ACTIVE HALF-LIFE
2 days
CLASSIFICATION
Non-steroidal aromatase inhibitor
DOSAGE
0.5 - 2.5 mg/day
ACNE
No
WATER RETENTION
No
HBR
No
HEPATOTOXICITY
No
AROMATIZATION
No
MANUFACTURER
Beligas - US
LAB TEST
See Document
WAREHOUSE
USA Warehouse 2
SUBSTANCE
Letrozole
,
Mono-Femara is a nonsteroidal agent that inhibits estrogen synthesis and has anticancer properties. As a third-generation aromatase inhibitor, it selectively and reversibly blocks aromatase, potentially hindering the growth of estrogen-dependent breast cancer cells.
Aromatase is a cytochrome P-450 enzyme found in the endoplasmic reticulum of cells and in various tissues, including the premenopausal ovaries, liver, and breasts. It catalyzes the conversion of androstenedione and testosterone into estrone and estradiol, which is the final stage in the production of estrogen.
Estrogens are generated through the conversion of androgens via the aromatase enzyme's action. Mono-Femara inhibits estrogen production by competitively and reversibly binding to the heme component of its cytochrome P450 unit. This mechanism is selective, meaning that Mono-Femara does not affect the synthesis of mineralocorticoids or corticosteroids. In contrast, tamoxifen, the primary treatment option before the introduction of aromatase inhibitors, works as an anti-estrogen by blocking estrogen receptors instead of inhibiting estrogen production.
The United States Food and Drug Administration (FDA) has approved Mono-Femara for treating local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women. Side effects may include symptoms associated with low estrogen levels. There are concerns about the potential for long-term use to lead to osteoporosis, which is why doctors often prescribe medications like Fosamax alongside Mono-Femara to combat this risk.
Mono-Femara has been shown to lower estrogen levels by as much as 98% while increasing testosterone levels.
Athletes and bodybuilders often prefer Mono-Femara to mitigate water retention and prevent the development of gynecomastia, which can occur with some anabolic steroids during a steroid cycle. However, doses exceeding 2.5 mg/day may temporarily reduce libido, and prolonged use above 5 mg/day can lead to kidney issues.
Additionally, Mono-Femara has been demonstrated to delay the fusion of growth plates in adolescents, possibly enhancing the effectiveness of growth hormone, making it useful in treating short stature in children and adolescents.