What is Letrozole?
Letrozole, commercially known as Femara®, is an oral non-steroidal aromatase inhibitor designed for the adjuvant treatment of hormonally-responsive breast cancer. It operates by blocking the production of estrogens, which are formed through the conversion of androgens by the aromatase enzyme. Letrozole achieves this by competitively and reversibly binding to the heme component of its cytochrome P450 unit. Importantly, its action is highly specific and does not interfere with the production of mineralo- or corticosteroids.
In contrast to tamoxifen, the primary medical therapy used before the advent of aromatase inhibitors, which acts by disrupting the estrogen receptor, Letrozole targets estrogen production directly. The United States Food and Drug Administration (FDA) has granted approval for Letrozole’s use in postmenopausal women with local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status.
Users of Letrozole may experience side effects associated with reduced estrogen levels, including hypoestrogenism symptoms. Prolonged usage raises concerns about potential osteoporosis development. Consequently, healthcare professionals often prescribe osteoporosis-preventing medications such as Fosamax alongside Letrozole.
Letrozole has demonstrated its capability to decrease estrogen levels by an impressive 98 percent while simultaneously elevating testosterone levels. This unique anti-estrogenic action is favored by athletes and bodybuilders during steroid cycles as it reduces bloating caused by excess water retention and prevents the formation of gynecomastia-linked breast tissue, a side effect associated with certain anabolic steroids.
However, it is worth noting that doses exceeding 2.5 mg/day may temporarily diminish libido, and prolonged use at levels exceeding 5 mg/day carries the risk of kidney complications. Additionally, Letrozole has been found to delay the fusion of growth plates in adolescents. This property is sometimes harnessed to enhance the effectiveness of growth hormone treatment, making Letrozole a choice for managing short stature in adolescents and children.
NOTE: This information does not constitute medical advice, and it is imperative to seek consultation with your healthcare provider before initiating any new medication.
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