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説明

Everolimus is a Kinase Inhibitor. It’s brand name is Afinitor. Everolimus is a derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties.The mechanism of action of everolimus is as a Protein Kinase Inhibitor, and Cytochrome P450 3A4 Inhibitor, and P-Glycoprotein Inhibitor, and Cytochrome P450 2D6 Inhibitor.
In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production.
Everolimus is a biological therapy treatment for
Advanced breast cancer if you have been through the menopause (post menopausal). You take it with the hormone therapy drug exemestane
Advanced kidney cancer that has come back either during or after treatment.
Neuroendocrine tumours of the pancreas that can't be removed with surgery or have spread (metastatic disease).
Researchers are also looking at everolimus as a treatment for head and neck cancer and cancer of the food pipe (oesophageal cancer).