A randomized long-term trial of tacrolimus and sirolimus versus tacrolimus and mycophenolate mofetil versus cyclosporine (NEORAL) and sirolimus in renal transplantation. I. Drug interactions and rejection at one year

Transplantation. 2004 Jan 27;77(2):244-51. doi: 10.1097/01.TP.0000101290.20629.DC.

Abstract

Background: To reduce long-term nephrotoxic calcineurin inhibitor dosage, adjunctive sirolimus or mycophenolate mofetil (MMF) was used in a 150-patient, randomized, three-armed trial in cadaveric or human leukocyte antigen non-identical living-donor first renal transplant recipients (n=50/group).

Methods: Group A received tacrolimus and sirolimus. Target tacrolimus trough levels postoperatively were 10, 8, and 6 ng/mL at 1 month, 6 months, and 1 year, respectively. Group B received tacrolimus and MMF. Target tacrolimus trough levels were 10 and 8 ng/mL at 1 month and 1 year, with a targeted dose of MMF of 1 g twice daily. Group C received cyclosporine A (CsA) (Neoral, Novartis, Basel, Switzerland) and sirolimus with target CsA trough levels of 225 and 175 ng/mL at 1 month and 1 year. Maintenance sirolimus target trough levels were 8 ng/mL in groups A and C. Each group received daclizumab induction and methylprednisolone maintenance. This first of two companion 1-year reports details demographics, drug-dosing interactions, and rejection.

Results: There were no notable differences in group demographics, but a somewhat less favorable course occurred in group C, despite higher bioavailability of sirolimus in group C versus group A (P<0.001). Acute rejection rates were lower in groups A (4%) and B (4%) combined versus group C (14%) (P=0.03). Histopathologic findings were supported by comparing perioperative with 1-year postoperative protocol biopsies.

Conclusions: This 1-year interim analysis indicates that a decreasing dosage of tacrolimus with either adjunctive sirolimus or MMF may optimize future graft survival versus a less favorable outcome using a similar algorithm with CsA and sirolimus.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Area Under Curve
  • Biological Availability
  • Cadaver
  • Cyclosporine / blood
  • Cyclosporine / pharmacokinetics
  • Cyclosporine / therapeutic use*
  • Drug Interactions
  • Drug Therapy, Combination
  • Female
  • Graft Rejection / epidemiology*
  • Graft Rejection / prevention & control
  • Humans
  • Immunosuppressive Agents / blood
  • Immunosuppressive Agents / pharmacokinetics
  • Immunosuppressive Agents / therapeutic use*
  • Kidney Transplantation / immunology*
  • Living Donors
  • Male
  • Middle Aged
  • Mycophenolic Acid / analogs & derivatives*
  • Mycophenolic Acid / blood
  • Mycophenolic Acid / pharmacokinetics
  • Mycophenolic Acid / therapeutic use*
  • Sirolimus / blood
  • Sirolimus / pharmacokinetics
  • Sirolimus / therapeutic use*
  • Tacrolimus / blood
  • Tacrolimus / pharmacokinetics
  • Tacrolimus / therapeutic use*
  • Time Factors
  • Tissue Donors

Substances

  • Immunosuppressive Agents
  • Cyclosporine
  • Mycophenolic Acid
  • Sirolimus
  • Tacrolimus