PMID- 22954349 OWN - NLM STAT- MEDLINE DCOM- 20130317 LR - 20151119 IS - 1744-764X (Electronic) IS - 1474-0338 (Linking) VI - 11 IP - 6 DP - 2012 Nov TI - A drug safety evaluation of everolimus in kidney transplantation. PG - 1013-22 LID - 10.1517/14740338.2012.722993 [doi] AB - INTRODUCTION: Calcineurin inhibitors (CNI) have greatly reduced the rate of acute rejection and improved short-term graft survival after organ transplantation, however, long-term survival has hardly changed since their introduction. CNIs are believed to contribute to graft fibrosis, have side effects that adversely affect cardiovascular risk, and are associated with an increased rate of post-transplant malignancies. Everolimus, a mammalian target of rapamycin (mTOR) inhibitor, is not associated with graft fibrosis, has a superior cardiovascular risk profile to CNI therapy and has shown potential for the prevention and treatment of diverse forms of cancer. AREAS COVERED: This review summarizes key aspects of everolimus, including its mechanism of action, pharmacokinetics, pharmacodynamics, drug-drug interactions and pivotal clinical studies with a focus on safety and efficacy. EXPERT OPINION: Everolimus is effective in improving graft function in selected kidney transplant patients. Most adverse events are present for a short time after the introduction of everolimus, and are manageable. Everolimus has the potential to become an important agent in de novo and maintenance immunotherapy in kidney transplant recipients. FAU - Holdaas, Hallvard AU - Holdaas H AD - Oslo University Hospital, Department of Transplant Medicine, Section of Nephrology, Rikshospitalet, Postbox 4950 Nydalen, N-0424 Oslo, Norway. hallvard.holdaas@rikshospitalet.no FAU - Midtvedt, Karsten AU - Midtvedt K FAU - Asberg, Anders AU - Asberg A LA - eng PT - Journal Article PT - Review DEP - 20120906 PL - England TA - Expert Opin Drug Saf JT - Expert opinion on drug safety JID - 101163027 RN - 0 (Calcineurin Inhibitors) RN - 0 (Immunosuppressive Agents) RN - 9HW64Q8G6G (Everolimus) RN - W36ZG6FT64 (Sirolimus) SB - IM MH - Animals MH - Calcineurin Inhibitors MH - Clinical Trials as Topic MH - Drug Interactions MH - Everolimus MH - Graft Rejection/prevention & control MH - Graft Survival/drug effects MH - Humans MH - Immunosuppressive Agents/*adverse effects/pharmacology/therapeutic use MH - Kidney Transplantation/*methods MH - Sirolimus/adverse effects/*analogs & derivatives/pharmacology/therapeutic use MH - Time Factors EDAT- 2012/09/08 06:00 MHDA- 2013/03/19 06:00 CRDT- 2012/09/08 06:00 PHST- 2012/09/08 06:00 [entrez] PHST- 2012/09/08 06:00 [pubmed] PHST- 2013/03/19 06:00 [medline] AID - 10.1517/14740338.2012.722993 [doi] PST - ppublish SO - Expert Opin Drug Saf. 2012 Nov;11(6):1013-22. doi: 10.1517/14740338.2012.722993. Epub 2012 Sep 6.