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Everolimus

依維莫司
Mechanism of action:
Everolimus 是一種 mTOR 抑制劑(mammalian target of rapamycin inhibitor),為雷帕黴素(rapamycin)的衍生物。Everolimus 會先與細胞內的 FKBP-12(FK506-binding protein 12)結合,形成 Everolimus-FKBP-12 複合體。該複合體會抑制 mTORC1 的激酶活性,阻斷下游訊號分子磷酸化,使細胞週期停滯於 G1 期,抑制細胞增殖。
Reference(s):
1. Kuhn B et al. (2001). Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem.
2. Krueger DA et al. (2010). Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis. N Engl J Med.
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