Mycophenolate mofetil enhances the negative effects of sirolimus and tacrolimus on rat kidney cell metabolism

PLoS One. 2014 Jan 30;9(1):e86202. doi: 10.1371/journal.pone.0086202. eCollection 2014.

Abstract

Background and purpose: Mycophenolate mofetil (MMF) per se is not known to have negative effects on the kidney. MMF alone or in combination with sirolimus, can be the basis of calcineurin inhibitor (CNI)-free, kidney sparing drug protocols. However, long-term outcomes in patients on MMF/SRL seem to be inferior to those treated with regimens that include the CNI tacrolimus (TAC) due to an increased risk of allo-immune reactions. Interestingly, potential enhancement of the negative effects of SRL and TAC on the kidney by MMF has never been considered.

Experimental approach: It was our aim to study the effects of TAC, SRL and MMF alone and evaluate their interactions when combined on the rat kidney. For this purpose we used a comprehensive molecular marker approach including measurements of urinary 8-isoprostane concentrations (oxidative stress marker) and changes of urinary metabolite patterns ((1)H-NMR spectroscopy) and comparing these markers to renal function (glomerular filtration rate (GFR)) and morphologic alterations (histology).

Key results: While MMF alone did not impact GFR, its interaction with SRL and TAC led to a significant decrease of rats' renal function. The decline went in parallel with a significant increase in urinary isoprostane concentrations and an enhancement of negative effects on urinary metabolite patterns.

Conclusions: In broad summary, the present study showed that MMF may enhance the negative effects of TAC on kidney function and may even display nephrotoxic properties when combined with SRL.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Drug Synergism
  • Glomerular Filtration Rate / drug effects
  • Graft Rejection / prevention & control
  • Immunosuppressive Agents / adverse effects*
  • Immunosuppressive Agents / pharmacokinetics
  • Immunosuppressive Agents / therapeutic use
  • Kidney / drug effects
  • Kidney / metabolism
  • Kidney / pathology
  • Kidney / physiopathology*
  • Kidney Transplantation
  • Male
  • Mycophenolic Acid / adverse effects
  • Mycophenolic Acid / analogs & derivatives*
  • Mycophenolic Acid / pharmacokinetics
  • Mycophenolic Acid / therapeutic use
  • Rats, Inbred WF
  • Sirolimus / adverse effects*
  • Sirolimus / pharmacokinetics
  • Sirolimus / therapeutic use
  • Tacrolimus / adverse effects*
  • Tacrolimus / pharmacokinetics
  • Tacrolimus / therapeutic use
  • Tissue Distribution

Substances

  • Immunosuppressive Agents
  • Mycophenolic Acid
  • Sirolimus
  • Tacrolimus