656
Views
19
CrossRef citations to date
0
Altmetric
Drug Safety Evaluations

A drug safety evaluation of everolimus in kidney transplantation

, &
Pages 1013-1022 | Published online: 06 Sep 2012

Bibliography

  • Nankivell BJ, Borrows RJ, Fung CL, The natural history of chronic allograft nephropathy. N Engl J Med 2003;349:2326-33
  • Nankivell BJ, Wavamunno MD, Borrows RJ, Mycophenolate mofetil is associated with altered expression of chronic renal transplant histology. Am J Transplant 2007;7:366-76
  • Matas AJ. Chronic progressive calcineurin nephrotoxicity: an overstated concept. Am J Transplant 2011;11:687-92
  • Snanoudj R, Royal V, Elie C, Specificity of histological markers of long-term CNI nephrotoxicity in kidney-transplant recipients under low-dose cyclosporine therapy. Am J Transplant 2011;11:2635-46
  • Naesens M, Kuypers DR, Sarwal M. Calcineurin inhibitor nephrotoxicity. Clin J Am Soc Nephrol 2009;4:481-508
  • Chapman JR. Chronic calcineurin inhibitor nephrotoxicity-lest we forget. Am J Transplant 2011;11:693-7
  • Grinyo JM, Bestard O, Torras J, Cruzado JM. Optimal immunosuppression to prevent chronic allograft dysfunction. Kidney Int Suppl 2010;119:S66-70
  • Budde K, Sommerer C, Becker T, Sotrastaurin, a novel small molecule inhibiting protein kinase C: first clinical results in renal-transplant recipients. Am J Transplant 2010;10:571-81
  • Vincenti F, Larsen C, Durrbach A, Costimulation blockade with belatacept in renal transplantation. N Engl J Med 2005;353:770-81
  • Campistol JM, de Fijter JW, Nashan B, Everolimus and long-term outcomes in renal transplantation. Transplantation 2011;92:S3-26
  • Mita MM, Mita A, Rowinsky EK. The molecular target of rapamycin (mTOR) as a therapeutic target against cancer. Cancer Biol Ther 2003;2:S169-77
  • Watanabe R, Wei L, Huang J. mTOR signaling, function, novel inhibitors, and therapeutic targets. J Nucl Med 2011;52:497-500
  • Brazelton TR, Morris RE. Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide. Curr Opin Immunol 1996;8:710-20
  • Schuler W, Sedrani R, Cottens S, SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo. Transplantation 1997;64:36-42
  • Kahan BD, Gibbons S, Tejpal N, Synergistic interactions of cyclosporine and rapamycin to inhibit immune performances of normal human peripheral blood lymphocytes in vitro. Transplantation 1991;51:232-9
  • Dumont FJ, Kastner C, Iacovone F Jr, Fischer PA. Quantitative and temporal analysis of the cellular interaction of FK-506 and rapamycin in T-lymphocytes. J Pharmacol Exp Ther 1994;268:32-41
  • Crowe A, Bruelisauer A, Duerr L, Absorption and intestinal metabolism of SDZ-RAD and rapamycin in rats. Drug Metab Dispos 1999;27:627-32
  • Neumayer HH, Paradis K, Korn A, Entry-into-human study with the novel immunosuppressant SDZ RAD in stable renal transplant recipients. Br J Clin Pharmacol 1999;48:694-703
  • Lamoureux F, Picard N, Boussera B, Sirolimus and everolimus intestinal absorption and interaction with calcineurin inhibitors: a differential effect between cyclosporine and tacrolimus. Fundam Clin Pharmacol 2012;26(4):463-72
  • Jacobsen W, Serkova N, Hausen B, Comparison of the in vitro metabolism of the macrolide immunosuppressants sirolimus and RAD. Transplant Proc 2001;33:514-15
  • Levy GA, Grant D, Paradis K, Pharmacokinetics and tolerability of 40-0-[2-hydroxyethyl]rapamycin in de novo liver transplant recipients. Transplantation 2001;71:160-3
  • Kovarik JM, Sabia HD, Figueiredo J, Influence of hepatic impairment on everolimus pharmacokinetics: implications for dose adjustment. Clin Pharmacol Ther 2001;70:425-30
  • Kovarik JM, Kalbag J, Figueiredo J, Differential influence of two cyclosporine formulations on everolimus pharmacokinetics: a clinically relevant pharmacokinetic interaction. J Clin Pharmacol 2002;42:95-9
  • Brandhorst G, Tenderich G, Zittermann A, Everolimus exposure in cardiac transplant recipients is influenced by concomitant calcineurin inhibitor. Ther Drug Monit 2008;30:113-16
  • Kovarik JM, Curtis JJ, Hricik DE, Differential pharmacokinetic interaction of tacrolimus and cyclosporine on everolimus. Transplant Proc 2006;38:3456-8
  • Amundsen R, Asberg A, Ohm IK, Christensen H. Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro. Drug Metab Dispos 2012;40:655-61
  • Kovarik JM, Noe A, Berthier S, Clinical development of an everolimus pediatric formulation: relative bioavailability, food effect, and steady-state pharmacokinetics. J Clin Pharmacol 2003;43:141-7
  • Kovarik JM, Hartmann S, Figueiredo J, Effect of food on everolimus absorption: quantification in healthy subjects and a confirmatory screening in patients with renal transplants. Pharmacotherapy 2002;22:154-9
  • Picard N, Levoir L, Lamoureux F, Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica 2011;41:752-7
  • Pascual J, del CD, Cabello M, Interaction between everolimus and tacrolimus in renal transplant recipients: a pharmacokinetic controlled trial. Transplantation 2010;89:994-1000
  • Kovarik JM, Kahan BD, Kaplan B, 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 2001;69:48-56
  • Lorber MI, Mulgaonkar S, Butt KM, Everolimus versus mycophenolate mofetil in the prevention of rejection in de novo renal transplant recipients: a 3-year randomized, multicenter, phase III study. Transplantation 2005;80:244-52
  • Vitko S, Margreiter R, Weimar W, Everolimus (Certican) 12-month safety and efficacy versus mycophenolate mofetil in de novo renal transplant recipients. Transplantation 2004;78:1532-40
  • Vitko S, Margreiter R, Weimar W, Three-year efficacy and safety results from a study of everolimus versus mycophenolate mofetil in de novo renal transplant patients. Am J Transplant 2005;5:2521-30
  • Nashan B, Curtis J, Ponticelli C, Everolimus and reduced-exposure cyclosporine in de novo renal-transplant recipients: a three-year phase II, randomized, multicenter, open-label study. Transplantation 2004;78:1332-40
  • Tedesco-Silva H Jr, Vitko S, Pascual J, 12-month safety and efficacy of everolimus with reduced exposure cyclosporine in de novo renal transplant recipients. Transpl Int 2007;20:27-36
  • Tedesco SH Jr, Cibrik D, Johnston T, Everolimus plus reduced-exposure CsA versus mycophenolic acid plus standard-exposure CsA in renal-transplant recipients. Am J Transplant 2010;10:1401-13
  • Chan L, Hartmann E, Cibrik D, Optimal everolimus concentration is associated with risk reduction for acute rejection in de novo renal transplant recipients. Transplantation 2010;90:31-7
  • Ekberg H, Tedesco-Silva H, Demirbas A, Reduced exposure to calcineurin inhibitors in renal transplantation. N Engl J Med 2007;357:2562-75
  • Flechner SM, Glyda M, Cockfield S, The ORION study: comparison of two sirolimus-based regimens versus tacrolimus and mycophenolate mofetil in renal allograft recipients. Am J Transplant 2011;11:1633-44
  • Asberg A, Midtvedt K, Line PD, Calcineurin inhibitor avoidance with daclizumab, mycophenolate mofetil, and prednisolone in DR-matched de novo kidney transplant recipients. Transplantation 2006;82:62-8
  • Holdaas H, Bentdal O, Pfeffer P, Early, abrupt conversion of de novo renal transplant patients from cyclosporine to everolimus: results of a pilot study. Clin Transplant 2008;22:366-71
  • Mjörnstedt L, Sørensen SS, von zur Mühlen B, Improved renal function after early conversion from a calcineurin inhibitor to everolimus: a randomized trial in kidney transplantation. Am J Transplant 2012; In press
  • Schena FP, Pascoe MD, Alberu J, Conversion from calcineurin inhibitors to sirolimus maintenance therapy in renal allograft recipients: 24-month efficacy and safety results from the CONVERT trial. Transplantation 2009;87:233-42
  • Budde K, Becker T, Arns W, Everolimus-based, calcineurin-inhibitor-free regimen in recipients of de-novo kidney transplants: an open-label, randomised, controlled trial. Lancet 2011;377:837-47
  • Budde K, Arns W, Sommerer C, Improved renal function of an everolimus/enteric coated mychophenolate sodium regimen after calcineurin inhibitor withdrawal in De Novo renal transplant patients: 3 years follow-up of the ZEUS trial. Am J Transplant 2011;11(Suppl 2):66
  • Bemelman FJ, de Maar EF, Press RR, Minimization of maintenance immunosuppression early after renal transplantation: an interim analysis. Transplantation 2009;88:421-8
  • Holdaas H, Rostaing L, Seron D, Conversion of long-term kidney transplant recipients from calcineurin inhibitor therapy to everolimus: a randomized, multicenter, 24-month study. Transplantation 2011;92:410-18
  • Vajdic CM, McDonald SP, McCredie MR, Cancer incidence before and after kidney transplantation. JAMA 2006;296:2823-31
  • Pilmore H, Dent H, Chang S, Reduction in cardiovascular death after kidney transplantation. Transplantation 2010;89:851-7
  • Kahan BD. Cyclosporine. N Engl J Med 1989;321:1725-38
  • Hojo M, Morimoto T, Maluccio M, Cyclosporine induces cancer progression by a cell-autonomous mechanism. Nature 1999;397:530-4
  • Maluccio M, Sharma V, Lagman M, Tacrolimus enhances transforming growth factor-beta1 expression and promotes tumor progression. Transplantation 2003;76:597-602
  • Dantal J, Hourmant M, Cantarovich D, Effect of long-term immunosuppression in kidney-graft recipients on cancer incidence: randomised comparison of two cyclosporin regimens. Lancet 1998;351:623-8
  • Geissler EK, Schlitt HJ, Thomas G. mTOR, cancer and transplantation. Am J Transplant 2008;8:2212-18
  • Guba M, Graeb C, Jauch KW, Geissler EK. Pro- and anti-cancer effects of immunosuppressive agents used in organ transplantation. Transplantation 2004;77:1777-82
  • Koehl GE, Andrassy J, Guba M, Rapamycin protects allografts from rejection while simultaneously attacking tumors in immunosuppressed mice. Transplantation 2004;77:1319-26
  • Kauffman HM, Cherikh WS, Cheng Y, Maintenance immunosuppression with target-of-rapamycin inhibitors is associated with a reduced incidence of de novo malignancies. Transplantation 2005;80:883-9
  • Campistol JM, Eris J, Oberbauer R, Sirolimus therapy after early cyclosporine withdrawal reduces the risk for cancer in adult renal transplantation. J Am Soc Nephrol 2006;17:581-9
  • Stallone G, Schena A, Infante B, Sirolimus for Kaposi's sarcoma in renal-transplant recipients. N Engl J Med 2005;352:1317-23
  • Campistol JM, Gutierrez-Dalmau A, Torregrosa JV. Conversion to sirolimus: a successful treatment for posttransplantation Kaposi's sarcoma. Transplantation 2004;77:760-2
  • Saggar S, Zeichner JA, Brown TT, Kaposi's sarcoma resolves after sirolimus therapy in a patient with pemphigus vulgaris. Arch Dermatol 2008;144:654-7
  • Campbell SB, Walker R, See Tai S, Randomized controlled trial of sirolimus for renal transplant recipients at high risk for nonmelanoma skin cancer. Am J Ttransplant 2012;12(5):1146-56
  • Salgo R, Gossmann J, Schofer H, Switch to a sirolimus-based immunosuppression in long-term renal transplant recipients: reduced rate of (pre-)malignancies and nonmelanoma skin cancer in a prospective, randomized, assessor-blinded, controlled clinical trial. Am J Transplant 2010;10:1385-93
  • Baselga J, Semiglazov V, van DP, Phase II randomized study of neoadjuvant everolimus plus letrozole compared with placebo plus letrozole in patients with estrogen receptor-positive breast cancer. J Clin Oncol 2009;27:2630-7
  • Pavel E, Hainswroth JD, Baudin E, Everolimus plus octreotide long-acting repeatable for the treatment of advanced neuroendocrine tumours associated with carcinoid syndrome (RADIANT-2): a randomised, placebo-controlled, phase 3 study. Original Text Lancet 2011;378:2005-12
  • Yao JC, Shah MH, Ito T, Everolimus for advanced pancreatic neuroendocrine tumors. N Engl J Med 2011;364:514-23
  • Motzer RJ, Escudier B, Oudard S, Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial. Lancet 2008;372:449-56
  • Fishman JA. Infection in solid-organ transplant recipients. N Engl J Med 2007;357:2601-14
  • Sagedal S, Nordal KP, Hartmann A, The impact of cytomegalovirus infection and disease on rejection episodes in renal allograft recipients. Am J Transplant 2002;2:850-6
  • Brennan DC, Legendre C, Patel D, Cytomegalovirus incidence between everolimus versus mycophenolate in de novo renal transplants: pooled analysis of three clinical trials. Am J Transplant 2011;11:2453-62
  • Eisen HJ, Tuzcu EM, Dorent R, Everolimus for the prevention of allograft rejection and vasculopathy in cardiac-transplant recipients. N Engl J Med 2003;349:847-58
  • Hill JA, Hummel M, Starling RC, A lower incidence of cytomegalovirus infection in de novo heart transplant recipients randomized to everolimus. Transplantation 2007;84:1436-42
  • Sabe N, Gonzales-Costello J, Rama I, Successful outcome of ganciclovir-resistant cytomegalovirus infection in organ transplant recipients after conversion to mTOR inhibitors. Transplant Int 2012;25(7):e78-82
  • Clippinger AJ, Maguire TG, Alwine JC. The changing role of mTOR kinase in the maintenance of protein synthesis during human cytomegalovirus infection. J Virol 2011;85:3930-9
  • Moorman NJ, Shenk T. Rapamycin-resistant mTORC1 kinase activity is required for herpesvirus replication. J Virol 2010;84:5260-9
  • Egli A, Infanti L, Dumoulin A, Prevalence of polyomavirus BK and JC infection and replication in 400 healthy blood donors. J Infect Dis 2009;199:837-46
  • Egli A, Kohli S, Dickenmann M, Hirsch HH. Inhibition of polyomavirus BK-specific T-Cell responses by immunosuppressive drugs. Transplantation 2009;88:1161-8
  • Liacini A, Seamone ME, Muruve DA, Tibbles LA. Anti-BK virus mechanisms of sirolimus and leflunomide alone and in combination: toward a new therapy for BK virus infection. Transplantation 2010;90:1450-7
  • Jardine AG, Gaston RS, Fellstrom BC, Holdaas H. Prevention of cardiovascular disease in adult recipients of kidney transplants. Lancet 2011;378:1419-27
  • Holdaas H, Fellstrom B, Jardine AG, Effect of fluvastatin on cardiac outcomes in renal transplant recipients: a multicentre, randomised, placebo-controlled trial. Lancet 2003;361:2024-31
  • Holdaas H, Fellstrom B, Cole E, Long-term cardiac outcomes in renal transplant recipients receiving fluvastatin: the ALERT extension study. Am J Transplant 2005;5:2929-36
  • Kasiske BL, de MA, Flechner SM, Mammalian target of rapamycin inhibitor dyslipidemia in kidney transplant recipients. Am J Transplant 2008;8:1384-92
  • Kidney Disease: improving global outcomes (KDIGO) Transplant working group. KDIGO clinical practice guideline for the care of kidney transplant recipients. Am J Transplant 2009;9(Suppl 3):S1-157
  • Blum CB. Effects of sirolimus on lipids in renal allograft recipients: an analysis using the Framingham risk model. Am J Transplant 2002;2:551-9
  • Johnston O, Rose CL, Webster AC, Gill JS. Sirolimus is associated with new-onset diabetes in kidney transplant recipients. J Am Soc Nephrol 2008;19:1411-18
  • Midtvedt K, Ihlen H, Hartmann A, Reduction of left ventricular mass by lisinopril and nifedipine in hypertensive renal transplant recipients: a prospective randomized double-blind study. Transplantation 2001;72:107-11
  • Siedlecki A, Foushee M, Curtis JJ, The impact of left ventricular systolic dysfunction on survival after renal transplantation. Transplantation 2007;84:1610-17
  • Atkison P, Joubert G, Barron A, Hypertrophic cardiomyopathy associated with tacrolimus in paediatric transplant patients. Lancet 1995;345:894-6
  • McMullen JR, Sherwood MC, Tarnavski O, Inhibition of mTOR signaling with rapamycin regresses established cardiac hypertrophy induced by pressure overload. Circulation 2004;109:3050-5
  • Paoletti E, Marsano L, Bellino D, Effect of everolimus on left ventricular hypertrophy of de novo kidney transplant recipients: a 1 year, randomized, controlled trial. Transplantation 2012;93:503-8
  • Friedman AN, Rosenberg IH, Selhub J, Hyperhomocysteinemia in renal transplant recipients. Am J Transplant 2002;2:308-13
  • Bostom AG, Carpenter MA, Kusek JW, Homocysteine-lowering and cardiovascular disease outcomes in kidney transplant recipients: primary results from the Folic Acid for Vascular Outcome Reduction in Transplantation trial. Circulation 2011;123:1763-70
  • Farsetti S, Zanazzi M, Caroti L, Lower homocysteine levels in renal transplant recipients treated with everolimus: a possible link with a decreased cardiovascular risk? Transplant Proc 2010;42:1381-2
  • Rostaing L, Kamar N. mTOR inhibitor/proliferation signal inhibitors: entering or leaving the field? J Nephrol 2010;23:133-42
  • Duran I, Siu LL, Oza AM, Characterisation of the lung toxicity of the cell cycle inhibitor temsirolimus. Eur J Cancer 2006;42:1875-80
  • Cho D, Signoretti S, Regan M, The role of mammalian target of rapamycin inhibitors in the treatment of advanced renal cancer. Clin Cancer Res 2007;13:758s-63s
  • Porta C, Osanto S, Ravaud A, Management of adverse events associated with the use of everolimus in patients with advanced renal cell carcinoma. Eur J Cancer 2011;47:1287-98
  • Rehm B, Keller F, Mayer J, Stracke S. Resolution of sirolimus-induced pneumonitis after conversion to everolimus. Transplant Proc 2006;38:711-13
  • Loriga G, Ciccarese M, Pala PG, De novo everolimus-based therapy in renal transplant recipients: effect on proteinuria and renal prognosis. Transplant Proc 2010;42:1297-302
  • Schonenberger E, Ehrich JH, Haller H, Schiffer M. The podocyte as a direct target of immunosuppressive agents. Nephrol Dial Transplant 2011;26:18-24
  • Franz S, Regeniter A, Hopfer H, Tubular toxicity in sirolimus- and cyclosporine-based transplant immunosuppression strategies: an ancillary study from a randomized controlled trial. Am J Kidney Dis 2010;55:335-43
  • Diekmann F, Budde K, Oppenheimer F, Predictors of success in conversion from calcineurin inhibitor to sirolimus in chronic allograft dysfunction. Am J Transplant 2004;4:1869-75
  • Letavernier E, Legendre C. mToR inhibitors-induced proteinuria: mechanisms, significance, and management. Transplant Rev (Orlando) 2008;22:125-30
  • Stallone G, Infante B, Grandaliano G, Gesualdo L. Management of side effects of sirolimus therapy. Transplantation 2009;87:S23-6
  • Yatscoff RW, Fryer J, Thliveris JA. Comparison of the effect of rapamycin and FK506 on release of prostacyclin and endothelin in vitro. Clin Biochem 1993;26:409-14
  • Mahe E, Morelon E, Lechaton S, Cutaneous adverse events in renal transplant recipients receiving sirolimus-based therapy. Transplantation 2005;79:476-82
  • Montalbano M, Neff GW, Yamashiki N, A retrospective review of liver transplant patients treated with sirolimus from a single center: an analysis of sirolimus-related complications. Transplantation 2004;78:264-8
  • Chuang P, Langone AJ. Clobetasol ameliorates aphthous ulceration in renal transplant patients on sirolimus. Am J Transplant 2007;7:714-17
  • Huyghe E, Zairi A, Nohra J, Gonadal impact of target of rapamycin inhibitors (sirolimus and everolimus) in male patients: an overview. Transpl Int 2007;20:305-11
  • Zuber J, Anglicheau D, Elie C, Sirolimus may reduce fertility in male renal transplant recipients. Am J Transplant 2008;8:1471-9
  • Boobes Y, Bernieh B, Saadi H, Gonadal dysfunction and infertility in kidney transplant patients receiving sirolimus. Int Urol Nephrol 2010;42:493-8
  • Dean PG, Lund WJ, Larson TS, Wound-healing complications after kidney transplantation: a prospective, randomized comparison of sirolimus and tacrolimus. Transplantation 2004;77:1555-61
  • Albano L, Berthoux F, Moal MC, Incidence of delayed graft function and wound healing complications after deceased-donor kidney transplantation is not affected by de novo everolimus. Transplantation 2009;88:69-76
  • Mehrabi A, Fonouni H, Wente M, Wound complications following kidney and liver transplantation. Clin Transplant 2006;20(Suppl 17):97-110
  • Valente JF, Hricik D, Weigel K, Comparison of sirolimus vs. mycophenolate mofetil on surgical complications and wound healing in adult kidney transplantation. Am J Transplant 2003;3:1128-34
  • Humar A, Ramcharan T, Denny R, Are wound complications after a kidney transplant more common with modern immunosuppression? Transplantation 2001;72:1920-3
  • Ojo AO, Held PJ, Port FK, Chronic renal failure after transplantation of a nonrenal organ. N Engl J Med 2003;349:931-40
  • Powles AV, Cook T, Hulme B, Renal function and biopsy findings after 5 years' treatment with low-dose cyclosporin for psoriasis. Br J Dermatol 1993;128:159-65
  • Sellares J, de Freitas DG, Mengel M, Inflammation lesions in kidney transplant biopsies: association with survival is due to the underlying diseases. Am J Transplant 2011;11:489-99

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.