Experience with everolimus.

Abstract

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.