Population pharmacokinetics of everolimus in cardiac recipients: Comedications, ABCB1, and CYP3A5 polymorphisms

Therapeutic Drug Monitoring

Volumn 34, Issue 6, 2012, Pages 686-694

  Lemaitre, Florian ^a,b   Bezian, Elodie ^a   Goldwirt, Lauriane ^a,b   Fernandez, Christine ^a,b   Farinotti, Robert ^a,b   Varnous, Shaida ^a   Urien, Saik ^c   Antignac, Marie ^a  

^a ASSISTANCE PUBLIQUE HÔPITAUX DE PARIS   (France)

^b EA4123   (France)

^c UNIVERSITÉ PARIS DESCARTES   (France)

Author keywords

everolimus; heart transplantation; immunosuppressive drugs; pharmacokinetics; population pharmacokinetics

Indexed keywords

AZATHIOPRINE; CYCLOSPORIN; CYTOCHROME P450 3A5; EVEROLIMUS; MULTIDRUG RESISTANCE PROTEIN 1; MYCOPHENOLIC ACID 2 MORPHOLINOETHYL ESTER; PREDNISOLONE; PREDNISONE; TACROLIMUS;

ADOLESCENT; ADULT; AGED; ARTICLE; BLOOD SAMPLING; BOOTSTRAPPING; CARDIAC GRAFT REJECTION; CLINICAL ARTICLE; CLINICAL TRIAL; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; FEMALE; GRAFT RECIPIENT; HEART TRANSPLANTATION; HUMAN; HYPERBILIRUBINEMIA; IMMUNOSUPPRESSIVE TREATMENT; MALE; PRIORITY JOURNAL; SINGLE NUCLEOTIDE POLYMORPHISM;

ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; ALLELES; CYTOCHROME P-450 CYP3A; DRUG INTERACTIONS; FEMALE; FOLLOW-UP STUDIES; GENETIC ASSOCIATION STUDIES; GRAFT REJECTION; HEART TRANSPLANTATION; HUMANS; IMMUNOSUPPRESSIVE AGENTS; MALE; MIDDLE AGED; P-GLYCOPROTEIN; PARIS; POLYMORPHISM, SINGLE NUCLEOTIDE; PROSPECTIVE STUDIES; SIROLIMUS; YOUNG ADULT;

EID: 84870067029     PISSN: 01634356     EISSN: 15363694     Source Type: Journal    
DOI: 10.1097/FTD.0b013e318273c899     Document Type: Article

References (34)

1. Kirchner GI, Meier-Wiedenbach I, Manns MP. Clinical pharmacokinetics of everolimus. Clin Pharmacokinet. 2004;43:83-95. (Pubitemid 38283132)
2. Eisen HJ, Tuzcu EM, Dorent R, et al; RAD B253 Study Group. Everolimus for the prevention of allograft rejection and vasculopathy in cardiac-Transplant recipients. N Engl J Med. 2003;349:847-858. (Pubitemid 37025404)
3. Lehmkuhl HB, Mai D, Dandel M, et al. Observational study with everolimus (Certican) in combination with low-dose cyclosporine in de novo heart transplant recipients. J Heart Lung Transplant. 2007;26:700-704. (Pubitemid 47007710)
4. Nashan B, Curtis J, Ponticelli C, et al; 156 Study Group. Everolimus and reduced-exposure cyclosporine in de novo renal-Transplant recipients: a three-year phase II, randomized, multicenter, open-label study. Transplantation. 2004;78:1332-1340.
5. Vitko S, Tedesco H, Eris J, et al. Everolimus with optimized cyclosporine dosing in renal transplant recipients: 6-month safety and efficacy results of two randomized studies. Am J Transplant. 2004;4:626-635. (Pubitemid 38523586)
6. Motzer RJ, Escudier B, Oudard S, et al. Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebocontrolled phase III trial. Lancet. 2008;372:449-456.
7. Yao JC, Chan MH, Ito T, et al. Everolimus for advanced pancreatic neuroendocrine tumors. N Engl J Med. 2011;364:514-523.
8. Starling RC, Hare JM, Hauptman P, et al. Therapeutic drug monitoring for everolimus in heart transplant recipients based on exposure-effect modeling. Am J Transplant. 2004;4:2126-2131.
9. Chan L, Hartmann E, Cibrik D, et al. Optimal everolimus concentration is associated with risk reduction for acute rejection in de novo renal transplant recipients. Transplantation. 2010;90:31-37.
10. Monchaud C, Marquet P. Pharmacokinetic optimisation of immunossupressive therapy in thoracic transplantation: part II. Clin Pharmacokinet. 2009;48:489-516.
11. Kovarik JM, Kaplan B, Tedesco Silva H, et al. Exposure-response relationships for everolimus in de novo kidney transplantation: defining a therapeutic range. Transplantation. 2002;73:920-925.
12. Certican-[package insert]. Vidal medical dictionary, France; 2010.
13. Kovarik JM, Eisen H, Dorent R, et al. Everolimus in de novo cardiac transplantation: pharmacokinetics, therapeutic range, and influence on cyclosporine exposure. J Heart Lung Transplant. 2003;22:1117-1125.
14. Brignol N, McMahon LM, Luo S, et al. High-Throughput semi-Automated 96-well liquid/liquid extraction and liquid chromatography/mass spectrometric analysis of everolimus (RAD 001) and cyclosporin a (CsA) in whole blood. Rapid Commun Mass Spectrom. 2001;15:898-907.
15. Strom T, Haschke M, Boyd J, et al. Crossreactivity of isolated everolimus metabolites with the Innofluor Certican immunoassay for therapeutic drug monitoring of everolimus. Ther Drug Monit. 2007;29: 743-749.
16. Le Meur Y, Djebli N, Szelag JC, et al. CYP3A53 influences sirolimus oral clearance in de novo and stable renal transplant recipients. Clin Pharmacol Ther. 2006;80:51-60.
17. Boekmann AJ, Sheiner LB, Beal SL. NONMEM User's Guide: Part V. Introductory Guide. San Francisco, CA: University of California; 1992.
18. Kovarik JM, Hsu CH, McMahon L, et al. Population pharmacokinetics of everolimus in de novo renal transplant patients: impact of ethnicity and comedications. Clin Pharmacol Ther. 2001;70:247-254.
19. Parke J, Holford NH, Charles BG. A procedure for generating bootstrap samples for the validation of nonlinear mixed-effects population models. Comput Methods Programs Biomed. 1999;59:19-29.
20. Kovarik JM, Sabia HD, Figueiredo J, et al. Influence of hepatic impairment on everolimus pharmacokinetics: implications for dose adjustment. Clin Pharmacol Ther. 2001;70:425-430.
21. Kovarik JM, Kalbag J, Figueiredo J, et al. Differential influence of two cyclosporine formulations on everolimus pharmacokinetics: a clinically relevant pharmacokinetic interaction. J Clin Pharmacol. 2002;42:95-99. (Pubitemid 34038374)
22. MacPhee IA, Fredericks S, Tai T, et al. The influence of pharmacogenetics on the time to achieve target tacrolimus concentrations after kidney transplantation. Am J Transplant. 2004;4:914-919. (Pubitemid 38745590)
23. Jacobsen W, Serkova N, Hausen B, et al. Comparison of the in vitro metabolism of the macrolide immunosuppressants sirolimus and RAD. Transplant Proc. 2001;33:514-515. (Pubitemid 32237488)
24. Kovarik JM, Hartmann S, Figueiredo J, et al. Effect of rifampin on apparent clearance of everolimus. Ann Pharmacother. 2002;36:981-985.
25. Kovarik JM, Beyer D, Bizot MN, et al. Blood concentrations of everolimus are markedly increased by ketoconazole. J Clin Pharmacol. 2005; 45:514-518.
26. Picard N, Rouguieg-Malki K, Kamar N, et al. CYP3A5 genotype does not influence everolimus in vitro metabolism and clinical pharmacokinetics in renal transplant recipients. Transplantation. 2011;91:652-656.
27. Chinn LW, Kroetz DL. ABCB1 pharmacogenetics: progress, pitfalls, and promise. Clin Pharmacol Ther. 2007;81:265-269.
28. Staatz CE, Goodman LK, Tett SE. Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors: part I. Clin Pharmacokinet. 2010;49: 141-175.
29. Antignac M, Barrou B, Farinotti R, et al. Population pharmacokinetics and bioavailability of tacrolimus in kidney transplant patients. Br J Clin Pharmacol. 2007;64:750-757. (Pubitemid 350222052)
30. Kovarik JM, Curtis JJ, Hricik DE, et al. Differential pharmacokinetic interaction of tacrolimus and cyclosporine on everolimus. Transplant Proc. 2006;38:3456-3458.
31. Brandhorst G, Tenderich G, Zittermann A, et al. Everolimus exposure in cardiac transplant recipients is influenced by concomitant calcineurin inhibitor. Ther Drug Monit. 2008;30:113-116.
32. Murthy JN, Davis DL, Yatscoff RW, et al. Tacrolimus metabolite crossreactivity in different tacrolimus assays. Clin Biochem. 1998;31: 613-617.
33. D'Alessandro M, Mariani P, Mennini G, et al. Falsely elevated tacrolimus concentrations measured using the ACMIA method due to circulating endogenous antibodies in a kidney transplant recipient. Clin Chim Acta. 2011;412:245-248.
34. Dailly E, Deslandes G, Hourmant M, et al. Comparison between a liquid chromatography-Tandem mass spectrometry assay and a fluorescent polarization immunoassay to measure whole blood everolimus concentration in heart and renal transplantations. J Clin Lab Anal. 2008;22: 282-285.