Experience with everolimus.
Everolimus is a novel macrolide immunosuppressant that acts as a T-lymphocyte proliferation signal inhibitor. Its actions are complementary to and synergistic with those of the calcineurin inhibitors. Compared with sirolimus, everolimus has unique pharmacokinetic characteristics including greater bioavailability and a shorter half-life, allowing more rapid achievement of a steady state. Clinical experience to date, largely limited to use in kidney transplant patients receiving cyclosporine-based immunosuppression, indicates that administration of everolimus is associated with low rates of acute rejection and a tolerable safety profile. Recent observations in heart transplant patients suggest that the antiproliferative effects of everolimus may prevent allograft vasculopathy.
Augustine
J J
JJ
Department of Medicine Case Western Reserve University and the Transplantation Service, University Hospitals of Cleveland, Cleveland, OH 44106, USA.
Hricik
D E
DE
D003404:Creatinine / Q000097:blood; D016572:Cyclosporine / Q000627:therapeutic use; D004359:Drug Therapy, Combination; D000068338:Everolimus; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016030:Kidney Transplantation / Q000276:immunology* / Q000502:physiology; D008213:Lymphocyte Activation / Q000187:drug effects / Q000276:immunology; D020123:Sirolimus / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013601:T-Lymphocytes / Q000276:immunology; D013997:Time Factors; D014181:Transplantation Immunology
D007166:Immunosuppressive Agents; D016572:Cyclosporine; D000068338:Everolimus; D003404:Creatinine; D020123:Sirolimus