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
Euro-Pharmacies - US
LAB TEST
See Document
WAREHOUSE
USA Warehouse 3
SUBSTANCE
Letrozole
,
Letrozolexin is a nonsteroidal agent that inhibits estrogen synthesis and exhibits antineoplastic properties. As a third-generation aromatase inhibitor, Letrozolexin specifically and reversibly blocks aromatase, potentially inhibiting the growth of estrogen-dependent breast cancer cells.
Aromatase is a cytochrome P-450 enzyme found in various tissues, including the premenopausal ovary, liver, and breast, and is located in the endoplasmic reticulum. It catalyzes the conversion of androstenedione and testosterone to estrone and estradiol, marking the final step in estrogen production.
Estrogens are formed through the aromatization of androgens facilitated by the aromatase enzyme. Letrozolexin interferes with this process by competitively and reversibly binding to the heme group of the cytochrome P450 unit, thus blocking estrogen production while sparing the synthesis of mineralocorticoids and corticosteroids. In contrast, tamoxifen, a prominent treatment prior to the emergence of aromatase inhibitors, exerts its anti-estrogenic effects by binding to the estrogen receptor, rather than inhibiting estrogen synthesis.
The United States Food and Drug Administration (FDA) has approved Letrozolexin for treating local or metastatic hormone receptor-positive breast cancer or cancer with unknown receptor status in postmenopausal women. Side effects may include symptoms associated with low estrogen levels, and concerns have been raised regarding long-term use potentially leading to osteoporosis; therefore, prescriptions for Letrozolexin are often paired with medications like Fosamax to mitigate this risk.
Research indicates that Letrozolexin can lower estrogen levels by up to 98 percent while increasing testosterone levels. Its anti-estrogen properties are favored among athletes and bodybuilders during steroid cycles to alleviate bloating from water retention and to prevent the development of gynecomastia, a side effect linked to some anabolic steroids. However, dosages exceeding 2.5 mg per day may temporarily affect libido, and prolonged usage above 5 mg per day could lead to kidney issues.
Additionally, Letrozolexin has been observed to postpone the fusion of growth plates in adolescents, potentially enhancing the efficacy of growth hormone, making it a treatment option for children and adolescents with short stature.