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Anastrozole Overview Primary Constituent: Anastrozole Category: Aromatase Inhibitors Administration: Oral (tablets) Brief Overview Anastrozole is a potent, third-generation non-steroidal aromatase inhibitor. Initially crafted for cancer treatment, especially breast cancer, it plays a pivotal role in manipulating hormone levels. Men employ Anastrozole to diminish estrogen concentrations in the bloodstream and amplify their intrinsic testosterone and gonadotropic hormone levels..