Mechanism of Action: Exemestane is an irreversible aromatase inhibitor that blocks the conversion of androgens to estrogens, lowering circulating estrogen levels.
Indications & Off-Label Uses: FDA-approved for estrogen receptor–positive breast cancer in postmenopausal women. Off-label uses include managing estrogen-related side effects in men on testosterone therapy or other hormonal treatments (e.g., prevention of gynecomastia).
FDA Status: Approved for breast cancer treatment; other uses are off-label.
Clinical Evidence: Strong evidence supports use in postmenopausal breast cancer. Small studies and clinical experience suggest efficacy in reducing estrogen-related side effects in men on testosterone therapy, but long-term safety in this population is less well established.
Safety & Monitoring: Common side effects include joint pain, fatigue, hot flashes, and decreased bone mineral density. Monitoring of bone health, liver function, and hormone levels is recommended during therapy.
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