Effect of ritonavir on 99mtechnetium-mebrofenin disposition in humans: A semi-pbpk modeling and in vitro approach to predict transporter-mediated DDIs

CPT: Pharmacometrics and Systems Pharmacology

Volumn 2, Issue 1, 2013, Pages

  Pfeifer, N D ^a   Goss, S L ^a   Swift, B ^a   Ghibellini, G ^a   Ivanovic, M ^b   Heizer, W D ^c   Gangarosa, L M ^c   Brouwer, K L R ^a  

^a University of North Carolina   (United States)

^b UNIVERSITY OF NORTH CAROLINA HOSPITALS   (United States)

^c UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

MEBROFENIN TC 99M; RITONAVIR;

ARTICLE; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG EFFECT; DRUG EXPOSURE; DRUG UPTAKE; HEPATOBILIARY RADIOGRAPHY; HUMAN; IN VITRO STUDY; LIVER CELL; NORMAL HUMAN; PRIORITY JOURNAL; SENSITIVITY ANALYSIS; SIMULATION;

EID: 84879412321     PISSN: None     EISSN: 21638306     Source Type: Journal    
DOI: 10.1038/psp.2012.21     Document Type: Article

References (50)

1. US Food and Drug Administration. Draft Guidance for Industry: Drug Interaction Studies, Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations. (US Department of Health and Human Services, FDA, Center for Drug Use and Evaluation (CDER), Silver Spring, MD, 2012).
2. European Medical Agency. Guideline on the Investigation of Drug Interactions. (Committee for Human Medicinal Products (CHMP), London, UK, 2012).
3. Funk, C. The role of hepatic transporters in drug elimination. Expert Opin. Drug Metab. Toxicol. 4, 363-379 (2008). (Pubitemid 351728512)
4. Pauli-Magnus, C. & Meier, P.J. Hepatobiliary transporters and drug-induced cholestasis. Hepatology 44, 778-787 (2006). (Pubitemid 46489540)
5. Hendrikse, N.H., Franssen, E.J., van der Graaf, W.T., Vaalburg, W. & de Vries, E.G.Visualization of multidrug resistance in vivo. Eur. J. Nucl. Med. 26, 283-293 (1999). (Pubitemid 29139861)
6. Michael, M. et al. Relationship of hepatic functional imaging to irinotecan pharmacokinetics and genetic parameters of drug elimination. J. Clin. Oncol. 24, 4228-4235 (2006). (Pubitemid 46630779)
7. Wong, M. et al. Predictors of vinorelbine pharmacokinetics and pharmacodynamics in patients with cancer. J. Clin. Oncol. 24, 2448-2455 (2006). (Pubitemid 46630621)
8. Chen, C.C. et al. Detection of in vivo P-glycoprotein inhibition by PSC 833 using Tc-99m sestamibi. Clin. Cancer Res. 3, 545-552 (1997). (Pubitemid 27211831)
9. Ghibellini, G., Leslie, E.M., Pollack, G.M. & Brouwer, K.L.R. Use of tc-99m mebrofenin as a clinical probe to assess altered hepatobiliary transport: integration of in vitro, pharmacokinetic modeling, and simulation studies. Pharm. Res. 25, 1851-1860 (2008).
10. Ghibellini, G., Johnson, B.M., Kowalsky, R.J., Heizer, W.D. & Brouwer, K.L.R. A novel method for the determination of biliary clearance in humans. AAPS J. 6, e33 (2004).
11. Giacomini, K.M. et al. Membrane transporters in drug development. Nat Rev Drug Discov 9, 215-236 (2010).
12. Swift, B., Pfeifer, N.D. & Brouwer, K.L.R. Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metab. Rev. 42, 446-471 (2010).
13. Balon, H.R. et al. Procedure guideline for hepatobiliary scintigraphy. Society of Nuclear Medicine. J. Nucl. Med. 38, 1654-1657 (1997). (Pubitemid 27443973)
14. Doo, E., Krishnamurthy, G.T., Eklem, M.J., Gilbert, S. & Brown, P.H. Quantification of hepatobiliary function as an integral part of imaging with technetium-99m-mebrofenin in health and disease. J. Nucl. Med. 32, 48-57 (1991).
15. Loberg, M.D., Cooper, M., Harvey, E., Callery, P. & Faith, W. Development of new radiopharmaceuticals based on N-substitution of iminodiacetic acid. J. Nucl. Med. 17, 633-638 (1976).
16. Swift, B., Yue, W. & Brouwer, K.L.R. Evaluation of (99m)technetium-mebrofenin and (99m) technetium-sestamibi as specific probes for hepatic transport protein function in rat and human hepatocytes. Pharm. Res. 27, 1987-1998 (2010).
17. de Graaf, W. et al. Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J. Hepatol. 54, 738-745 (2011).
18. Bhargava, K.K. et al. Adenosine triphosphate-binding cassette subfamily C member 2 is the major transporter of the hepatobiliary imaging agent (99m)Tc-mebrofenin. J. Nucl. Med. 50, 1140-1146 (2009).
19. Pinós, T., Figueras, C. & Herranz, R. Scintigraphic diagnosis of Dubin-Johnson syndrome: DISIDA is also useful. Am. J. Gastroenterol. 86, 1687-1688 (1991).
20. Hendrikse, N.H. et al. In vivo imaging of hepatobiliary transport function mediated by multidrug resistance associated protein and P-glycoprotein. Cancer Chemother. Pharmacol. 54, 131-138 (2004). (Pubitemid 39044242)
21. Pinós, T., Constansa, J.M., Palacin, A. & Figueras, C. A new diagnostic approach to the Dubin-Johnson syndrome. Am. J. Gastroenterol. 85, 91-93 (1990). (Pubitemid 20038990)
22. Hirsch, M.S. Initiating therapy: when to start, what to use. J. Infect. Dis. 197 (suppl. 3), S252-S260 (2008). (Pubitemid 351717316)
23. Vourvahis, M. & Kashuba, A.D. Mechanisms of pharmacokinetic and pharmacodynamic drug interactions associated with ritonavir-enhanced tipranavir. Pharmacotherapy 27, 888-909 (2007). (Pubitemid 46849432)
24. Huisman, M.T. et al. Multidrug resistance protein 2 (MRP2) transports HIV protease inhibitors, and transport can be enhanced by other drugs. AIDS 16, 2295-2301 (2002). (Pubitemid 35449015)
25. Ye, Z.W., Camus, S., Augustijns, P. & Annaert, P. Interaction of eight HIV protease inhibitors with the canalicular efflux transporter ABCC2 (MRP2) in sandwich-cultured rat and human hepatocytes. Biopharm. Drug Dispos. 31, 178-188 (2010).
26. Gutmann, H., Fricker, G., Drewe, J., Toeroek, M. & Miller, D.S. Interactions of HIV protease inhibitors with ATP-dependent drug export proteins. Mol. Pharmacol. 56, 383-389 (1999). (Pubitemid 29347615)
27. Ye, Z.W., Augustijns, P. & Annaert, P. Cellular accumulation of cholyl-glycylamido-fluorescein in sandwich-cultured rat hepatocytes: kinetic characterization, transport mechanisms, and effect of human immunodeficiency virus protease inhibitors. Drug Metab. Dispos. 36, 1315-1321 (2008). (Pubitemid 351929316)
28. Annaert, P., Ye, Z.W., Stieger, B. & Augustijns, P. Interaction of HIV protease inhibitors with OATP1B1, 1B3, and 2B1. Xenobiotica. 40, 163-176 (2010).
29. Krishnamurthy, S. & Krishnamurthy, G.T. Technetium-99m-iminodiacetic acid organic anions: review of biokinetics and clinical application in hepatology. Hepatology 9, 139-153 (1989). (Pubitemid 19046316)
30. Lee, J.K., Brouwer, K.R. Determination of intracellular volume of rat and human sandwichcultured hepatocytes (Abstract ID 1595). The Toxicologist, Supplement to Toxicological Sciences 114, 339 (2010).
31. Chervu, L.R., Nunn, A.D. & Loberg, M.D. Radiopharmaceuticals for hepatobiliary imaging. Semin. Nucl. Med. 12, 5-17 (1982).
32. Hawkins, R.A. et al. Radionuclide evaluation of liver transplants. Semin. Nucl. Med. 18, 199-212 (1988).
33. Brown, P.H., Juni, J.E., Lieberman, D.A. & Krishnamurthy, G.T. Hepatocyte versus biliary disease: a distinction by deconvolutional analysis of technetium-99m IDA time-activity curves. J. Nucl. Med. 29, 623-630 (1988).
34. Peters, A.M., Myers, M.J., Mohammadtaghi, S., Mubashar, M. & Mathie, R.T. Bidirectional transport of iminodiacetic organic anion analogues between plasma and hepatocyte. Eur. J. Nucl. Med. 25, 766-773 (1998). (Pubitemid 28377041)
35. Ito, K. et al. Which concentration of the inhibitor should be used to predict in vivo drug interactions from in vitro data? AAPS PharmSci 4, E25 (2002).
36. van Heeswijk, R.P. et al. Time-dependent interaction between lopinavir/ritonavir and fexofenadine. J. Clin. Pharmacol. 46, 758-767 (2006). (Pubitemid 43882799)
37. Jones, H.M. et al. Mechanistic pharmacokinetic modeling for the prediction of transportermediated disposition in humans from sandwich culture human hepatocyte data. Drug Metab. Dispos. 40, 1007-1017 (2012).
38. Ménochet, K., Kenworthy, K.E., Houston, J.B. & Galetin, A. Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes. Drug Metab. Dispos. 40, 1744-1756 (2012).
39. Abe, K., Bridges, A.S., Yue, W. & Brouwer, K.L.R. In vitro biliary clearance of angiotensin II receptor blockers and 3-hydroxy-3-methylglutaryl- coenzyme A reductase inhibitors in sandwich-cultured rat hepatocytes: comparison with in vivo biliary clearance. J. Pharmacol. Exp. Ther. 326, 983-990 (2008).
40. Higgins, J.W., Bedwell, D.W. & Zamek-Gliszczynski, M.J. Ablation of both organic cation transporter (OCT)1 and OCT2 alters metformin pharmacokinetics but has no effect on tissue drug exposure and pharmacodynamics. Drug Metab. Dispos. 40, 1170-1177 (2012).
41. Watanabe, T., Kusuhara, H., Maeda, K., Shitara, Y. & Sugiyama, Y. Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J. Pharmacol. Exp. Ther. 328, 652-662 (2009).
42. Poirier, A., Funk, C., Scherrmann, J.M. & Lavé, T. Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine. Mol. Pharm. 6, 1716-1733 (2009).
43. Jones, H.M., Parrott, N., Jorga, K. & Lavé, T. A novel strategy for physiologically based predictions of human pharmacokinetics. Clin. Pharmacokinet. 45, 511-542 (2006).
44. Kawai, R., Mathew, D., Tanaka, C. & Rowland, M. Physiologically based pharmacokinetics of cyclosporine A: extension to tissue distribution kinetics in rats and scale-up to human. J. Pharmacol. Exp. Ther. 287, 457-468 (1998). (Pubitemid 29133641)
45. Takeda, M. et al. Evidence for a role of human organic anion transporters in the muscular side effects of HMG-CoA reductase inhibitors. Eur. J. Pharmacol. 483, 133-138 (2004). (Pubitemid 38068393)
46. Knauer, M.J. et al. Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ. Res. 106, 297-306 (2010).
47. Rezk, N.L., Crutchley, R.D., Yeh, R.F. & Kashuba, A.D. Full validation of an analytical method for the HIV-protease inhibitor atazanavir in combination with 8 other antiretroviral agents and its applicability to therapeutic drug monitoring. Ther. Drug Monit. 28, 517-525 (2006). (Pubitemid 44181485)
48. Jung, B.H., Rezk, N.L., Bridges, A.S., Corbett, A.H. & Kashuba, A.D. Simultaneous determination of 17 antiretroviral drugs in human plasma for quantitative analysis with liquid chromatography-tandem mass spectrometry. Biomed. Chromatogr. 21, 1095-1104 (2007). (Pubitemid 47490320)
49. Leslie, E.M., Mao, Q., Oleschuk, C.J., Deeley, R.G. & Cole, S.P. Modulation of multidrug resistance protein 1 (MRP1/ABCC1) transport and atpase activities by interaction with dietary flavonoids. Mol. Pharmacol. 59, 1171-1180 (2001). (Pubitemid 32381597)
50. Kalvass, J.C. & Maurer, T.S. Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharm. Drug Dispos. 23, 327-338 (2002). (Pubitemid 36124162)