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Sirolimus

AY 22989, NSC 226080, NSC 606698, Rapamycin, Rapamune®

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References

  1. Quion-Verde H, Cutler RE. Clinical pharmacology of rapamycin: an immunosuppressive relative of FK 506. Dial Transplant 1993 Nov; 22: 693

    Google Scholar 

  2. Sehgal SN, Molnarkimber K, Ocain TD, et al. Rapamycin: a novel immunosuppressive macrolide. Med Res Rev 1994 Jan; 14: 1–22

    Article  PubMed  CAS  Google Scholar 

  3. Streit F, Christians U, Schiebel H-M, et al. Structural identification of three metabolites and a degradation product of the macrolide immunosuppressant sirolimus (rapamycin) by electrospray-MS/MS after incubation with human liver microsomes. Drug Metab Dispos 1996 Nov; 24: 1272–8

    PubMed  CAS  Google Scholar 

  4. Supko JG, Malspeis L. Dose-dependent pharmacokinetics of rapamycin-28-N,N-dimethylglycinate in the mouse. Can Chemother Pharmacol 1994 Jan; 33: 325–30

    Article  CAS  Google Scholar 

  5. Lampen A, Zhang Y, Hackbarth I, et al. Metabolism and transport of the macrolide immunosuppressant sirolimus in the small intestine. J Pharmacol Exper Ther 1998 Jun; 285: 1104–12

    CAS  Google Scholar 

  6. Johnson EM, Zimmerman J, Duderstadt K, et al. A randomized, double-blind, placebo-controlled study of the safety, tolerance, and preliminary pharmacokinetics of ascending single doses of orally administered sirolimus (rapamycin) in stable renal transplant recipients. Transplant Proc 1996 Apr: 28: 987

    PubMed  CAS  Google Scholar 

  7. Brattström C, Tydén G, Säwe J, et al. A randomized, doubleblind, placebo-controlled study to determine safety, tolerance, and preliminary pharmacokinetics of ascending single doses of orally administered sirolimus (rapamycin) in stable renal transplant recipients. Transplant Proc 1996 Apr; 28: 985–6

    PubMed  Google Scholar 

  8. Ferron GM, Mishina EV, Zimmerman JJ, et al. Population pharmacokinetics of sirolimus in kidney transplant patients. Clin Pharmacol Ther 1997 Apr; 61: 416–28

    Article  PubMed  CAS  Google Scholar 

  9. Hughes SE, Gruber SA. New immunosuppressive drugs in organ transplantation. J Clin Pharmacol 1996 Dec; 36: 1081–92

    PubMed  CAS  Google Scholar 

  10. Kaplan B, Meier-Kriesche H-U, Napoli KL, et al. The effects of relative timing of sirolimus and cyclosporine microemulsion formulation coadministration on the pharmacokinetics of each agent. Clin Pharmacol Ther 1998 Jan; 63: 48–53

    Article  PubMed  CAS  Google Scholar 

  11. Fealy MJ, Umansky WS, Bickel KD, et al. Efficacy of rapamycin and FK 506 in prolonging rat hind limb allograft survival. Ann Surg 1994 Jan; 219: 88–93

    Article  PubMed  CAS  Google Scholar 

  12. Collier DStJ, Caine RY, Pollard SG, et al. Rapamycin in experimental renal allografts in primates. Transplant Proc 1991 Aug; 23: 2246–7

    PubMed  Google Scholar 

  13. Almond PS, Moss A, Nakhleh R, et al. Rapamycin in a porcine renal transplant model. Transplant Proc 1993 Feb; 25 Pt 1: 716

    PubMed  CAS  Google Scholar 

  14. Ochiai T, Gunji Y, Nagata M, et al. Effects of rapamycin in experimental organ allografting. Transplantation 1993 Jul; 56: 15–9

    Article  PubMed  CAS  Google Scholar 

  15. Slaton JW, Murgia MG, Jordan S, et al. Rapamycin in conjunction with cyclosporine/steroids in HLA-DR mismatched living-related renal transplants. J Urol 1995 Apr; 153 Suppl.: 400

    Google Scholar 

  16. Brattström C, Wilczek H, Tydén G, et al. Hyperlipidemia in renal transplant recipients treated with sirolimus (rapamycin). Transplantation 1998 May 15; 65: 1272–4

    Article  PubMed  Google Scholar 

  17. Stepkowski SM, Napoli KL, Wang M-E, et al. Effects of the pharmacokinetic interaction between orally administered sirolimus and cyclosporine on the synergistic prolongation of heart allograft survival in rats. Transplantation 1996 Oct 15; 62: 986–94

    Article  PubMed  CAS  Google Scholar 

  18. Yoshimura R, Yoshimura N, Nakatani T, et al. Study of the effect of immunosuppressive agents on renal cytochrome P- 450 system in the rat. Transplant Proc 1994 Aug; 26: 1913–4

    PubMed  CAS  Google Scholar 

  19. Blazar BR, Taylor PA, Snover DC, et al. Murine recipients of fully mismatched donor marrow are protected from lethal graft-versus-host disease by the in vivo administration of rapamycin but develop an autoimmune-like syndrome. J Immunol 1993 Nov 15; 151: 5726–41

    PubMed  CAS  Google Scholar 

  20. Wieder KJ, Hancock WW, Schmidbauer G, et al. Rapamycin treatment depresses intragraft expression of KC/MIP-2, granzyme B, and IFN-gamma in rat recipients of cardiac allografts. J Immuno 1993 Jul 15; 151: 1158–66

    CAS  Google Scholar 

  21. Chen H, Luo H, Daloze P, et al. Rapamycin-induced long-term allograft survival depends on persistence of alloantigen. J Immunol 1994 Mar; 152: 3107–18

    PubMed  CAS  Google Scholar 

  22. Schmid C, Heemann U, Azuma H, et al. Rapamycin inhibits transplant vasculopathy in long-surviving rat heart allografts. Transplantation 1995 Oct 15; 60: 729–33

    Article  PubMed  CAS  Google Scholar 

  23. Yatscoff RW, Wang S, Keenan R, et al. Efficacy of rapamycin, RS-61443, and cyclophosphamide in the prolongation of survival of discordant pig-to-rabbit cardiac xenografts. Transplant Proc 1994 Jun; 26: 1271–3

    PubMed  CAS  Google Scholar 

  24. Stepkowski SM, Tu Y, Chou T-C, et al. Synergistic interactions of cyclosporine, rapamycin, and brequinar on heart allograft survival in mice. Transplant Proc 1994 Oct; 26: 3025–7

    PubMed  CAS  Google Scholar 

  25. Granger DK, Cromwell JW, Chen SC, et al. Prolongation of renal allograft survival in a large animal model by oral rapamycin monotherapy. Transplantation 1995 Jan 27; 59: 183–6

    PubMed  CAS  Google Scholar 

  26. Ferraresso M, Knight R, Tu Y, et al. Triple combination of cyclosporine, brequinar, and rapamycin prolongs kidney allograft survival in the mongrel dog. Transplant Proc 1994 Oct; 26: 3028

    PubMed  CAS  Google Scholar 

  27. Fabian MC, Lakey JRT, Rajotte RV, et al. The efficacy and toxicity of rapamycin in murine islet transplantation: in vitro and in vivo studies. Transplantation 1993 Nov; 56: 1137–42

    Article  PubMed  CAS  Google Scholar 

  28. Yakimets WJ, Lakey JRT, Yatscoff RW, et al. Prolongation of canine pancreatic islet allograft survival with combined rapamycin and cyclosporin therapy at low doses: rapamycin efficacy is blood level related. Transplantation 1993 Dec; 56: 1293–8

    Article  PubMed  CAS  Google Scholar 

  29. Vilquin J-T, Asselin I, Guérette B, et al. Successful myoblast allotransplantation in mdx mice using rapamycin. Transplantation 1995 Feb 15; 59: 422–6

    PubMed  CAS  Google Scholar 

  30. Dono K, Wood ML, Ozato H, et al. Marked prolongation of rat skin xenografts induced by intrathymic injection of xenogeneic splenocytes and a short course of rapamycin in antilymphocte serum-treated mice. Transplantation 1995 Apr 15; 59: 929–32

    Article  PubMed  CAS  Google Scholar 

  31. Hale DA, Gottschalk R, Fukuzaki T, et al. Superiority of sirolimus (Rapamycin) over cyclosporine in augmenting allograft and xenograft survival in mice treated with antilymphocyte serum and donor-specific bone marrow. Transplantation 1997 Feb 15; 63: 359–64

    Article  PubMed  CAS  Google Scholar 

  32. Chen H, Qi S, Xu D, et al. Combined effect of rapamycin and FK 506 in prolongation of small bowel graft survival in the mouse. Transplant Proc 1998 Sep; 30: 2579–81

    Article  PubMed  CAS  Google Scholar 

  33. Clin Investig News 1996 Aug: 9

  34. AHP’s Rapamune improves 6-month graft survival. Marketletter 1998 Jul; 25: 23

    Google Scholar 

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Sirolimus. Drugs R&D 1, 100–107 (1999). https://doi.org/10.2165/00126839-199901010-00033

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