Experimental estimation of the role of P-Glycoprotein in the pharmacokinetic behaviour of telithromycin, a novel ketolide, in comparison with roxithromycin and other macrolides using the Caco-2 cell model

Journal of Pharmacy and Pharmaceutical Sciences

Volumn 6, Issue 1, 2003, Pages 1-12

  Pachot, Jean I ^a   Botham, Roger P ^a   Haegele, Klaus D ^a   Hwang, Kinkai ^a  

^a SANOFI   (France)

Author keywords

[No Author keywords available]

Indexed keywords

AZITHROMYCIN; CLARITHROMYCIN; ERYTHROMYCIN; GLYCOPROTEIN P; KETOCONAZOLE; KETOLIDE; MACROLIDE; MANNITOL; ROXITHROMYCIN; TELITHROMYCIN; VERAPAMIL;

ARTICLE; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; CONTROLLED STUDY; CROSS REACTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG DISTRIBUTION; DRUG DOSE; DRUG ELIMINATION; DRUG MECHANISM; DRUG PENETRATION; DRUG TARGETING; DRUG TRANSPORT; HUMAN; HUMAN CELL; INTESTINE ABSORPTION; MATHEMATICAL MODEL; MONOLAYER CULTURE; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION; TISSUE DISTRIBUTION;

ANTI-BACTERIAL AGENTS; BIOLOGICAL TRANSPORT; CACO-2 CELLS; CELL MEMBRANE; HUMANS; KETOLIDES; MACROLIDES; P-GLYCOPROTEIN; ROXITHROMYCIN;

EID: 0038725719     PISSN: 14821826     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Chin J.E., Soffir R., Noonan K.E., Choi K., and Roninson I.B., Structure and expression of the human MDR (P-Glycoprotein) gene family. Mol. Cell. Biol., 9: 3808-3820, 1989.
2. Oudard S., Thierry A., Jorgensen T.J., and Rahman A., Sensitization of multidrug-resistance colon cancer cells to doxorubicin encapsulated in liposomes. Cancer Chemother. Pharmacol. 28: 259-265, 1991.
3. Hunter J., Hirst B.H., and Simmons N.L., Drug absorption limited by P-glycoprotein-mediated secretoy drug transport in human intestinal epithelial Caco-2 cell layers. Pharm. Res., 10: 743-749, 1993.
4. Schinkel A.H., Wagenaar E., Van Deemter L., Mol C.A., and Borst P., Absence of the mdr1a P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, dogoxin, and cyclosporin A. J. Clin. Invest. 96: 1698-16705, 1995.
5. Sparreboom A., Van Asperen J., Mayer U., Schinkel A.H., Smit J.W., Meijer D.K.F., Borst P., Nooijen W.J., Beijnen J.H., and Van Tellingen O., Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc. Natl. Acad. Sci. 94: 2031-2035, 1997.
6. Wakasugi, H., Yano, I., Ito T., Hashida, T., Futami, T., Nohara, R., Sasayama, S., and Inui, K., Effect of clarithromycin on renal excretion of digoxin: interaction with P-glycoprotein. Clin. Pharmacol. Ther. 64: 123-128, 1998.
7. Zhang Y., Hsieh Y., Izumi T., Lin E.T., and Benet L.Z., Effects of ketoconazole on the intestinal metabolism, transport and oral bioavailability of K02, a novel Vinylsulfone peptidomimetic cysteine protease inhibitor and a P450 3A, P-glycoprotein dual substrate, in male Sprague-Dawley rats., J. Pharmacol. Exp. Ther. 287: 246-252, 1998.
8. Yu D.K., The contribution of P-glycoprotein to pharmacokinetic drug-drug interaction., 39: 1203-1211, 1999.
9. Hsing S., Gatmaitan Z., and Arias I.M., The function of Gp170, the multidrug-resistance gene product, in the brush border of rat intestinal mucosa. Gastroenterology, 102: 879-885, 1992.
10. Pavelic Z.P., Reising J., Pavelic L., Kelley D.J., Stambrook P.J., and Gluckman J.L., Detection of P-glycoprotein with four monoclonal antibodies in normal and tumor tissues. Arch. Otolaryngol. Head Neck Surg. 119: 753-757, 1993.
11. Terao T., Hisanaga E., Sai Y., Tamai I., and Tsuji A., Active secretion of drugs from the small intestinal epithelium in rats bu P-glycoprotein functioning as an absorption barrier. J. Pharm. Pharmacol., 48: 1083-1089, 1996.
12. Makhey V.D., Guo A., Norris D.A., Hu P., Yan J., and Sinko P.J., Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells. Pharm. Res. 15: 1160-1167, 1998.
13. Saitoh H. and Aungst B.J., Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Phram. Res. 12: 1304-1310, 1995.
14. Lown K.S., Mayo R.R., Leichtman A.B., Hsiao H.L., Turgeon D.K., Schmiedlin-Ren P., Brown M.B., Guo W., Rossi S.J., Benet L.Z., and Watkins P.B., Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin. Pharmacol. Ther. 62: 248-260, 1997.
15. Kim, R.B., Fromm, M.F., Wandel, B.L., Wood, A.J.J., Roden D.M., and Wilkinson G.R., The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J. Clin. Invest., 101: 289-294, 1998.
16. Van Asperen, J., Van Tellingen, O., Schinkel, A.H., and Beijnen,J.H., Comparative pharmacokinetics of vinblastine after a 96-hour continuous infusion in wild-type mice and mice lacking mdr1a P-glycoprotein. J. Pharmacol. Exp. Ther., 289: 329-333, 1999.
17. Emi, Y., Tsunashima, D., Ogawara, K-I., Higaki, K., and Kimura T., Role of P-glycoprotein as a secretory mechanism in quinidine absorption from rat small intestine. J. Phram. Sci. 87: 295-299, 1997.
18. Van Asperen, J., Van Tellingen, O., Schinkel, A.H., and Beijnen, J.H., The pharmacological role of P-glycoprotein in the intestinal epithelium. Pharm. Res. 37: 429-435, 1998.
19. Ito, K., Kusuhara, H., Sugiyama, Y., Effects of Cyp3A4 and P-glycoprotein on oral drug absorption-theoretical approach. Pharm. Res., 16: 225-231, 1999.
20. Kim, D.-C., Burton, P.S., and Borchardt, R.T., A correlation between the permeability characteristics of a series of peptides using an in vitro cell culture model (Caco-2) and those using an in situ perfused rat ileum model of the intestinal mucosa. Pharm. Res., 10: 1710-1714, 1993.
21. Artursson, P., Palm, K., and Luthman, K., Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv. Drug Deliv. Rev. 22: 67-84, 1996.
22. Bayley, C.A., Bryla, P., and Malick, A.W., The use of the intestinal epithelial cell culture model, Caco-2, in pharmaceutical development. Adv. Drug Deliv. Rev., 22: 85-103, 1996.
23. Gan, L.-S. L. and Thakker, D.R., Applications of the Caco-2 model in the design and development of orally active drugs : elucidation of biochemical and physical barriers posed by the intestinal epithelium. Adv. Drug Deliv. Rev., 23: 77-98, 1997.
24. Yee, S., In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal absorption in man - fact or myth. Pharm. Res., 14: 763-766, 1997.
25. Garrigos, M., Belehradek J.Jr., Mir, L.M., and Orlowski S., Absence of cooperativity for MgATP and verapamil effects on the ATPase activity of P-glycoprotein containing membrane vesicules. Biochem. Bioph. Res. Com., 196: 1034-1041, 1993.
26. Orlowsky, S., Mir, L.M., Belehradek, J., and Garrigos, M., Effects of steroids and verapamil on P-glycoprotein ATPase activity: progesterone, desoxycorticosterone, corticosterone and verapamil are mutually non exclusive modulators. Biochem. J. 317: 515-522, 1996.
27. Orlowsky, S., Valente, D., Garrigos, M., and Ezan, E., Bromocriptine modulates P-glycoprotein function. Biochem. Bioph. Res. Com., 244: 481-488, 1998.
28. Döppenschmitt, S., Spahn-Langguth, H., Regårdh, C.G., and Langguth P., Radioligand-binding assay employing P-glycoprotein overexpression cells: Testing drug affinities to the secretory intestinal multidrug transporter. Pharm. Res., 15: 1001-1006, 1998.
29. Döppenschmitt, S., Spahn-Langguth, H., Regr̊dh, C.G., and Langguth P., Role of P-glycoprotein-mediated secretion in absorptive drug permeability: an approach using passive membrane permeability and affinity to P-glycoprotein. J. Pharm. Sci., 88: 1067-1072, 1999.
30. Garrigos, M., Mir, L.M., and Orlowski S., Competitive and non-competitive inhibition of the multidrug-resistance-associated P-glycoprotein ATPase. Further experimental evidence for a multisite model. Eur. J. Biochem., 244: 664-673, 1997.
31. Pascaud, C., Garrigos, M., Orlowski, S., Multidrug resistance transporter P-glycoprotein has distinct but interacting binding sites for cytotoxic drugs and reversing agents. Biochem. J., 333: 351-358, 1998.
32. Denis, A., Agouridas, C., Auger, J.M., Benedetti, Y., Bonnefoy, A., Bretin, F., Chantot, J.F., Dussarat, A., Fromentin, C., D'Ambrières, S.G., Lachaud, S., Laurin, P., Le Martret, O., Loyau, V., Tessot, N., Pejac, J-M. Perron, S., Synthesis and antibacterial activity of HMR 3647 a new ketolide highly potent against erythromycin-resistant and susceptible pathogens. Bioorg Med Chem Lett., 9: 3075-3080, 1999.
33. Rawadi, G., Lecaque, D., Pirot, D., and Roman-Roman, S., Detection and identification of mycoplasma contamination in cell cultures by polymerase chain reaction. Meth. Molec. & Cell. Biol. 4: 147-156, 1993.
34. Boisset, M., Botham, R.P., Haegele, D.K., Lenfant, B., Pachot, J.I., Absorption of angiotensin II antagonists in Ussing chambers, Caco-2, perfused jejunum loop and in vivo: Importance of drug ionization in the in vitro prediction of in vivo absorption. E. J. Pharm. Sci, 10: 215-224, 2000.
35. Pontier C., Pachot J., Botham R., Lenfant B., and Arnaud P., HT29-MTX and Caco-2/TC7 monolayers as predictive models for human intestinal absorption: Role of the mucus layer. J. Pharm. Sci. 90: 1608-1619, 2001.
36. Takano M., Hasegawa R., Fukuda T., Yumoto R., Nagai J., and Murakami T., Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells. Eur. J. Pharmacol. 358: 289-294, 1998.
37. [37] Saito H., Fukasawa Y., Otsubo Y., Yamada K., Sezaki H., and Yamashita S., Carrier-mediated transport of macrolide antibacterial agents across Caco-2 cell molnolayers. Pharm. Res. 17: 761-765, 2000.
38. He L., and Liu G.Q., Effects of various principles from Chinese herbal medicine on rhodamine123 accumulation in brain capillary endothelial cells. Acta Pharmacol. Sin., 2002, 23: 591-596, 2002.
39. Anderle P., Niederer E., Rubas W., Hilgendorf C., Spahn-Langguth H., Wunderli-Allenspach H., Merkle H.P., and Langguth P., P-glycoprotein (P-GP) mediated efflux in Caco-2 monolayers: the influence of culturing conditions and drug exposure on P-GP expression levels. J. Pharm. Sci., 87: 757-762, 1998.
40. Zhang Y., and Benet L.Z., Characterization of P-glycoprotein mediated transport of K02, a novel vinylsulfone peptidomimetic cysteine protease inhibitor, across MDR1-MDCK and Caco-2 cell monolayers. Pharm. Res. 15: 1520-1524, 1998.
41. Walle, U.K., and Walle, T., Taxol transport by human intestinal epithelial Caco-2 cells. J. Pharmacol. Exp. Ther. 26: 343-346, 1998.