Sirolimus (rapamycin) potentiates cyclosporine in prevention of acute lung rejection

J Thorac Cardiovasc Surg. 1999 Apr;117(4):714-8. doi: 10.1016/S0022-5223(99)70291-6.

Abstract

Background: Cyclosporine-based immunosuppressive regimens (INN: ciclosporin) in human lung transplantation continue to result in a high incidence of acute cellular rejection. We investigated the use of sirolimus, a macrolide with structural similarity to tacrolimus, as monotherapy and in combination with cyclosporine in a rodent lung transplant model.

Methods: Orthotopic left lung transplantation was performed in Lewis recipients from Brown-Norway donor rats with syngeneic Lewis-to-Lewis controls. Open biopsies were performed on postoperative day 7, and the severity of acute lung rejection was graded by a pathologist blinded to the protocol.

Results: All recipients survived despite the amount of acute rejection seen on examination of the biopsy tissue. Lewis-to-Lewis isografts demonstrated near normal pulmonary architecture. Allogeneic recipients receiving high-dose cyclosporine (25 mg/kg) monotherapy showed mild to moderate acute rejection with some perivascular focal interstitial infiltrates. Recipients receiving low-dose cyclosporine (5 mg/kg) monotherapy or low- or high-dose sirolimus (0.5 or 2.0 mg/kg, respectively) monotherapy demonstrated massive cellular infiltration leading to necrosis and infarction and could not be graded. However, the addition of low-dose sirolimus (0.5 mg/kg) to low-dose cyclosporine (5 mg/kg) demonstrated a significant potentiating immunosuppressive effect, and the addition of high-dose sirolimus (2.0 mg/kg) to low-dose cyclosporine (5.0 mg/kg) demonstrated an even greater effect, with rejection scores better than those obtained with high-dose cyclosporine monotherapy and similar to those obtained with isografts.

Conclusions: This study demonstrates that low-dose sirolimus has a cyclosporine-sparing effect and that a higher dose of sirolimus in combination with cyclosporine strongly protects lung allografts from acute cellular rejection. These results suggest that sirolimus may be indicated as an adjunct to current cyclosporine-based immunosuppressive regimens in clinical lung transplantation.

Publication types

  • Comparative Study

MeSH terms

  • Acute Disease
  • Animals
  • Cyclosporine / administration & dosage
  • Cyclosporine / therapeutic use*
  • Drug Synergism
  • Drug Therapy, Combination
  • Graft Rejection / prevention & control*
  • Immunosuppressive Agents / administration & dosage
  • Immunosuppressive Agents / therapeutic use*
  • Lung Transplantation / immunology*
  • Random Allocation
  • Rats
  • Rats, Inbred BN
  • Rats, Inbred Lew
  • Sirolimus / administration & dosage
  • Sirolimus / therapeutic use*

Substances

  • Immunosuppressive Agents
  • Cyclosporine
  • Sirolimus