Everolimus may have a role in heart transplantation as it has been shown to reduce chronic allograft vasculopathy in such transplants. It also may have a similar role to sirolimus in kidney and other transplants.
Eisen HJ, Tuzcu EM, Dorent R, et al: Everolimus for the Prevention of Allograft Rejection and Vasculopathy in Cardiac-Transplant Recipients. New England Journal of Medicine 2003; 349:847-858
In comparison to sirolimus, everolimus has better pharmacokinetics: a shorter half-life (28 h instead of 60 h), a slightly higher bioavailability, and a higher correlation of bioavailability with the administered dose.
Everolimus is approved for the prevention of organ rejection after kidney and heart transplantations in combination with cyclosporine and corticosteroids.
Everolimus should also not be taken together with grapefruit juice since this juice can increase the bioavailability of various drugs by inhibition of the intestinal cytochrome P450-isoenzyme CYP3A4.
Described as a proliferation inhibitor, everolimus (Certican) was developed by Novartis for the prevention of transplant rejection (during chronic graft rejection, the arterial endothelium displays extensive proliferation that may gradually occlude the vessel lumen, resulting in ischemia and fibrosis of the graft).
Everolimus is an orally active derivative of the immunosuppressantsirolimus (Rapamune, Wyeth Laboratories, Philadelphia, PA), a macrolide synthesized by Streptomyces hygroscopicus.
At 6-month follow-up, the everolimus eluting stent had a much lower in-stent late lumen loss (due to endothelial proliferation) than controls and the extent of stenoses within the lesioned segment of vasculature were only 20% of the overall vessel diameter compared to 37% in controls.
Feeds |
Contact