nach oben

Journal of Nephrology

Erschienen in:

01.02.2017 | Review

Once-daily prolonged-release tacrolimus formulations for kidney transplantation: what the nephrologist needs to know

verfasst von: Giovanni Piotti, Elena Cremaschi, Umberto Maggiore

Erschienen in: Journal of Nephrology | Ausgabe 1/2017

Einloggen, um Zugang zu erhalten

Abstract

Tacrolimus has long been the cornerstone of the immunosuppressive standard-of-care in kidney transplantation. Until recently, only an immediate-release formulation of tacrolimus was available in the clinic for twice-daily administration, a schedule that is known to hamper prescription adherence and contributes to the already significant tacrolimus interactions with other drugs and meals. In order to improve patient compliance, two once-daily prolonged-release formulations of tacrolimus have recently been developed and approved. Here we will analyze the main characteristics of these two prolonged-release formulations with the aim to provide practical clinical information for a fully aware drug prescription. Finally, the theoretical advantages of the prolonged-release formulations in terms of prescription adherence, blood level steadiness and drug efficacy and tolerability will be critically reviewed, in order to define the profile of renal recipients who may benefit most from the switch to once-daily tacrolimus.

Kidney Disease: Improving Global Outcomes (KDIGO) Transplant Work Group (2009) KDIGO clinical practice guideline for the care of kidney transplant recipients. Am J Transplant 9(Suppl 3):S1–S155. doi:10.1111/j.1600-6143.2009.02834.x

Ekberg H, Tedesco-Silva H, Demirbas A et al (2007) Reduced exposure to calcineurin inhibitors in renal transplantation. N Engl J Med 357(25):2562–2575CrossRefPubMed

Webster AC, Woodroffe RC, Taylor RS, Chapman JR, Craig JC (2005) Tacrolimus versus ciclosporin as primary immunosuppression for kidney transplant recipients: meta-analysis and meta-regression of randomised trial data. BMJ 331(7520):810CrossRefPubMedPubMedCentral

Hart A, Smith JM, Skeans MA et al (2016) OPTN/SRTR annual data report 2014. Am J Transplant 16(S2):11–46. doi:10.1111/ajt.13666 (Special Issue) CrossRefPubMed

Halloran PF (2004) Immunosuppressive drugs for kidney transplantation. N Engl J Med 351(26):2715–2729CrossRefPubMed

Provenzani A, Santeusanio A, Mathis E et al (2013) Pharmacogenetic considerations for optimizing tacrolimus dosing in liver and kidney transplant patients. World J Gastroenterol 19(48):9156–9173. doi:10.3748/wjg.v19.i48.9156 CrossRefPubMedPubMedCentral

Grinyó JM, Petruzzelli S (2014) Once-daily LCP-Tacro MeltDose tacrolimus for the prophylaxis of organ rejection in kidney and liver transplantations. Expert Rev Clin Immunol. 10(12):1567–1579. doi:10.1586/1744666X.2014.983903 CrossRefPubMed

Garnock-Jones KP (2015) Tacrolimus prolonged release (Envarsus^®): a review of its use in kidney and liver transplant recipients. Drugs 75(3):309–320. doi:10.1007/s40265-015-0349-2 CrossRefPubMed

www.fda.gov/downloads/Drug/GuidanceComplianceRegulatoryInformation/Guidance/UCM181006.pdf. Accessed 16 Mar 2016

10.

Staatz CE, Tett SE (2004) Clinical pharmacokinetics and pharmacodynamics of tacrolimus in solid organ transplantation. Clin Pharmacokinet 43(10):623–653CrossRefPubMed

11.

Prograf (2013) Prescribing information. Astellas Pharma US, Inc; Northbrook

12.

Ekberg H, Bernasconi C, Tedesco-Silva H et al (2009) Calcineurin inhibitor minimization in the Symphony study: observational results 3 years after transplantation. Am J Transplant 9(8):1876–1885. doi:10.1111/j.1600-6143.2009.02726.x CrossRefPubMed

13.

Malvezzi P, Rostaing L (2015) The safety of calcineurin inhibitors for kidney-transplant patients. Expert Opin Drug Saf 14(10):1531–1546. doi:10.1517/14740338.2015.1083974 CrossRefPubMed

14.

Cippà PE, Schiesser M, Ekberg H et al (2015) Risk stratification for rejection and infection after kidney transplantation. Clin J Am Soc Nephrol 10(12):2213–2220. doi:10.2215/CJN.01790215 CrossRefPubMedPubMedCentral

15.

Vanhove T, Annaert P, Kuypers DR (2016) Clinical determinants of calcineurin inhibitor disposition: a mechanistic review. Drug Metab Rev 48(1):88–112. doi:10.3109/03602532.2016.1151037 CrossRefPubMed

16.

Paine MF, Khalighi M, Fisher JM et al (1997) Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 283(3):1552–1562PubMed

17.

Masuda S, Uemoto S, Goto M, Fujimoto Y, Tanaka K, Inui K (2004) Tacrolimus therapy according to mucosal MDR1 levels in small-bowel transplant recipients. Clin Pharmacol Ther 75(4):352–361CrossRefPubMed

18.

Christians U, Jacobsen W, Benet LZ, Lampen A (2002) Mechanisms of clinically relevant drug interactions associated with tacrolimus. Clin Pharmacokinet 41(11):813–851CrossRefPubMed

19.

Nowack R (2008) Herb-drug interactions in nephrology: documented and theoretical. Clin Nephrol 69(5):319–325CrossRefPubMed

20.

Bekersky I, Dressler D, Mekki QA (2001) Effect of low- and high-fat meals on tacrolimus absorption following 5 mg single oral doses to healthy human subjects. J Clin Pharmacol 41(2):176–182CrossRefPubMed

21.

Park SI, Felipe CR, Pinheiro-Machado PG, Garcia R, Tedesco-Silva H Jr, Medina-Pestana JO (2007) Circadian and time-dependent variability in tacrolimus pharmacokinetics. Fundam Clin Pharmacol 21(2):191–197CrossRefPubMed

22.

http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000712/WC500022237.pdf. Accessed 16 Mar 2016

23.

http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000712/WC500022234.pdf. Accessed 16 Mar 2016

24.

MeltDose^® Technology by the US Patent and Trademark Office. US7217431

25.

Nigro V, Glicklich A, Weinberg J (2013) Improved bioavailability of MELTDOSE once-daily formulation of tacrolimus (LCP-Tacro) with controlled agglomeration allows for consistent absorption over 24 Hrs: a scintigraphic and pharmacokinetic evaluation. Am J Transplant. Poster, Abstract# B1034

26.

http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002655/WC500170412.pdf. Accessed 16 Mar 2016

27.

Staatz CE, Tett SE (2015) Clinical pharmacokinetics of once-daily tacrolimus in solid-organ transplant patients. Clin Pharmacokinet 54(10):993–1025. doi:10.1007/s40262-015-0282-2 CrossRefPubMed

28.

de Jonge H, Kuypers DR, Verbeke K, Vanrenterghem Y (2010) Reduced C0 concentrations and increased dose requirements in renal allograft recipients converted to the novel once-daily tacrolimus formulation. Transplantation 90(5):523–529. doi:10.1097/TP.0b013e3181e9feda CrossRefPubMed

29.

Wu MJ, Cheng CY, Chen CH et al (2011) Lower variability of tacrolimus trough concentration after conversion from prograf to advagraf in stable kidney transplant recipients. Transplantation 92(6):648–652. doi:10.1097/TP.0b013e3182292426 CrossRefPubMed

30.

Hougardy JM, Broeders N, Kianda M et al (2011) Conversion from Prograf to Advagraf among kidney transplant recipients results in sustained decrease in tacrolimus exposure. Transplantation 91(5):566–569. doi:10.1097/TP.0b013e3182098ff0 CrossRefPubMed

31.

Gaber AO, Alloway RR, Bodziak K, Kaplan B, Bunnapradist S (2013) Conversion from twice-daily tacrolimus capsules to once-daily extended-release tacrolimus (LCPT): a phase 2 trial of stable renal transplant recipients. Transplantation 96(2):191–197. doi:10.1097/TP.0b013e3182962cc1 CrossRefPubMedPubMedCentral

32.

Alloway RR, Eckhoff DE, Washburn WK, Teperman LW (2014) Conversion from twice daily tacrolimus capsules to once daily extended-release tacrolimus (LCP-Tacro): phase 2 trial of stable liver transplant recipients. Liver Transpl 20(5):564–575. doi:10.1002/lt.23844 CrossRefPubMed

33.

Barraclough KA, Isbel NM, Johnson DW, Campbell SB, Staatz CE (2011) Once- versus twice-daily tacrolimus: are the formulations truly equivalent? Drugs 71(12):1561–1577. doi:10.2165/11593890-000000000-00000 CrossRefPubMed

34.

Alloway RR, Mulgaonkar S, Ueda D, et al (2011) A phase 2b, open-label, multi-center, prospective, randomized study to compare the pharmacokinetics and safety of LCP-Tacro™ tablets once-a-day to Prograf^® capsules twice-a-day in de novo kidney transplant patients. Am J Transplant. Poster, Abstratct #1106

35.

Niioka T, Satoh S, Kagaya H et al (2012) Comparison of pharmacokinetics and pharmacogenetics of once- and twice-daily tacrolimus in the early stage after renal transplantation. Transplantation 94(10):1013–1019. doi:10.1097/TP.0b013e31826bc400 CrossRefPubMed

36.

Tsuchiya T, Ishida H, Tanabe T et al (2013) Comparison of pharmacokinetics and pathology for low-dose tacrolimus once-daily and twice-daily in living kidney transplantation: prospective trial in once-daily versus twice-daily tacrolimus. Transplantation 96(2):198–204. doi:10.1097/TP.0b013e318296c9d5 CrossRefPubMed

37.

Stifft F, Stolk LM, Undre N, van Hooff JP, Christiaans MH (2014) Lower variability in 24-hour exposure during once-daily compared to twice-daily tacrolimus formulation in kidney transplantation. Transplantation 97(7):775–780. doi:10.1097/01.TP.0000437561.31212.0e PubMed

38.

Hardinger KL, Hutcherson T, Preston D, Murillo D (2012) Influence of pill burden and drug cost on renal function after transplantation. Pharmacot 32(5):427–432. doi:10.1002/j.1875-9114.2012.01032.x CrossRef

39.

Sellarés J, de Freitas DG, Mengel M et al (2012) Understanding the causes of kidney transplant failure: the dominant role of antibody-mediated rejection and nonadherence. Am J Transplant 12(2):388–399. doi:10.1111/j.1600-6143.2011.03840.x CrossRefPubMed

40.

Tielen M, van Exel J, Laging M et al (2014) Attitudes to medication after kidney transplantation and their association with medication adherence and graft survival: a 2-year follow-up study. J Transplant. doi:10.1155/2014/675301 PubMedPubMedCentral

41.

Shuker N, van Gelder T, Hesselink DA (2015) Intra-patient variability in tacrolimus exposure: causes, consequences for clinical management. Transplant Rev 9(2):78–84. doi:10.1016/j.trre.2015.01.002 CrossRef

42.

Claxton AJ, Cramer J, Pierce C (2001) A systematic review of the associations between dose regimens and medication compliance. J Clin Ther 23(8):1296–1310CrossRef

43.

Obi Y, Ichimaru N, Kato T et al (2013) A single daily dose enhances the adherence to immunosuppressive treatment in kidney transplant recipients: a cross-sectional study. Clin Exp Nephrol. 17(2):310–315. doi:10.1007/s10157-012-0713-4 CrossRefPubMed

44.

Kuypers DR, Peeters PC, Sennesael JJ et al (2013) Improved adherence to tacrolimus once-daily formulation in renal recipients: a randomized controlled trial using electronic monitoring. Transplantation 95(2):333–340. doi:10.1097/TP.0b013e3182725532 CrossRefPubMed

45.

van Boekel GA, Kerkhofs CH, Hilbrands LB (2013) Treatment satisfaction in renal transplant patients taking tacrolimus once daily. Clin Ther 35(11):1821–1829. doi:10.1016/j.clinthera.2013.09.014 CrossRefPubMed

46.

Singh N, Von Visger J, Zachariah M (2015) Extended release once a day tacrolimus. Curr Opin Organ Transplant. 20(6):657–662. doi:10.1097/MOT.0000000000000251 CrossRefPubMed

47.

Butler JA, Peveler RC, Roderick P, Horne R, Mason JC (2004) Measuring compliance with drug regimens after renal transplantation: comparison of self-report and clinician rating with electronic monitoring. Transplantation 77(5):786–789CrossRefPubMed

48.

Muduma G, Shaw J, Hart WM, Odeyemi A, Odeyemi I (2014) Cost utility analysis of immunosuppressive regimens in adult renal transplant recipients in England and Wales. Pat Pre Adher 8:1537–1546. doi:10.2147/PPA.S69461

49.

Hardinger KL, Park JM, Schnitzler MA, Koch MJ, Miller BW, Brennan DC (2004) Pharmacokinetics of tacrolimus in kidney transplant recipients: twice daily versus once daily dosing. Am J Transplant 4(4):621–625CrossRefPubMed

50.

Alloway R, Steinberg S, Khalil K et al (2005) Conversion of stable kidney transplant recipients from a twice daily Prograf-based regimen to a once daily modified release tacrolimus-based regimen. Transplant Proc. 37(2):867–870CrossRefPubMed

51.

van Hooff J, Van der Walt I, Kallmeyer J et al (2012) Pharmacokinetics in stable kidney transplant recipients after conversion from twice-daily to once-daily tacrolimus formulations. Ther Drug Monit 34(1):46–52. doi:10.1097/FTD.0b013e318244a7fd CrossRefPubMed

52.

Borra LC, Roodnat JI, Kal JA, Mathot RA, Weimar W, van Gelder T (2010) High within-patient variability in the clearance of tacrolimus is a risk factor for poor long-term outcome after kidney transplantation. Nephrol Dial Transplant 25(8):2757–2763. doi:10.1093/ndt/gfq096 CrossRefPubMed

53.

Revollo J (2015) Update on the clinical utility of once-daily tacrolimus in the management of transplantation. Drug Des Dev Ther 9:2581–2583. doi:10.2147/DDDT.S84301 CrossRef

54.

Niioka T, Kagaya H, Miura M et al (2013) Pharmaceutical and genetic determinants for interindividual differences of tacrolimus bioavailability in renal transplant recipients. Eur J Clin Pharmacol 69(9):1659–1665. doi:10.1007/s00228-013-1514-8 CrossRefPubMed

55.

Posadas Salas MA, Srinivas TR (2014) Update on the clinical utility of once-daily tacrolimus in the management of transplantation. Drug Des Dev Ther 8:1183–1194. doi:10.2147/DDDT.S55458 CrossRef

56.

Silva HT Jr, Yang HC, Abouljoud M et al (2007) One-year results with extended-release tacrolimus/MMF, tacrolimus/MMF and cyclosporine/MMF in de novo kidney transplant recipients. Am J Transpl 7(3):595–608CrossRef

57.

Silva HT Jr, Yang HC, Meier-Kriesche HU et al (2014) Long-term follow-up of a phase III clinical trial comparing tacrolimus extended-release/MMF, tacrolimus/MMF, and cyclosporine/MMF in de novo kidney transplant recipients. Transplantation 97(6):636–641. doi:10.1097/01.TP.0000437669.93963.8E CrossRefPubMedPubMedCentral

58.

Krämer BK, Charpentier B, Bäckman L et al (2010) Tacrolimus once daily (ADVAGRAF) versus twice daily (PROGRAF) in de novo renal transplantation: a randomized phase III study. Am J Transplant 10(12):2632–2643. doi:10.1111/j.1600-6143.2010.03256.x CrossRefPubMed

59.

Han DJ, Park JB, Kim YS et al (2012) A 39-month follow-up study to evaluate the safety and efficacy in kidney transplant recipients treated with modified-release tacrolimus (FK506E)-based immunosuppression regimen. Transpl Proc 44(1):115–117. doi:10.1016/j.transproceed.2011.12.070 CrossRef

60.

Albano L, Banas B, Klempnauer JL, Glyda M, Viklicky O, Kamar N (2013) OSAKA trial: a randomized, controlled trial comparing tacrolimus QD and BD in kidney transplantation. Transplantation 96(10):897–903. doi:10.1097/TP.0b013e3182a203bd CrossRefPubMedPubMedCentral

61.

Bunnapradist S, Ciechanowski K, West-Thielke P et al (2013) Conversion from twice-daily tacrolimus to once-daily extended release tacrolimus (LCPT): the phase III randomized MELT trial. Am J Transpl 13(3):760–769. doi:10.1111/ajt.12035 CrossRef

62.

Budde K, Bunnapradist S, Grinyó JM et al (2014) Novel once-daily extended-release tacrolimus (LCPT) versus twice-daily tacrolimus in de novo kidney transplants: one-year results of Phase III, double-blind, randomized trial. Am J Transpl 14(12):2796–2806. doi:10.1111/ajt.12955 CrossRef

63.

Rostaing L, Bunnapradist S, Grinyó JM et al (2016) Novel once-daily extended-release tacrolimus versus twice-daily tacrolimus in de novo kidney transplant recipients: two-year results of phase 3, double-blind, randomized trial. Am J Kidney Dis 67(4):648–659. doi:10.1053/j.ajkd.2015.10.024 CrossRefPubMed

64.

Considine A, Tredger JM, Heneghan M et al (2015) Performance of modified-release tacrolimus after conversion in liver transplant patients indicates potentially favorable outcomes in selected cohorts. Liver Transpl 21(1):29–37. doi:10.1002/lt.24022 CrossRefPubMed

65.

Adam R, Karam V, Delvart V et al (2015) Improved survival in liver transplant recipients receiving prolonged-release tacrolimus in the European Liver Transplant Registry. Am J Transplant 15(5):1267–1282. doi:10.1111/ajt.13171 CrossRefPubMed

66.

Uchida J, Kuwabara N, Machida Y et al (2012) Conversion of stable kidney transplant recipients from a twice-daily prograf to a once-daily tacrolimus formulation: a short-term study on its effects on glucose metabolism. Transpl Proc 44(1):128–133. doi:10.1016/j.transproceed.2011.11.005 CrossRef

67.

Uchida J, Iwai T, Kabei K et al (2014) Effects of conversion from a twice-daily tacrolimus to a once-daily tacrolimus on glucose metabolism in stable kidney transplant recipients. Transpl Proc 46(2):532–536. doi:10.1016/j.transproceed.2013.11.146 CrossRef

68.

Langone A, Steinberg SM, Gedaly R et al (2015) Switching STudy of Kidney TRansplant PAtients with Tremor to LCP-TacrO (STRATO): an open-label, multicenter, prospective phase 3b study. Clin Transplant 29(9):796–805. doi:10.1111/ctr.12581 CrossRefPubMedPubMedCentral

Titel: Once-daily prolonged-release tacrolimus formulations for kidney transplantation: what the nephrologist needs to know
verfasst von: Giovanni Piotti
Elena Cremaschi
Umberto Maggiore
Publikationsdatum: 01.02.2017
Verlag: Springer International Publishing
Erschienen in: Journal of Nephrology / Ausgabe 1/2017
Print ISSN: 1121-8428
Elektronische ISSN: 1724-6059
DOI: https://doi.org/10.1007/s40620-016-0316-3

Leitlinien kompakt für die Innere Medizin

Mit medbee Pocketcards sicher entscheiden.

^{Seit 2022 gehört die medbee GmbH zum Springer Medizin Verlag}

Kostenlos registrieren

Neu im Fachgebiet Innere Medizin

Notfall-TEP der Hüfte ist auch bei 90-Jährigen machbar

26.04.2024 Hüft-TEP Nachrichten

Ob bei einer Notfalloperation nach Schenkelhalsfraktur eine Hemiarthroplastik oder eine totale Endoprothese (TEP) eingebaut wird, sollte nicht allein vom Alter der Patientinnen und Patienten abhängen. Auch über 90-Jährige können von der TEP profitieren.

Niedriger diastolischer Blutdruck erhöht Risiko für schwere kardiovaskuläre Komplikationen

25.04.2024 Hypotonie Nachrichten

Wenn unter einer medikamentösen Hochdrucktherapie der diastolische Blutdruck in den Keller geht, steigt das Risiko für schwere kardiovaskuläre Ereignisse: Darauf deutet eine Sekundäranalyse der SPRINT-Studie hin.

Bei schweren Reaktionen auf Insektenstiche empfiehlt sich eine spezifische Immuntherapie

25.04.2024 Allergien und Intoleranzreaktionen Nachrichten

Insektenstiche sind bei Erwachsenen die häufigsten Auslöser einer Anaphylaxie. Einen wirksamen Schutz vor schweren anaphylaktischen Reaktionen bietet die allergenspezifische Immuntherapie. Jedoch kommt sie noch viel zu selten zum Einsatz.

Therapiestart mit Blutdrucksenkern erhöht Frakturrisiko

25.04.2024 Hypertonie Nachrichten

Beginnen ältere Männer im Pflegeheim eine Antihypertensiva-Therapie, dann ist die Frakturrate in den folgenden 30 Tagen mehr als verdoppelt. Besonders häufig stürzen Demenzkranke und Männer, die erstmals Blutdrucksenker nehmen. Dafür spricht eine Analyse unter US-Veteranen.

Update Innere Medizin

Bestellen Sie unseren Fach-Newsletter und bleiben Sie gut informiert.

Newsletter bestellen

Springer Medizin

Abstract

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

Weitere Artikel der Ausgabe 1/2017

Association of reduced kidney function with cardiovascular disease and mortality in elderly patients: comparison between the new Berlin initiative study (BIS1) and the MDRD study equations

Relevance of ANCA positivity at the time of renal transplantation in ANCA associated vasculitis

Improved renal recovery in patients with atypical hemolytic uremic syndrome following rapid initiation of eculizumab treatment

Interpreting the results of chemical stone analysis in the era of modern stone analysis techniques

Acute renal infarction: a single center experience

Impaired maturation of distal radio-cephalic fistula for haemodialysis: a review of treatment options