Exemestane is a steroidal suicide aromatase inhibitor. It is very similar in structure and action to formestane, although it is significantly more potent in comparison. As a class of drugs, aromatase inhibitors offer an anti-estrogenic effect by blocking the enzyme responsible for synthesizing estrogens. Exemestane is approved by the FDA for the treatment of breast cancer in women, specifically in post-menopausal patients whose cancer has progressed following therapy with tamoxifen. Male bodybuilders and athletes often use the drug for nonapproved purposes, namely to counter the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids. This may include gynecomastia, fat buildup, and water retention. In some instances aromatase inhibitors may also assist this group with the loss of body fat and increases in muscular definition. Exemestane is one of the most potent aromatase inhibitors presently available. The most commonly cited data (found in the Aromasin packaging insert) reports a lowering of serum estrogen levels by 85% on average in clinical studies with women.
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