Everolimus/[email protected]

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It is currently used as an immunosuppressant to prevent rejection of organ transplants and in the treatment of renal cell cancer and other tumours. Much research has also been conducted on everolimus and other mTOR inhibitors as targeted therapy for use in a number of cancers.

Usage

Everolimus is approved for various conditions:
Advanced kidney cancer
Prevention of organ rejection after renal transplant
Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis (TS) in patients who are not suitable for surgical intervention
Progressive or metastatic pancreatic neuroendocrine tumors not surgically removable
Breast cancer in post-menopausal women with advanced hormone-receptor positive, HER2-negative type cancer, in conjunction with exemestane
Prevention of organ rejection after liver transplant
Progressive, well-differentiated non-functional, neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin with unresectable, locally advanced or metastatic disease.

Role in heart transplantation
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.

Role in liver transplantation
Although, sirolimus had generated fears over use of m-TOR inhibitors in liver transplantation recipients, due to possible early hepatic artery thrombosis and graft loss, use of everolimus in the setting of liver transplantation is promising. Also, a possible role of everolimus in reducing the recurrence of hepatocellular carcinoma after liver transplantation was correlated.

Use in vascular stents
Everolimus is used in drug-eluting coronary stents as an immunosuppressant to prevent restenosis. Abbott Vascular produce an everolimus-eluting stent (EES) called Xience Alpine. It utilizes the Multi-Link Vision cobalt chromium stent platform and Novartis' everolimus.

Use in aging
Inhibition of mTOR, the molecular target of Everolimus, extends the lifespan of model organisms including mice,and mTOR inhibition has been suggested as an anti-aging therapy. Everolimus treatment of mice results in reduced metabolic side effects compared to sirolimus.