Literature DB >> 26722662

Combining cytochrome P-450 3A4 modulators and cyclosporine or everolimus in transplantation is successful.

Fernando González1, Ricardo Valjalo1.   

Abstract

AIM: To describe the long term follow-up of kidney allograft recipients receiving ketoconazole with calcineurin inhibitors (CNI) alone or combined with everolimus.
METHODS: This is an open-label, prospective observational clinical trial in low immunologic risk patients who, after signing an Institutional Review Board approved consent form, were included in one of two groups. The first one (n = 59) received everolimus (target blood level, 3-8 ng/mL) and the other (n = 114) azathioprine 2 mg/kg per day or mycophenolate mofetyl (MMF) 2 g/d. Both groups also received tapering steroids, the cytochrome P-450 3A4 (CYP3A4) modulator, ketoconazole 50-100 mg/d, and cyclosporine with C0 targets in the everolimus group of 200-250 ng/mL in 1 mo, 100-125 ng/mL in 2 mo, and 50-65 ng/mL thereafter, and in the azathioprine or MMF group of 250-300 ng/mL in 1 mo, 200-250 ng/mL in 2 mo, 180-200 ng/mL until 3-6 mo, and 100-125 ng/mL thereafter. Clinical visits were performed monthly the first year and quarterly thereafter by treating physicians and all data was extracted by the investigators.
RESULTS: The clinical characteristics of these two cohorts were similar. During the follow up (66 + 31 mo), both groups showed comparable clinical courses, but the biopsy proven acute rejection rate during the full follow-up period seemed to be lower in the everolimus group (20% vs 36%; P = 0.04). The everolimus group did not show a higher surgical complication rate than the other group. By the end of the follow-up period, the everolimus group tended to show a higher glomerular filtration rate. Nevertheless, we found no evidence of a consistent negative slope of the temporal allograft function estimated by the modification of the diet in renal disease formula in any of both groups. At 6 years of follow-up, the uncensored and death-censored graft survivals were 91% and 93%, and 91% and 83% in the everolimus plus cyclosporine, and cyclosporine alone groups, respectively. The addition of ketoconazole saved 80% of cyclosporine and 56% of everolimus doses.
CONCLUSION: Combining CYP3A4 modulators with CNI or mammalian target of rapamycin inhibitor, in low immunological risk kidney transplant recipients is feasible, effective, safe and affordable even in the long term.

Entities:  

Keywords:  Cyclosporine; Cytochrome P-450; Cytochrome P-450 3A4 modulator; Everolimus; Immunosuppressive; Ketoconazole; Kidney transplant

Year:  2015        PMID: 26722662      PMCID: PMC4689945          DOI: 10.5500/wjt.v5.i4.338

Source DB:  PubMed          Journal:  World J Transplant        ISSN: 2220-3230


  54 in total

1.  Efficacy and safety of low-dose ketoconazole (50 mg) to reduce the cost of cyclosporine in renal allograft recipients.

Authors:  M A Abraham; P P Thomas; G T John; V Job; V Shankar; C K Jacob
Journal:  Transplant Proc       Date:  2003-02       Impact factor: 1.066

2.  Everolimus plus reduced-exposure CsA versus mycophenolic acid plus standard-exposure CsA in renal-transplant recipients.

Authors:  H Tedesco Silva; D Cibrik; T Johnston; E Lackova; K Mange; C Panis; R Walker; Z Wang; G Zibari; Y S Kim
Journal:  Am J Transplant       Date:  2010-04-28       Impact factor: 8.086

3.  Concomitant administration of cyclosporine and ketoconazole in renal transplant patients.

Authors:  B V Gandhi; S Kale; D M Bhowmik; A K Jain
Journal:  Transplant Proc       Date:  1992-10       Impact factor: 1.066

4.  Cost-containment strategies in transplantation: the utility of cyclosporine-ketoconazole combination therapy.

Authors:  O Odocha; B Kelly; S Trimble; C Murigande; R M Toussaint; C O Callender
Journal:  Transplant Proc       Date:  1996-04       Impact factor: 1.066

5.  Ketoconazole-tacrolimus coadministration in kidney transplant recipients: two-year results of a prospective randomized study.

Authors:  Khalid Farouk El-Dahshan; Mohamed Adel Bakr; Ahmed Farouk Donia; Ali El-Sayed Badr; Mohamed Abdel-Kader Sobh
Journal:  Am J Nephrol       Date:  2006-06-22       Impact factor: 3.754

6.  Ketoconazole, cyclosporin metabolism, and renal transplantation.

Authors:  R M Ferguson; D E Sutherland; R L Simmons; J S Najarian
Journal:  Lancet       Date:  1982-10-16       Impact factor: 79.321

7.  Blood concentrations of everolimus are markedly increased by ketoconazole.

Authors:  J M Kovarik; D Beyer; M N Bizot; Q Jiang; M Shenouda; R L Schmouder
Journal:  J Clin Pharmacol       Date:  2005-05       Impact factor: 3.126

8.  The natural history of chronic allograft nephropathy.

Authors:  Brian J Nankivell; Richard J Borrows; Caroline L-S Fung; Philip J O'Connell; Richard D M Allen; Jeremy R Chapman
Journal:  N Engl J Med       Date:  2003-12-11       Impact factor: 91.245

9.  Cyclosporin C(2) and C(0) concentration monitoring in stable, long-term heart transplant recipients receiving metabolic inhibitors.

Authors:  John E Ray; Anne M Keogh; Andrew J McLachlan; Fatemah Akhlaghi
Journal:  J Heart Lung Transplant       Date:  2003-07       Impact factor: 10.247

10.  Limited utility of cyclosporine C2 monitoring in heart transplant recipients receiving ketoconazole.

Authors:  M Zakliczynski; A Krynicka; M Szewczyk; J Wojarski; M Zembala
Journal:  Transplant Proc       Date:  2003-09       Impact factor: 1.066

View more
  1 in total

1.  Switching Stable Kidney Transplant Recipients to a Generic Tacrolimus Is Feasible and Safe, but It Must Be Monitored.

Authors:  Fernando González; René López; Elizabeth Arriagada; René Carrasco; Natalia Gallardo; Eduardo Lorca
Journal:  J Transplant       Date:  2017-01-26
  1 in total

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