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Exemestane


Mechanism of action:

Exemestane is an aromatase inhibitor. Exemestane has a structure similar to androstenedione and can enter the active site of aromatase, where it forms a covalent bond and irreversibly inhibits aromatase activity. Once aromatase is inhibited, the concentrations of estradiol and estrone decline significantly, reducing estrogen-driven stimulation of breast cancer cells.

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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