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Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally ...
Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor medication that is used in the treatment of breast cancer for post-menopausal women. [1]It was patented in 1986 and approved for medical use in 1996. [4]
Side effects of antihormone therapy are generally minimal, but can produce similar feelings to menopause in women. [4] Common symptoms of all antihormone therapies include irregular menstrual cycles, hot flashes, weight gain, vaginal dryness, headaches, mood swings and hair thinning. [ 4 ]
Aromatase inhibitors, which stop the production of estrogen in postmenopausal women, have become useful in the management of patients with breast cancer whose lesion was found to be estrogen receptor positive. [33] Inhibitors that are in current clinical use include anastrozole, exemestane, and letrozole.
The progression has been necessary as the first-generation of drug-induced inhibitors of the enzyme were not particularly potent and lacked specificity that would often produce side effects unrelated to estrogen deprivation. Thus, development from first-generation to third-generation has given remarkable specificity and potency.
The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 mg/day in humans. [ 3 ] [ 2 ] As such, 1 mg/day is considered to be the minimal dosage required to achieve maximal suppression of aromatase with anastrozole. [ 3 ]
Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also ...