Clinical experience with everolimus (Certican): optimizing dose and tolerability

Transplantation. 2005 May 15;79(9 Suppl):S80-4. doi: 10.1097/01.tp.0000162433.34739.61.

Abstract

Background: Everolimus (Certican), a novel proliferation signal inhibitor, allows calcineurin inhibitor dose reduction in transplant patients, minimizing risk of nephrotoxicity without loss of immunosuppressive efficacy. As a result of its mode of action, this class of agent (i.e., everolimus and sirolimus) is associated with certain adverse events (e.g., lymphocele, arthralgia, edema and hyperlipidemia).

Methods: Three case studies from within an everolimus Phase III trial (A2306) are presented with the aim of illustrating how treatment-related adverse events can be managed.

Results: The combination of everolimus with reduced-exposure cyclosporine was efficacious in these patients. One experienced mild acute rejection that was managed with steroid boluses. All have acceptable graft function during follow-up to date. Moderate lymphocele either resolved spontaneously or was easily managed by povidine-iodine instillations. One patient developed serious early lymphocele that, unusually, required surgical intervention. Everolimus dose reduction or withdrawal was not necessary to effectively manage lymphocele of any severity. A case of bilateral multiple arthralgia was effectively managed with everolimus dose reduction, but still maintained everolimus trough blood levels at approximately 3 ng/ml. Eyelid and ankle edemas were also easily managed with low dose furosemide, preferably coupled with cyclosporine and everolimus dose reduction. Hyperlipidemia responded to statin therapy.

Conclusions: Everolimus-related adverse events can be effectively managed either with other treatments or, where necessary, by everolimus dose reduction, without loss of efficacy. Discontinuing everolimus therapy is generally not necessary.

Publication types

  • Case Reports

MeSH terms

  • Adult
  • Calcineurin Inhibitors
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Everolimus
  • Humans
  • Immunosuppressive Agents / therapeutic use*
  • Kidney Transplantation / immunology*
  • Middle Aged
  • Sirolimus / administration & dosage
  • Sirolimus / analogs & derivatives*
  • Sirolimus / therapeutic use*
  • Treatment Outcome

Substances

  • Calcineurin Inhibitors
  • Immunosuppressive Agents
  • Everolimus
  • Sirolimus