Challenge of Predicting Hepatic Clearance of Compounds Slowly Metabolized by Cytochrome P450 Using a Novel Hepatocyte Model, HepatoPac

Chan, T. S., Yu, H., Moore, A., Khetani, S. R., & Tweedie, D. (2013) · Cited by 1 · see citing works

State of the Science: Biologically Based Modeling in Risk Assessment

Caldwell, J., Krishnan, K., & Evans, M. (2012) · Journal of Toxicology · doi:10.1155/2012/758182

Avaliação de técnicas miniaturizadas de preparação de amostras em estudos estereosseletivos de biotransformação e metabolismo in vitro

Bocato, M. Z. (2017) · doi:10.11606/t.60.2017.tde-01112016-104713

Estudo in vitro do perfil metabólico do agente antitumoral piplartina frente às enzimas do citocromo P450 e predição de parâmetros farmacocinéticos

Moreira, F. D. L. (2017) · doi:10.11606/t.60.2017.tde-03052017-153134

In vitro-in vivo extrapolation of human hepatic and renal clearance

Alluri, R. V., & Varma, M. V. S. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-820018-6.00022-3

Comparative Assessment of In Vitro–In Vivo Extrapolation Methods used for Predicting Hepatic Metabolic Clearance of Drugs

Poulin, P., Hop, C. E. C. A., Ho, Q., Halladay, J. S., Haddad, S., & Kenny, J. R. (2012) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23288 · Cited by 64 · see citing works

Toward a new paradigm for the efficient in vitro–in vivo extrapolation of metabolic clearance in humans from hepatocyte data

Poulin, P., & Haddad, S. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23502 · Cited by 54 · see citing works

Prediction of Total Hepatic Clearance by Combining Metabolism, Transport, and Permeability Data in the In Vitro–In Vivo Extrapolation Methods: Emphasis on an Apparent Fraction Unbound in Liver for Drugs

Poulin, P. (2013) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.23562 · Cited by 37 · see citing works

Investigating the Theoretical Basis for In Vitro–In Vivo Extrapolation (IVIVE) in Predicting Drug Metabolic Clearance and Proposing Future Experimental Pathways

Benet, L. Z., & Sodhi, J. K. (2020) · The AAPS Journal · doi:10.1208/s12248-020-00501-9 · Cited by 36 · see citing works

A New Guidance for the Prediction of Hepatic Clearance in the Early Drug Discovery and Development from the in Vitro-to-in Vivo Extrapolation Method and an Approach for Exploring Whether an Albumin-Mediated Hepatic Uptake Phenomenon Could be Present Under in Vivo Conditions

Poulin, P., & Haddad, S. (2021) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2021.04.002 · Cited by 14 · see citing works