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What is anastrozole? Anastrozole is a drug that blocks the conversion of testosterone to estrogen. It was originally developed to treat breast cancer in women, but was later used in men as well, primarily to control estrogen levels during testosterone therapy or when aromatization is excessive. Excess estrogen in men can cause gynecomastia, fluid retention, and decreased testosterone production. Anastrozole helps maintain a balance between androgens and estrogens, supporting hormonal balance. ..