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Exemestane is an irreversible steroidal aromatase inhibitors, has similar structure with its substrate,natural androstenedione. And it is the pseudo substrate of aromatase . The inhibition of aromatase to estrogen deprivation is a effective method in the treatment of postmenopausal women with hormone dependent breast cancer.
Due to the estrogen of postmenopausal women is mainly produced by androgen (adrenal cortex) ,which transform in the aromatase of peripheral tissues. Exemestane inactivates estrogen by combine with the active site of aromatase irreversibly, then the level of estrogen significantly reduces in blood circulating.
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