Xevirol 5 mg (Everolimus)
Everolimus is indicated in advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer (Advanced HR BC), Advanced Neuroendocrine Tumors (NET); Advanced Renal Cell Carcinoma (RCC); Renal Angiomyolipoma With Tuberous Sclerosis Complex (TSC); Subependymal Giant Cell Astrocytoma (SEGA) With Tuberous Sclerosis Complex (TSC)
In combination with ciclosporin for microemulsion & corticosteroids for the prophylaxis of organ rejection in adult patients at low to moderate immunological risk receiving an allogeneic renal or cardiac transplant. In combination with tacrolimus & corticosteroids for the prophylaxis of organ rejection in patients receiving hepatic transplants.
*Take according to the doctor’s advice
Therapeutic Class
Immunosuppressant
Pharmacology
Everolimus, a proliferation signal inhibitor, prevents allograft rejection in rodent and nonhuman primate models of allotransplantation. It exerts its immunosuppressive effect by inhibiting the proliferation and thus, clonal expansion, of antigen-activated T cells which is driven by T cell-specific interleukins eg, interleukin-2, and interleukin-15. Everolimus inhibits an intracellular signaling pathway that normally leads to cell proliferation when triggered by the binding of these T cell growth factors to their receptors. The blockage of this signal by everolimus causes cells to be arrested at the G1 stage of the cell cycle.
At the molecular level, everolimus forms a complex with the cytoplasmic protein FKBP-12. In the presence of everolimus, the growth factor-stimulated phosphorylation of the p70 S6 kinase is inhibited. Since p70 S6 kinase phosphorylation is under the control of FRAP (also called mTOR), this finding suggests that the everolimus-FKBP-12 complex binds to and thus, interferes with the function of FRAP. FRAP is a key regulatory protein that governs cell metabolism, growth, and proliferation; disabling FRAP function thus explains the cell cycle arrest caused by everolimus.
Dosage & Administration
General kidney & heart transplant population: Initially 0.75 mg bd was administered as soon as possible after transplantation.
Hepatic transplant: 1 mg bd with initial dose starting 4 wk after transplantation.
Advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer, Advanced NET, Advanced RCC, And Renal Angiomyolipoma With TSC: The recommended dose is 10 mg, to be taken once daily at the same time every day. Administer either consistently with food or consistently without food. Everolimus Tablets should be swallowed whole with a glass of water. Do not break or crush tablets. Continue treatment until disease progression or unacceptable toxicity occurs.
*Take according to the doctor’s advice
Interaction
CYP3A4 inhibitors &/or inducers, CYP2D6 substrates with narrow therapeutic index, PGP inhibitors, rifampicin, ACE inhibitors, grapefruit juice & live vaccines.
