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Exemestane

依西美坦
Mechanism of action:
Exemestane 是一種芳香化酶抑制劑(aromatase inhibitor)。Exemestane 的結構類似雄烯二酮(androstenedione),可進入芳香化酶的活性位點,會形成共價結合,不可逆抑制芳香化酶的活性。芳香化酶被抑制後,雌二醇(estradiol)與雌酮(estrone)濃度顯著下降,減少雌激素對乳癌細胞的刺激。
Reference(s):
1. Coombes RC et al. (2007). Survival and safety of exemestane versus tamoxifen after 2–3 years' tamoxifen treatment (Intergroup Exemestane Study): a randomised controlled trial. Lancet.
2. Robinson A et al. (2009). A review of the use of exemestane in early breast cancer. Ther Clin Risk Manag.
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