COMPARATIVE PHARMACOKINETIC CHARACTERISTICS OF TACROLIMUS FOLLOWING APPLICATION OF ITS DIFFERENT PHARMACEUTICAL FORMULATIONS IN HUMANS

  • Nemanja Rančić Centar za kliničku farmakologiju; Medicinski fakultet Vojnomedicinske akademije, Univerzitet odbrane u Beogradu, Srbija
  • Viktorija Dragojević-Simić Centre for Clinical Pharmacology; Medical Faculty Military Medical Academy, University of Defence, Belgrade, Serbia
Keywords: transplantation, drug formulation, Tacrolimus, Pharmacokinetics,

Abstract


Takrolimus is a cornerstone immunosuppressant in the prevention of solid organ rejection following transplantation. After long-term use of twice daily tacrolimus, a new era of application of extended release tacrolimus for once-daily dosing ensued. The aim of this short communication was to compare pharmacokinetic characteristics of tacrolimus following its application as twice daily drug capsules, each 12 hours, and once-daily capsules with extended release in healthy people and patients. However, only future clinical trials would show whether these two drug formulations are really comparable as far as pharmacokinetic parameters are concerned, and, what is more important, taking into account long-term safety of extended release tacrolimus, survival of grafts and patients themselves.

References

Coilly A, Calmus Y, Chermak F, et al. Once-daily pro-longed release tacrolimus in liver transplantation: Experts' literature review and recommendations. Liver Transpl 2015; 21(10): 1312-21.

Sažetak karakteristika leka. Prograf®, kapsule, tvrde 0,5mg, 1mg i 5mg. Dostupno na: http://www.alims.gov.rs/ciril/lekovi/pretrazivanje-humanih-lekova/?a=p

Sažetak karakteristika leka. Advagraf®, kapsule sa produženim oslobađanjem, tvrde, 0,5mg, 1mg, 3mg i 5mg. Dostupno na: http://www.alims.gov.rs/ciril/ lekovi/pretrazivanje-humanih-lekova/?a=p

Michelon T, Dominguez V, Losekan A, et al. Kidney graft failure due to noncompliance. Transplant Proc 1999; 31(7): 3031-2.

Morrissey PE, Reinert S, Yango A, Gautam A, Monaco A, Gohh R. Factors contributing to acute rejection in renal transplantation: the role of non-compliance. Transplant Proc 2005; 37(5): 2044-7.

Patzer RE, Serper M, Reese PP, et al. Medication Understanding, Non-Adherence, and Clinical Out-comes among Adult Kidney Transplant Recipients. Clin Transplant 2016 Jul 22. doi: 10.1111/ctr.12821.

Jun H, Kim MG, Jung CW. Clinical advantages including medication adherence with conversion to once-daily advagraf and sirolimus combination in stable kidney recipients. Int J Clin Pharmacol Ther 2016; 54(2): 81-6.

Staatz CE, Tett SE. Clinical Pharmacokinetics of Once-Daily Tacrolimus in Solid-Organ Transplant Patients. Clin Pharmacokinet 2015; 54(10): 993-1025.

Lalić J, Veličković-Radovanović R, Mitić B, Paunović G, Cvetković T. Immunosuppressive medication adherence in kidney transplant patients. Med Princ Pract 2014; 23(4): 351-6.

Beckebaum S, Iacob S, Sweid D, et al. Efficacy, safety, and immunosuppressant adherence in stable liver transplant patients converted from a twice-daily tacrolimus-based regimen to once-daily tacrolimus extended-release formulation. Transpl Int 2011; 24(7): 666-75.

Dharancy S, Giral M, Tetaz R, Fatras M, Dubel L, Pageaux GP. Adherence with immunosuppressive treatment after transplantation: results from the French trial PREDICT. Clin Transplant 2012; 26(3): E293-9.

van Hooff JP, Alloway RR, Trunečka P, Mourad M. Four-year experience with tacrolimus once-daily prolonged release in patients from phase II conversion and de novo kidney, liver, and heart studies. Clin Transplant 2011; 25(1): E1-12.

Berquist RK, Berquist WE, Esquivel CO, Cox KL, Wayman KI, Litt IF. Non-adherence to post-transplant care: prevalence, risk factors and outcomes in adolescent liver transplant recipients. Pediatr Transplant 2008; 12(2): 194-200.

European medicines agency. SCIENTIFIC DISCUSSION. Dostupno na: http://www.ema.europa. eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000712/WC500022237.pdf

Rančić N, Dragojević-Simić V, Vavić N, et al. Tacrolimus concentration/dose ratio as a therapeutic drug monitoring strategy: the influence of gender and comedication. Vojnosanit Pregl 2015; 72(9): 813-22.

Vavic N, Rancic N, Dragojevic-Simic V, et al. The influence of comedication on tacrolimus blood concen-tration in patients subjected to kidney transplantation: a retrospective study. Eur J Drug Metab Pharmacokinet 2014; 39(4): 243-53.

Vavić N, Rančić N, Cikota-Aleksić B, et al. Distribucija polimorfizma gena koji kodiraju CYP3A5, CYP3A4 i P-glikoprotein kod bolesnika podvrgnutih transplantaciji bubrega. Vojnosanit Pregl 2016; 73(7): 663-7.

Piotti G, Cremaschi E, Maggiore U. Once-daily pro-longed-release tacrolimus formulations for kidney transplantation: what the nephrologist needs to know. J Nephrol. 2017; 30(1): 53-61.

Shi WL, Tang HL, Zhai SD. Effects of the CYP3A4*1B Genetic Polymorphism on the Phar-macokinetics of Tacrolimus in Adult Renal Transplant Recipients: A Meta-Analysis. PLoS One 2015; 10(6): e0127995.

Rojas L, Neumann I, Herrero MJ, et al. Effect of CYP3A5*3 on kidney transplant recipients treated with tacrolimus: a systematic review and meta-analysis of observational studies. Pharmacogenomics J 2015; 15(1): 38-48.

van Gelder T, van Schaik RH, Hesselink DA. Pharmacogenetics and immunosuppressive drugs in solid organ transplantation. Nat Rev Nephrol 2014; 10(12): 725-31.

Rostaing L, Bunnapradist S, Grinyó JM, et al. 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 2016; 67(4): 648-59.

Wlodarczyk Z, Squifflet JP, Ostrowski M, et al. Pharmacokinetics for once- versus twice-daily tacrolimus formulations in de novo kidney transplantation: a randomized, open-label trial. Am J Transplant 2009; 9(11): 2505-13.

Charco R, Caralt M, Lladó L, et al. A prospective, multicenter study of once-daily extended-release tacrolimus in de novo liver transplant recipients. Transplant Proc 2011; 43(3): 718-23.

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

Alloway R, Steinberg S, Khalil K, et al. Conversion of stable kidney transplant recipients from a twice daily Prograf-based regimen to a once daily modified release tacrolimus-based regimen. Transplant Proc 2005; 37(2): 867-70.

de Jonge H, Kuypers DR, Verbeke K, Vanrenterghem Y. Reduced C0 concentrations and increased dose requirements in renal allograft recipients converted to the novel once-daily tacrolimus formulation. Tran-splantation 2010; 90(5): 523-9.

Florman S, Alloway R, Kalayoglu M, et al. Conversion of stable liver transplant recipients from a twice-daily Prograf-based regimen to a once-daily modified release tacrolimus-based regimen. Transplant Proc 2005; 37(2): 1211-3.

Alloway R, Vanhaecke J, Yonan N, et al. Pharmacokinetics in stable heart transplant recipients after conversion from twice-daily to once-daily tacro-limus formulations. J Heart Lung Transplant 2011; 30(9): 1003-10.

Diez Ojea B, Alonso Alvarez M, Aguado Fernández S, et al. Three-month experience with tacrolimus once-daily regimen in stable renal allografts. Transplant Proc 2009; 41(6): 2323-5.

Marin-Gomez LM, Gomez-Bravo MA, Alamo-Martinez JA, et al. Evaluation of clinical safety of conversion to Advagraf therapy in liver transplant recipients: observational study. Transplant Proc 2009; 41(6): 2184-6.

Bunnapradist S, Rostaing L, Alloway RR, et al. LCPT once-daily extended-release tacrolimus tablets versus twice-daily capsules: a pooled analysis of two phase 3 trials in important de novo and stable kidney transplant recipient subgroups. Transpl Int 2016; 29(5): 603-11.

Ogura Y, Imai H, Kamei H, Hori T, Kurata N, Onishi Y. Early Conversion From Twice-Daily Tacrolimus to Prolonged-Release Tacrolimus in Liver Transplan-tation: A Single-Center Experience. Ann Transplant 2016; 21: 448-55.

Published
2017/11/14
Section
Short Report