References
Quion-Verde H, Cutler RE. Clinical pharmacology of rapamycin: an immunosuppressive relative of FK 506. Dial Transplant 1993 Nov; 22: 693
Sehgal SN, Molnarkimber K, Ocain TD, et al. Rapamycin: a novel immunosuppressive macrolide. Med Res Rev 1994 Jan; 14: 1–22
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
Supko JG, Malspeis L. Dose-dependent pharmacokinetics of rapamycin-28-N,N-dimethylglycinate in the mouse. Can Chemother Pharmacol 1994 Jan; 33: 325–30
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
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
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
Ferron GM, Mishina EV, Zimmerman JJ, et al. Population pharmacokinetics of sirolimus in kidney transplant patients. Clin Pharmacol Ther 1997 Apr; 61: 416–28
Hughes SE, Gruber SA. New immunosuppressive drugs in organ transplantation. J Clin Pharmacol 1996 Dec; 36: 1081–92
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
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
Collier DStJ, Caine RY, Pollard SG, et al. Rapamycin in experimental renal allografts in primates. Transplant Proc 1991 Aug; 23: 2246–7
Almond PS, Moss A, Nakhleh R, et al. Rapamycin in a porcine renal transplant model. Transplant Proc 1993 Feb; 25 Pt 1: 716
Ochiai T, Gunji Y, Nagata M, et al. Effects of rapamycin in experimental organ allografting. Transplantation 1993 Jul; 56: 15–9
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
Brattström C, Wilczek H, Tydén G, et al. Hyperlipidemia in renal transplant recipients treated with sirolimus (rapamycin). Transplantation 1998 May 15; 65: 1272–4
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
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
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
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
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
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
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
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
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
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
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
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
Vilquin J-T, Asselin I, Guérette B, et al. Successful myoblast allotransplantation in mdx mice using rapamycin. Transplantation 1995 Feb 15; 59: 422–6
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
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
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
Clin Investig News 1996 Aug: 9
AHP’s Rapamune improves 6-month graft survival. Marketletter 1998 Jul; 25: 23
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Sirolimus. Drugs R&D 1, 100–107 (1999). https://doi.org/10.2165/00126839-199901010-00033
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DOI: https://doi.org/10.2165/00126839-199901010-00033