Physiologically based pharmacokinetics of cyclosporine A: Extension to tissue distribution kinetics in rats and scale-up to human

Journal of Pharmacology and Experimental Therapeutics

Volumn 287, Issue 2, 1998, Pages 457-468

  Kawai, Ryosei ^a   Mathew, Diane ^b   Tanaka, Chiaki ^a   Rowland, Malcolm ^b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOSPORIN A; CYCLOSPORIN A [8 DEXTRO O (2 HYDROXYETHYL)SERINE];

ARTICLE; CELL MEMBRANE PERMEABILITY; CELLULAR DISTRIBUTION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG PENETRATION; DRUG TISSUE LEVEL; DRUG UPTAKE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; TARGET CELL; TISSUE DISTRIBUTION;

ANIMALS; AREA UNDER CURVE; CYCLOSPORINE; HUMANS; MALE; MODELS, BIOLOGICAL; RATS; RATS, SPRAGUE-DAWLEY; TISSUE DISTRIBUTION;

EID: 0032469937     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Akaike H (1976) An information criterion (AIC). Math Sci 14:5-9.
2. Altman P (1961) Analysis and compilation, in D. Dittman (eds), Biological Handbooks: Blood and Other Body Fluids (Dittman D ed) FASEB, Washington DC.
3. 3H]-radio-immunoassay with a monoclonal antibody for monitoring cyclosporin in blood. Clin Chem 34:257-260.
4. Bernareggi A and Rowland M (1991) Physiological modeling of cyclosporin kinetics in rats and man. J Pharmacokinet Biopharm 19:21-50.
5. 1H NMR studies on bovine cyclophilin: Preliminary structural characterization of this specific cyclosporin A binding protein. Biochemistry 25:6778.
6. Dedrick RL, Zaharko DS and Lutz RJ (1973) Transport and binding of Methotrexate in vivo. J Pharm Sci 62:882-890.
7. Fahr A (1993) Cyclosporin clinical pharmacokinetics. Clin Pharmacokinet 24:472-495.
8. Gallo JM, Lam FC and Perrier DG (1987) Area method for the estimation of partition coefficients for physiological pharmacokinetic models. J Pharmacokinet Biopharm 15:271-280.
9. Gupta SK, Legg B, Solomon LR, Johnson RWG and Rowland M (1987) Pharmacokinetics of cyclosporin: influence of rate of constant intravenous infusion in renal transplant patients. Br J Clin Pharm 24:519-526.
10. Gupta S, Manfro R, Tomlanovich S, Gambertoglio J, Garovoy M and Benet LZ (1990) Effect of food on the pharmacokinetics of cyclosporine in healthy subjects following oral and intravenous administration. J Clin Pharmacol 30:643-653.
11. Holt D, Johanston A, Roberts N, Tredger J and Trull A (1994) Methodological and clinical aspects of cyclosporin monitoring: Report of the Association of Clinical Biochemists task force. Ann Clin Biochem 31:420-446.
12. Kawai R and Lemaire M (1993) Role of blood cell uptake on cyclosporin pharmacokinetics, in Proceeding of the International Symposium on Blood Binding and Drug Transfer (Tellement P and Eckert H eds) pp 89-108, EFC Publishing, Paris.
13. Kawai R, Lemaire M, Steimer J-L, Bruelisauer A, Niederberger W and Rowland M (1994) Physiologically-based pharmacokinetic study on a cyclosporin derivative, SDZ IMM 125. J Pharmacokinet Biopharm 22:327-365.
14. Khor S and Mayersohn M (1991) Potential error in the measurement of tissue to blood distribution coefficients in physiological pharmacokinetic modeling; Residual tissue blood. I. Theoretical considerations. Drug Metab Disp 19:478-485.
15. Khor S, Bozigian H and Mayersohn M (1991) Potential error in the measurement of tissue to blood distribution coefficients in physiological pharmacokinetic modeling; residual tissue blood. II. Distribution of phencyclidine in the rat. Drug Metab Disp 19:486-490.
16. Legg B and Rowland M (1988) Cyclosporin: erythrocyte binding and an examination of its use to estimate unbound concentration. Ther Drug Monit 10:16-19.
17. Lindholm A (1991) Factors influencing the pharmacokinetics of cyclosporine in man. Ther Drug Monit 13:465-477.
18. Luke D, Brunner L, Lopez-Berestein G and Yau J (1992) Pharmacokinetics of cyclosporine in bone marrow transplantation: Longitudinal characterization of drug in lipoprotein fractions. J Pharm Sci 81:208-211.
19. Mueller E, Kovarik J, van Bree J, Lison A and Kutz K (1994) Pharmacokinetics and tolerability of a microemulsion formulation of cyclosporine in renal allograft recipients - a concentration-controlled comparison with the commercial formulation. Transplantation 57:1178-1182.
20. Pang S and Rowland M (1977) Hepatic clearance of drugs. I. Theoretical considerations of a "well-stirred" model and a "parallel tube" model. Influence of hepatic blood flow, plasma and blood cell binding and hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 5:625-653.
21. Ryffel B, Woerly G, Greiner B, Haendler B, Mihatsch MJ and Poxwell BMJ (1991) Distribution of the cyclosporine binding protein cyclophilin in human tissues. Immunology 72:399-404.
22. Ryffel B (1993) Cyclosporin binding proteins. Biochem Pharmacol 46:1-12.
23. Sangalli L, Bortolotti A, Jiritano L and Bonati M (1988) Cyclosporine pharmacokinetics in rats and interspecies comparison in dogs, rabbits, rats, and humans. Drug Metab Disp 16:749-753.
24. Schneider H, Charara N, Schmitz R, Wehrli R, Mikol V, Zurini MGM, Quesniaux VFJ and Movva NR (1994) Human cyclophilin C: Primary structure, tissue distribution, and determination of binding specificity for cyclosporins. Biochemistry 33:8218-8224.
25. Sloop C, Dory L and Roheim P (1987) Interstitial fluid lipoproteins. J Lipid Res 28:225-237.
26. Sparreboom A, van Tellingen O, Nooijen WJ and Heijnen JH (1996) Nonlinear Pharmacokinetics of Paclitaxel in mice results from the pharmaceutical vehicle cremophor EL. Cancer Res 56:2112-2115.
27. Tamai I and Safa AR (1990) Competitive interaction of cyclosporins with the Vinca alkaloid-binding site of P-glycoprotein in multidrug-resistant cells. J Biol Chem 265:16509-16513.
28. Tsuji A, Yoshikawa T, Nishide K, Minami H, Kimura M, Nakashima E, Terasaki T, Miyamoto E, Nightingale C and Yamana T (1933) Physiologically based pharmacokinetic model for beta-lactam antibiotics I: Tissue distribution and elimination in rats. J Pharm Sci 72:1239-1252.
29. Tsuji A, Nishide K, Minami H, Nakashima E, Terasaki T and Yamana T (1985) Physiologically based pharmacokinetic model for cefazolin in rabbits and its preliminary extrapolation to man. Drug Metab Dispos 13:729-739.
30. Tsuji A, Sato H, Tamai I, Adachi H, Nishihara T, Ishiguro M, Ohnuma N and Noguchi T (1990) Physiologically based pharmacokinetics of a new penem, SUN5555, for evaluation of in vivo efficacy. Drug Metab Dispos 18:245-252.
31. Urien S, Zini R, Lemaire M and Tillement J-P (1990) Assessment of cyclosporine A interactions with human plasma lipoproteins in vitro and in vivo in the rat. J Pharm Exp Ther 253:305-309.
32. Vickers A, Fischer V, Connors S, Fischer R, Baldeck J-P, Maurer G and Brendel K (1992) Cyclosporin A metabolism in human liver, kidney, and intestine slices: Comparison to rat and dog slices and human cell lines. Drug Metab Dispos 20:802-809.
33. von Ahsen N, Helmhold M, Schütz E, Eisenhauer T, Armstrong V and Oellerich M (1997) Cyclosporin A trough levels correlate with serum lipoproteins and apolipoproteins: Implications for therapeutic drug monitoring of cyclosporin A. Ther Drug Monit 19:140-145.
34. Wallwork J (1986) Cyclosporin: Issues of Today, pp 39-44. Medical Education Services Ltd, Oxford, and Sandoz Pharmaceuticals Ltd, Frimley.
35. White DJG (1981) Cyclosporin A, Elsevier Biomedical Press, Amsterdam.
36. Wuesniaux V, Schreier M, Wenger R, Hiestand P, Harding M and van Regenmortel M (1988) Molecular characteristics of cyclophilin-cyclosporin interaction. Transplantation 46(Suppl):23s-28s.
37. Yang H and Elmquist WF (1996) The binding of cyclosporin A to human plasma: an in vitro microdialysis study. Pharm Res 13:622-627.