Effect of intestinal and hepatic first-pass extraction on the pharmacokinetics of everolimus in rats

Drug Metabolism and Pharmacokinetics

Volumn 23, Issue 6, 2008, Pages 469-475

  Yokomasu, Akira ^a   Yano, Ikuko ^a   Sato, Eriko ^a   Masuda, Satohiro ^a   Katsura, Toshiya ^a   Inui, Ken Ichi ^a  

^a KYOTO UNIVERSITY HOSPITAL   (Japan)

Author keywords

Cyclosporine; Everolimus; First pass effect; Interaction; Pharmacokinetics; Tacrolimus

Indexed keywords

CYCLOSPORIN; CYCLOSPORIN A; EVEROLIMUS; TACROLIMUS;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG POTENTIATION; FIRST PASS EFFECT; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; MALE; NONHUMAN; QUANTITATIVE ANALYSIS; RAT; TANDEM MASS SPECTROMETRY;

EID: 64049116793     PISSN: 13474367     EISSN: 18800920     Source Type: Journal    
DOI: 10.2133/dmpk.23.469     Document Type: Article

References (29)

1. Schuler, W., Sedrani, R., Cottens, S., Haberlin, B., Schulz, M., Schuurman, H. J., Zenke, G., Zerwes, H. G. and Schreier, M. H.: SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo. Transplantation, 64: 36-42 (1997).
2. Crowe, A., Bruelisauer, A., Duerr, L., Guntz, P. and Lemaire, M.: Absorption and intestinal metabolism of SDZ-RAD and rapamycin in rats. Drug Metab. Dispos., 27: 627-632 (1999).
3. Neumayer, H. H., Paradis, K., Korn, A., Jean, C., Fritsche, L., Budde, K., Winkler, M., Kliem, V., Pichlmayr, R., Hauser, I. A., Burkhardt, K., Lison, A. E., Barndt, I. and Appel-Dingemanse, S.: Entry-into-human study with the novel immunosuppressant SDZ RAD in stable renal transplant recipients. Br. J. Clin. Pharmacol., 48: 694-703 (1999).
4. Pascual, J.: Everolimus in clinical practice-renal transplantation. Nephrol. Dial. Transplant., 21 (Suppl 3): iii18-23 (2006).
5. Schweiger, M., Wasler, A., Prenner, G., Stiegler, P., Stadlbauer, V., Schwarz, M. and Tscheliessnigg, K.: Everolimus and reduced cyclosporine trough levels in maintenance heart transplant recipients. Transplant. Immunol., 16: 46-51 (2006).
6. Lehmkuhl, H., Ross, H., Eisen, H. and Valantine, H.: Everolimus (certican) in heart transplantation: optimizing renal function through minimizing cyclosporine exposure. Transplant. Proc., 37: 4145-4149 (2005).
7. Hausen, B., Boeke, K., Berry, G. J., Segarra, I., Benet, L. Z., Christians, U. andMorris, R. E.: Coadministration of neoral and the novel rapamycin analog, SDZ RAD, to rat lung allograft recipients: potentiation of immunosuppressive efficacy and improvement of tolerability of staggered versus simultaneous treatment. Transplantation, 67: 956-962 (1999).
8. Kovarik, J. M., Kahan, B. D, Kaplan, B., Lorber, M., Winkler, M., Rouilly, M., Gerbeau, C., Cambon, N., Boger, R., Rordorf, C. and Everolimus Phase 2 Study Group.: Longitudinal assessment of everolimus in de novo renal transplant recipients over the first post-transplant year: pharmacokinetics, exposure-response relationships, and influence on cyclosporine. Clin. Pharmacol. Ther., 69: 48-56 (2001).
9. Crowe, A. and Lemaire, M.: In vitro and in situ absorption of SDZ-RAD using a human intestinal cell line (Caco-2) and a single pass perfusion model in rats: comparison with rapamycin. Pharm. Res., 15: 1666-1672 (1998)
10. Jacobsen, W., Serkova, N., Hausen, B., Hausen, B., Morris R. E., Benet, L. Z. and Christians, U.: Comparison of the in vitro metabolism of the macrolide immunosuppressants sirolimus and RAD. Transplant. Proc., 33: 514-515 (2001).
11. Hebert, M. F.: Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Adv. Drug Deliv. Rev., 27: 201-214 (1997).
12. Mabasa, V. H. and Ensom, M. H.: The role of therapeutic monitoring of everolimus in solid organ transplantation. Ther. Drug Monit., 27: 666-676 (2005).
13. Kovarik, J. M., Kalbag, J., Figueiredo, J., Rouilly, M., Frazier, O. L. and Rordorf, C.: Differential influence of two cyclosporine formulations on everolimus pharmacokinetics: a clinically relevant pharmacokinetic interaction. J. Clin. Pharmacol., 42: 95-99 (2002).
14. Sato, E., Shimomura, M., Masuda, S., Yano, I., Katsura, T., Matsumoto, S., Okitsu, T., Iwanaga, Y., Noguchi, H., Nagata, H., Yonekawa, Y. and Inui, K.: Temporal decline in sirolimus elimination immediately after pancreatic islet transplantation. Drug Metab. Pharmacokinet., 21: 492-500 (2006).
15. Masuda, S. and Inui, K.: An up-date review on individualized dosage adjustment of calcineurin inhibitors in organ transplant patients. Pharmacol. Ther., 112: 184-198 (2006).
16. Matsubara, T., Kim, H. J., Miyata, M., Shimada, M., Nagata, K. and Yamazoe, Y.: Isolation and characterization of a new major intestinal CYP3A form, CYP3A62, in the rat. J. Pharmacol. Exp. Ther., 309: 1282-1290 (2004).
17. Cao, X., Gibbs, S. T., Fang, L., Miller, H. A., Landowski, C. P., Shin, H. C., Lennernas, H., Zhong, Y., Amidon, G.L., Yu, L. X. and Sun, D.: Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model. Pharm. Res., 23: 1675-1686 (2006).
18. Venkataramanan, R., Swaminathan, A., Prasad, T., Jain, A., Zuckerman, S., Warty, V.,McMichael, J., Lever, J., Burckart, G. and Starzl, T.: Clinical pharmacokinetics of tacrolimus. Clin. Pharmacokinet., 29: 404-430 (1995).
19. Ptachcinski, R. J., Venkataramanan, R. and Burckart, G. J.: Clinical pharmacokinetics of cyclosporin. Clin. Pharmacokinet., 11: 107-132 (1986).
20. Hashimoto, Y., Sasa, H., Shimomura, M. and Inui, K.: Effects of intestinal and hepatic metabolism on the bioavailability of tacrolimus in rats. Pharm. Res., 15: 1609-1613 (1998).
21. Igarashi, T., Yano, I., Saito, H. and Inui, K.: Decreased cyclosporin A concentrations in the absorption phase using microemulsion preconcentrate formulation in rats with cisplatin-induced acute renal failure. Biol. Pharm. Bull., 26: 1591-1595 (2003).
22. Laplanche, R., Meno-Tetang, G. M. and Kawai, R.: Physiologically based pharmacokinetic (PBPK) modeling of everolimus (RAD001) in rats involving non-linear tissue uptake. J. Pharmacokinet. Pharmacodyn., 34: 373-400 (2007).
23. Fukudo, M., Yano, I., Masuda, S., Fukatsu, S., Katsura, T., Ogura, Y., Oike, F., Takada, Y., Tanaka, K. and Inui, K.: Pharmacodynamic analysis of tacrolimus and cyclosporine in living-donor liver transplant patients. Clin. Pharmacol. Ther., 78, 168-181 (2005).
24. Yasuhara, M., Hashida, T., Toraguchi, M., Hashimoto, Y., Kimura, M., Inui, K., Hori, R., Inomata, Y., Tanaka, K. and Yamaoka, Y.: Pharmacokinetics and pharmacodynamics of FK506 in pediatric patients receiving living-related donor liver transplantations. Transplant. Proc., 27: 1108-1110 (1995).
25. Kovarik, J. M., Curtis, J. J., Hricik, D. E., Pescovitz, M. D., Scantlebury, V. and Vasquez, A.: Differential pharmacokinetic interaction of tacrolimus and cyclosporine on everolimus. Transplant. Proc., 38: 3456-3458 (2006).
26. Niwa, T., Yamamoto, S., Saito, M., Shiraga, T. and Takagi, A.: Effect of cyclosporine and tacrolimus on cytochrome P450 activities in human liver microsomes. Yakugaku Zasshi., 127: 209-216 (2007).
27. Rao, U. S. and Scarborough, G. A.: Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein. Mol. Pharmacol., 45: 773-776 (1994).
28. Siekierka, J. J., Staruch, M. J., Hung, S. H. and Sigal, N. H.: FK-506, a potent novel immunosuppressive agent, binds to a cytosolic protein which is distinct from the cyclosporin A-binding protein, cyclophilin. J. Immunol., 143: 1580-1583 (1989).
29. Thummel, K. E., Kunze, K. L. and Shen, D. D.: Enzyme-catalyzed processes of first-pass hepatic and intestinal drug extraction. Adv. Drug Deliv. Rev., 27: 99-127 (1997).