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Exemestane is an irreversible inhibitor of aromatase (Ki = 26 nM).1 It is selective for aromatase over 5α-reductase when used at a concentration of 30 µM. Subcutaneous administration of exemestane (3-100 mg/kg per day) decreases tumor proliferation in rats with mammary tumors induced by the carcinogenic polycyclic aromatic hydrocarbon 7,12-dimethylbenz(a)anthracene (DMBA; Item No. 30383).2 Formulations containing exemestane have been used in the treatment of estrogen receptor-positive breast cancers in postmenopausal women.
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2. A new irreversible aromatase inhibitor, 6-