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Everolimus

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Information about Everolimus

Everolimus is an inhibitor of cell proliferation and immunosuppressive agent that is used alone or in combination with calcineurin inhibitors to prevent cellular rejection after organ transplantation, and in combination with other anticancer agents as treatment of advanced renal cell and other cancers.

Liver toxicity of Everolimus

Everolimus therapy can be associated with mild serum enzyme elevations, but has yet to be linked to instances of clinically apparent liver injury with jaundice. 

Mechanism of action of Everolimus

Everolimus (e" ver oh' li mus) binds to the same intracellular receptor as tacrolimus and cyclosporine, but does not inhibit calcineurin; rather, it blocks the "mammalian target of rapamycin" (mTOR), which interrupts signaling pathways of several cytokines and growth factors including IL2 and causes a decrease in protein synthesis and cell cycle arrest.  Everolimus therapy has been shown to improve graft survival after solid organ transplantation and to improve time to progression in several forms of cancer. 

FDA approval information for Everolimus

Everolimus was approved for use in the United States in 2009 initially as an agent to prevent rejection after kidney and liver transplantaiton and later, in higher doses, as therapy of advanced renal cell, breast and pancreatic neuroendocrine cancers given alone or in combination with other antineoplastic agents.  More recently, everolimus was approved as therapy of renal angiomyolipoma and subependymal giant cell astrocytoma associated with tuberous sclerosis complex (in which mTOR signaling is dysregulated).  Everolimus like sirolimus is also used in drug eluting arterial stents, to prevent stenosis. 

Dosage and administration for Everolimus

Everolimus is available as tablets of 0.25, 0.50 and 0.75 mg under the brand name of Zortress for management of solid organ transplantation, and as tablets of 2.5, 5, 7.5 and 10 mg under the brand name of Afinitor, and tablets of 2, 3 and 5 mg for oral suspension under the brand name Afinitor-Disprez for use in cancer chemotherapy.  The typical dose in organ transplantation is 1.0 to 1.5 mg in two divided doses daily but therapeutic drug level monitoring for dosing is recommended.  The doses using in cancer chemotherapy are higher than those used in prevention of organ rejection, usually starting at 10 mg once daily and varying somewhat by indication. 

Side effects of Everolimus

Everolimus is less nephrotoxic than the calcineurin inhibitors but does have many, largely dose dependent side effects including oral ulcers, somatitis, diarrhea, nausea, poor appetite, fatigue, peripheral edema, rash, anemia, impaired wound healing and renal dysfunction.  Less common but potentially severe adverse events include interstitial pneumonitis, reanl failure, hypersensitivity reactions and embryo-fetal toxicity. 

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