Tissue distribution and clinical monitoring of the novel macrolide immunosuppressant SDZ-RAD and its metabolites in monkey lung transplant recipients: Interaction with cyclosporine

Journal of Pharmacology and Experimental Therapeutics

Volumn 294, Issue 1, 2000, Pages 323-332

  Serkova, Natalie ^a   Hausen, Bernard ^b   Berry, Gerald J ^b   Jacobsen, Wolfgang ^a   Benet, Leslie Z ^a   Morris, Randall E ^b   Christians, Uwe ^a,b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOSPORIN; EVEROLIMUS;

ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG MONITORING; GRAFT REJECTION; IMMUNOSUPPRESSIVE TREATMENT; LUNG TRANSPLANTATION; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL;

ANIMALS; CYCLOSPORINE; DRUG INTERACTIONS; DRUG MONITORING; IMMUNOSUPPRESSIVE AGENTS; LUNG TRANSPLANTATION; MACACA FASCICULARIS; SIROLIMUS; TISSUE DISTRIBUTION;

EID: 0033932343     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Benet LZ, Wu CY, Hebert MF and Wacher VJ (1996) Intestinal drug metabolism and antitransport processes: A potential paradigm shift in oral drug delivery. J Control Release 39:139-143.
2. Böhler T, Waiser J, Budde K, Lichter S, Jauho A, Fritsche L, Korn A and Neumayer HH (1998) The in vivo effect of rapamycin derivative SDZ RAD on lymphocyte proliferation. Transplant Proc 30:2195-2197.
3. Christians U, Strohmeyer S, Kownatzki R, Schiebel HM, Bleck JS, Greipel J, Kohlhaw K, Schottmann R and Sewing KF (1991) Investigations on the metabolic pathways of cyclosporine: I. Excretion of cyclosporine and its metabolites in human bile - Isolation of 12 new cyclosporine metabolites. Xenobiotica 21:1185-1198.
4. Collier DS, Calne R, Thiru S, Lim S, Pollard SG, Barron P, Da Costa M and White DJ (1990) Rapamycin in experimental renal allografts in dogs and pigs. Transplant Proc 22:1674-1675.
5. Collier DS, Calne RY, Pollard SG, Friend PJ and Thiru S (1991) Rapamycin in experimental renal allografts in primates. Transplant Proc 23:2246-2247.
6. Cooper JD (1989) Herbert Sloan lecture. Lung transplantation. Ann Thorac Surg 47:28-44.
7. Crowe A, Brülisauer A, Dürr L, Guntz P and Lemaire M (1999) Absorption and intestinal metabolism of SDZ-RAD and rapamycin in rats. Drug Metab Dispos 27:627-632.
8. Crowe A and Lemaire M (1998) 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.
9. Dias VC, Madsen KL, Mulder KE, Keelan M, Yatscoff RW and Thomson AB (1998) Oral administration of rapamycin and cyclosporine differentially alter intestinal function in rabbits. Dig Dis Sci 43:2227-2236.
10. Gan LSL, Moseley MA, Koshla B, Augustijns PF, Bradshaw TP, Hnedren RW and Thakker DR (1996) CYP3A-like cytochrome P450-mediated metabolism and polarized efflux of cyclosporine in Caco-2 cells. Interaction between the biochemical barriers to intestinal transport. Drug Metab Dispos 24:344-349.
11. Hausen B, Ikonen T, Briffa N, Berry GJ, Christians U, Robbins RC, Hook L, Serkova N, Benet LZ, Schuler W and Morris RE (2000) Combined immunosuppression with cyclosporine (Neoral) and SDZ RAD in non-human primate lung transplantation: Systematic pharmacokinetic-based trials to improve efficacy and tolerability. Transplantation 69:76-86.
12. Kahan BD (1989) Cyclosporine. New Engl J Med 321:1725-1738.
13. Kolars JC, Lown KS, Schmiedlin-Ren P, Gosh M, Fang C, Wrighton SA, Merion RM and Watkins PB (1994) CYP3A gene expression in human gut epithelium. Pharmacogenetics 4:247-259.
14. Lemaire M and Tillement JP (1982) Role of lipoproteins and erythrocytes in the in vitro binding and distribution of cyclosporin A in blood. J Pharm Pharmacol 34:715-718.
15. Lensmeyer GL, Wiebe DA, Carlson IH and Subramanian R (1991) Concentration of cyclosporine A and its metabolites in human tissues postmortem. J Anal Toxicol 15:110-115.
16. Lown KS, Mayo RR, Leichtman AB, Hsiao HL, Turgeon DK, Schmiedlin-Ren P, Brown MB, Guo W, Rossi SJ, Benet LZ and Watkins PB (1997) Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther 62:248-260.
17. Mraz W, Zink RA, Graf A, Preis D, Illner WD, Land W, Siebert W and Zöttlein H (1983) Distribution and transfer of cyclosporine among various human lipoprotein classes. Transplant Proc 15:2426-2429.
18. Murgia MG, Jordan S and Kahan BD (1996) The side effect profile of sirolimus: A phase I study in quiescent cyclosporine-prednisolone-treated renal transplant patients. Kidney Int 49:209-216.
19. Napoli KL, Wang ME, Stepkowski SM and Kahan BD (1997) Distribution of sirolimus in rat tissue. Clin Biochem 30:135-142.
20. Napoli KL, Wang ME, Stepkowski SM and Kahan BD (1998) Relative tissue distributions of cyclosporine and sirolimus after concomitant peroral administration to the rat: Evidence for pharmacokinetic interactions. Theor Drug Monit 20:123-133.
21. Oellerich M, Armstrong VW, Kahan BD, Shaw L, Holt DW, Yatscoff R, Lindholm A, Halloran P, Gallicano K and Wonigeit K (1995) Lake Louise consensus conference on cyclosporin monitoring in organ transplantation: Report of the consensus panel. Theor Drug Monit 17:642-654.
22. Rödl S and Khoshsorur G (1990) Binding of cyclosporine to human serum lipoproteins. Transplant Proc 22:287-288.
23. Ryffel B, Woerly G, Greiner B, Haendler B, Mihatsch MJ and Foxwell BMJ (1991) Distribution of cyclosporine binding protein cyclosphilin in human tissues. Immunology 72:399-404.
24. Sangalli L, Bortolloti A, Passerini F and Bonati M (1990) Placental transfer, tissue distribution, and pharmacokinetics of cyclosporine in the pregnant rabbit. Drug Metab Dispos 18:102-106.
25. Schuler W, Sedrani R, Cottens S, Haberlin B, Schulz M, Schuurman HJ, Zenke G, Zerwes HG and Schreier MH (1997) SDZ RAD, a new rapamycin derivative: Pharmacological properties in vitro and in vivo. Transplantation 64:36-42.
26. Schuurman HJ, Cottens S, Fuchs S, Joergensen J, Meerloo T, Sedrani R, Tanner M, Zenke G and Schuler W (1997) SDZ RAD, a new rapamycin derivative: Synergism with cyclosporine. Transplantation 64:32-35.
27. Schuurman HJ, Hengy J-C, Ringers J, Schuler W and Jonker W (1996) Neoral pharmacokinetics in cynomolgus monkeys: Relation to efficacy in renal allografting. Transplant Proc 28:3142-3144.
28. Schuurman HJ, Schuler W, Ringers J and Jonker M (1998) The macrolide SDZ RAD is efficacious in a nonhuman primate model of allotransplantation. Transplant Proc 30:2198-2199.
29. Segarra I, Brazelton TR, Gutermann N, Hausen B, Morris RE, Benet LZ and Christians U (1998) Development of a high-performance liquid chromatographic electrospray mass spectrometric assay for the specific and sensitive quantification of the novel immunosuppressive macrolide 40-O-(2-hydroxethyl) rapamycin. J Chromatogr 720:179-187.
30. Stepkowski SM, Napoli KL, Wang ME, Qu X, Chou TC and Kahan BD (1996) Effects of the pharmacokinetic interaction between orally administered sirolimus and cyclosporine on the synergistic prolongation of heart allograft survival in rats. Transplantation 62:986-994.
31. Streit F, Christians U, Schiebel HM, Napoli KL, Ernst L, Linck A, Kahan BD and Sewing KF (1996) Sensitive and specific quantification of sirolimus (rapamycin) and its metabolites in blood of kidney graft recipients by HPLC/electrospray-mass spectrometry. Clin Chem 42:1417-1425.
32. Trulock EP (1993) Management of lung transplant rejection. Chest 103:1566-1576.
33. Vidal C, Kirchner GI and Sewing KF (1998) Structural elucidation by electrospray mass spectrometry: An approach to the in vitro metabolism of the macrolide immunosuppressant SDZ RAD. J Am Soc Mass Spectrom 9:1267-1274.
34. Wacher VJ, Silverman JA, Zhang Y and Benet LZ (1998) Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J Pharm Sci 87:1322-1330.
35. Wang CP, Chan KW, Schiksnis RA, Scatina J and Sisenwine SF (1994) High performance liquid chromatographic isolation, spectroscopic characterization, and immunosuppressive activities of two rapamycin degradation products. J Liq Chromatogr 17:3383-3389.
36. Yatscoff RW, Boeckx R, Holt DW, Kahan BD, LeGatt DF, Sehgal S, Soldin SJ, Napoli K and Stiller C (1995) Consensus guidelines for therapeutic drug monitoring of rapamycin: Report of the consensus panel. Theor Drug Monit 17:676-680.
37. Yousem SA, Berry GJ, Cagle PT, Chamberlain D, Husain AN, Hruban RH, Marchevsky A, Ohori NP, Ritter J, Stewart S and Tazelaar HD (1996) Revision of the 1990 working formulation for the classification of pulmonary allograft rejection: Lung rejection study group. J Heart Lung Transplant 15:1-15.