1 Rowland, M, Tozer, TN. Clinical Pharmacokinetics: Concepts and Applications
. Philadeliphia, PA: Lea %26 Febiger
2 Shargel, L, Yu, A. Applied Biopharmaceutics and Pharmacokinetics
. New York: McGraw‐Hill
3 Paalzow, LK. Torsten Teorell, the father of pharmacokinetics. Ups Med J 1995, 100:41–46.
4 Hall, SD, Thummel, KE, Watkins, PB, Lown, KS, Benet, LZ, Paine, MF, Mayo, RR, Turgeon, DK, Bailey, DG, Fontana, RJ, et al. Molecular and physical mechanisms of first‐pass extraction. Drug Metab Dispos 2002, 27: 161–166.
5 Kararli, TT. Gastrointestinal absorption of drugs. Ther Drug Carrier Syst 1989, 6:39–86.
6 Amidon, GE, Lennernas, H, Shan, VP, Crison, JR. A theoretical basis for a biopharmaceutical classification system: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995, 12: 413–420.
7 Himmelstein, KJ, Lutz, RJ. A review of the applications of physiologically based pharmacokinetic modeling. J Pharmacokinet Biopharm 1979, 7:127–145.
8 Oie, S, Tozer, TN. Effect of altered plasma protein binding on apparent volume of distribution. J Pharm Sci 1979, 68:1203–1205.
9 Tse, FLS, Ballard, F, Skinn, J. Estimating the fraction reabsorbed in drugs undergoing enterohepatic recycling. J Pharmacokinet Biopharm 1982, 10:455–461.
10 Berezhkovsky, LM. On the influence of protein binding on pharmacological activity of drugs. J Pharm Sci 2010, 99:2153–2165.
11 Zini, R, Riant, P, Barre, J, Tillement, JP. Disease‐induced variations in plasma protein levels: implications for drug dosage regimens (part 1). Clin Pharmacokinet 1990, 19:147–159.
12 Aggeler, PM, O`Reilly, RA, Leong, L, Kowitz, PE. Potentiation of anticoagulant effect of warfarin by phenylbutazone. New Engl J Med 1967, 276:496–501.
13 Benet, LZ, Hoener, B‐A. Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 2002, 71:115–121.
14 Testa, B, Kramer, S. The Biochemistry of Drug Metabolism: Principles, Redox Reactions, and Hydrolyses
. New York: John Wiley %26 Sons, Inc
15 Lin, JH, Lu, AYH. Role of pharmacokinetics and metabolism in drug discovery and development. Pharmacol Rev 1997, 49:403–449.
16 Jann, MW, Lam, YWF, Gray, EC, Chang, W‐H. Reversible metabolism of drugs. Drug Metabol Drug Interact 1994, 11:1–24.
17 Atkinson, AJ, Stec, GP, Lertora, JJL, Ruo, TI, Thenot, JP. Impact of active metabolites on monitoring plasma concentrations of therapeutic drugs. Ther Drug Monit 2010, 2:19–27.
18 Bonate, PL, Arthaud, L, Stuhler, J, Yerino, P, Press, RJ, Rose, JQ. The distribution, metabolism, and elimination of clofarabine in rats. Drug Metab Dispos 2005, 33: 739–748.
19 Bonate, PL, Cunningham, C, Gaynon, P, Jeha, S, Lam, GN, Razzouk, B, Steinherz, P, Weitman, S. Population pharmacokinetics of clofarabine and its metabolite, 6‐keto‐clofarabine, in adult and pediatric patients with cancer. Cancer Chemother Pharmacol (epub; June 26, 2010).
20 International Transporter Consortium, Giacomini, KM, Huang, S‐M, Tweedie, D, Benet, LZ, Brouwer, X Chu, A, Dhalin, R, Evers, V, Fischer, KM, et al. Membrane transporters in drug development. Nat Rev Drug Dis 2010, 9: 215–236.
21 Lin, JH. How significant is the role of p‐glycoprotein in drug absorption and brain uptake? Drugs Today 2004, 40:5–22.
22 Wilkinson, GR, Shand, DG. A physiological approach to hepatic drug clearance. Clin Pharmacol Therap 1975, 18:377–390.
23 Bekersky, I. Renal excretion. J Clin Pharmacol 1987, 27:447–449.
24 Rowland, M, Benet, LZ, Graham, GG. Clearance concepts in pharmacokinetics. J Pharmacokinet Biopharm 1973, 1:123–136.
25 Gibaldi, M, Levy, G, Weintraub, H. Drug distribution and pharmacologic effects. Clin Pharmacol Therap 1971, 12:734–742.
26 United States Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, and Center for Biologics Evaluation and Research. Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products ‐ General Considerations; 2000.
27 Muir, KT, Gomeni, R. %22Non‐compartmental analysis.%22 In: Bonate, PL, Howard, DR, eds. Pharmacokinetics in Drug Development: Clinical Study Design and Analysis
. Arlington, VA: AAPS Press
; 2004, 235–265.
28 Pharsight Corporation
. WinNonlin Reference Guide, Version 3.2
. Mountain View, CA: Pharsight Corporation
29 Purves, RD. Optimum numerical integration methods for area‐under‐the‐curve (AUC) and area‐under‐the‐moment‐curve (AUMC). J Pharmacokinet Biopharm 1992, 20:211–226.
30 Gough, K, Hutchison, M, Keene, O, Byrom, B, Ellis, S, Lacey, L, McKellar, J. Assessment of dose proportionality: report from the Statisticians in the Pharmaceutical Industry/Pharmacokinetics UK Joint Working Party. Drug Inf J 1995, 29:1039–1048.
31 Lacey, LF, O`Keene, ON, Pritchard, JF, Bye, A. Common noncompartmental pharmacokinetic variables: are they normally and log‐normally distributed? J Biopharm Stat 1997, 7:171–178.
32 Cobelli, C, Foster, DM. Compartmental models: theory and practice using the SAAM II software system. Adv Exp Med Biol 1998, 445:79–101.
33 Zierler, K. A critique of compartmental analysis. Ann Rev Biophys Bioeng 1981, 10:531–562.
34 Sheiner, LB, Beal, SL. Evaluation of methods for estimating population pharmacokinetics parameters. I. Michaelis‐Menten model: routine clinical pharmacokinetic data. J Pharmacokinet Biopharm 1980, 8: 553–571.
35 Sheiner, LB, Beal, SL. Evaluation of methods for estimating population pharmacokinetic parameters. II. Biexponential model and experimental pharmacokinetic data. J Pharmacokinet Biopharm 1981, 9:635–651.
36 Sheiner, LB, Beal, SL. Evaluation of methods for estimating population pharmacokinetic parameters. III. Monoexponential model: routine clinical pharmacokinetic data. J Pharmacokinet Biopharm 1983, 11:303–319.
37 Boeckmann, AJ, Sheiner, LB, Beal, SL. NONMEM Users Guide (1989
. Ellicott City, MD: ICON Development Solutions
38 Bonate, PL. %22Pharmacokinetic‐Pharmacodynamic Modeling and Simulation%22. New York: Springer
39 Holford, NHG, Kimko, HC, Monteleone, JPR, Peck, CC. Simulation of clinical trials. Ann Rev Pharmacol Toxicol 2000, 40:209–234.
40 Kimko, HC, Reele, SSB, Holford, NHG, Peck, CC. Prediction of the outcome of a phase 3 clinical trial of an antipsychotic agent (quetiapine fumarate) by simulation with a population pharmacokinetic and pharmacodynamic model. Clin Pharmacol Ther 2000, 68:568–577.
41 Kimko, HC, Duffull, SB, eds. Simulation for Designing Clinical Trials: A Pharmacokinetic‐Pharmacodynamic Modeling Perspective. New York: Marcel Dekker
42 Lalonde, R, Kowalski, KG, Hutmacher, MM, Ewy, W, Nichols, DJ, Milligan, PA, Corrigan, BW, Lockwood, PA, Marshall, SA, Benincosa, LJ, et al. Model‐based drug development. Clin Pharmacol Ther 2007, 82:21–32.
43 Sheiner, LB, Steimer, JL. Pharmacokinetic/ pharmacodynamic modeling in drug development. Ann Rev Pharmacol Toxicol 2000, 40:67–95.
44 Holford, NHG, Sheiner, LB. Understanding the dose‐effect relationship: clinical application of of pharmacokinetic‐pharmacodynamic models. Clin Pharmacokinet 1981, 6:429–453.
45 Jusko, WJ, Ko, HC. Physiologic indirect response models characterize diverse types of pharmacodynamic effects. Clin Pharmacol Ther 1994, 56:406–419.
46 Mager, DE, Wyska, E, Jusko, WJ. Diversity of mechanism‐based pharmacodynamic models. Drug Metab Dispos 2003, 31:510–519.
47 Bonate, PL, Craig, A, Gaynon, P, Gandhi, V, Jeha, S, Kadota, R, Lam, GN, Plunkett, W, Razzouk, B, Rytting, M, et al. Population pharmacokinetics of clofarabine, a second‐generation nucleoside analog, in pediatric patients with acute leukemia. J Clin Pharmacol 2004, 44:1309–1322.
48 Gobburu, JVS, Lesko, LJ. Quantitative disease, drug, and trial models. Ann Rev Pharmacol Toxicol 2008, 49:291–301.
49 McDonald, CJ, Mazzuca, SA, McCabe, GP. How much of the placebo ‘effect’ is really statistical regression? Stat Med 1983, 2:417–427.
50 Bhattaram, AV, Siddiqui, O, Kapcala, LP, Gobburu, JVS. Endpoints and analyses to discern disease‐modifying drug‐effects in early Parkinson`s disease. AAPS J 2009, 11:456–464.
51 Wang, Y, Sung, C, Dartois, C, Ramchandani, R, Booth, BP, Rock, E, Gobburu, J. Elucidation of relationship between tumor size and survival in non‐small‐cell lung cancer patients can aid early decision making in clinical drug development. Clin Pharmacol Ther 2009, 86:167–174.
52 Mathijssen, RHJ, van Alphen, RJ, Verweij, J, Loos, WJ, Nooter, K, Stoter, G, Sparreboom, A. Clinical pharmacokinetics and metabolism of irinotecan (CPT‐11). Clin Cancer Res 2001, 7:2182–2194.
53 Xie, R, Mathijssen, RHJ, Sparreboom, A, Verweij, J, Karlsson, MO. Clinical pharmacokinetics of irinotecan its metabolite in relation with diarrhea. Clin Pharmacol Ther 2002, 72:265–272.
54 O`Dwyer, PJ, Catalano, RB. Uridine diphosphate glucuronyltransferase (UGT) 1A1 and irinotecan: practical pharmacogenomics arrives in cancer therapy. J Clin Oncol 2006, 28:4534–4538.
55 United States Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, and Center for Biologics Evaluation and Research. Guidance for Industry: Pharmacokinetics in Patients with Impaired Renal Function ‐ Study Design, Data Analysis, and Impact on Dosing and Labeling; 1998.
56 United States Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, and Center for Biologics Evaluation and Research. Guidance for Industry: Pharmacokinetics in Patients with Impaired Hepatic Function: Study Design, Data Analysis, and Impact on Labelling; 2003.
57 United States Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, and Center for Biologics Evaluation and Research. Guidance for Industry: Guideline for the Study of Drugs Likely to be Used in the Elderly; 1989.
58 Kimko, HC, Peck, CC. Clinical trial simulations: applications and trends. New York: Springer; 2011.