Everolimus.
Everolimus is an immunosuppressant that blocks growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Oral everolimus 0.75 or 1.5mg twice daily significantly reduced the incidence of the primary composite endpoint, efficacy failure 6 months after transplantation, compared with azathioprine 1-3 mg/kg/day, in adult cardiac transplant recipients. All patients also received baseline immunosuppression with cyclosporin and corticosteroids. The incidence of efficacy failure remained significantly lower in everolimus recipients than in those receiving azathioprine 1 and 2 years after cardiac transplantation. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus or azathioprine. The incidence of graft vasculopathy 2 years after transplantation was significantly lower in cardiac transplant recipients receiving everolimus 0.75 mg twice daily than in those receiving azathioprine. The combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in adult patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil (MMF) 2 g/day 1 or 3 years after renal transplantation. Patients also received baseline immunosuppression with cyclosporin and corticosteroids. Compared with azathioprine and MMF, everolimus is associated with a lower incidence of cytomegalovirus infection in cardiac and renal transplant recipients. Everolimus has been associated with thrombocytopenia, leucopenia and elevated serum lipids and creatinine.
Chapman
Therese M
TM
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Perry
Caroline M
CM
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D002908:Chronic Disease; D004195:Disease Models, Animal; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D000068338:Everolimus; D006084:Graft Rejection / Q000188:drug therapy*; D006207:Half-Life; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D008658:Inactivation, Metabolic / Q000235:genetics; D015337:Multicenter Studies as Topic; D016377:Organ Transplantation / Q000009:adverse effects / Q000473:pathology; D016032:Randomized Controlled Trials as Topic; D051381:Rats; D038762:Ribosomal Protein S6 Kinases, 70-kDa / Q000037:antagonists & inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D020123:Sirolimus / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013552:Swine; D013997:Time Factors; D016896:Treatment Outcome
D007166:Immunosuppressive Agents; D000068338:Everolimus; D038762:Ribosomal Protein S6 Kinases, 70-kDa; D020123:Sirolimus