Everolimus: an update on the mechanism of action, pharmacokinetics and recent clinical trials.
BACKGROUND
A growing body of evidence suggests that everolimus might offer effective immunosuppressive activity together with antiproliferative effects that may address some of the unmet needs in the long-term therapeutic management of the post-transplant patient.


OBJECTIVE
To summarize the emerging evidence for employing everolimus-based immunosuppression.


METHODS
A systematic review was conducted of the Medline, Embase and Renal Health Library (Cochrane Collaboration) databases, and of the summary publications from international transplant meetings and congresses during 2000-2008.


RESULTS
This article summarizes this analysis, with special focus on the pharmacokinetic characteristics of everolimus and on the results of its use in renal transplantation. Some data has also been included about the efficacy of the drug in other solid organ transplantation and in tumours.


CONCLUSIONS
Everolimus is an immunosuppressant drug with proven efficacy in transplantation. When used in combination with cyclosporin, better results are obtained in renal function with low cyclosporin doses. Adverse events related to this drug are frequent and lead to moderate dropout rates.
Sánchez-Fructuoso
Ana I
AI
Nephorology Department, Hospital Clinico, Avda Martin Lagos s/n, 28040 Madrid, Spain. sanchezfruct@telefonica.net
D000970:Antineoplastic Agents / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D003586:Cytomegalovirus Infections / Q000276:immunology / Q000517:prevention & control; D016903:Drug Monitoring; D000068338:Everolimus; D006084:Graft Rejection / Q000276:immunology / Q000517:prevention & control*; D006085:Graft Survival / Q000187:drug effects*; D016027:Heart Transplantation; D006801:Humans; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016030:Kidney Transplantation; D009369:Neoplasms / Q000188:drug therapy; D016377:Organ Transplantation / Q000009:adverse effects; D020123:Sirolimus / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016896:Treatment Outcome
D000970:Antineoplastic Agents; D007166:Immunosuppressive Agents; D000068338:Everolimus; D020123:Sirolimus