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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 ...
Among all aromatase inhibitors, Letrozole is commonly used for improving female fertility. It works by inhibiting aromatase which is an enzyme that catalyses the conversion of androstenedione and testosterone to estrogen by hydroxylation. Hence, Letrozole inhibits the synthesis of estrogen. [18] The hypoestrogenic state boosts the release of ...
Letrozole is an orally active, nonsteroidal, selective aromatase inhibitor and hence an antiestrogen. It prevents aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of corticosteroids. [citation needed
Aromatase is localized in the endoplasmic reticulum where it is regulated by tissue-specific promoters that are in turn controlled by hormones, cytokines, and other factors. It catalyzes the last steps of estrogen biosynthesis from androgens (specifically, it transforms androstenedione to estrone and testosterone to estradiol ).
Aromatase inhibitors are a common fertility treatment to treat women with PCOS. A meta-analysis analyzing live birth rates for women with PCOS treated with clomiphene compared to letrozole found that letrozole resulted in higher live birth rates. [11] However, ovulation induction remains an off-label indication, which affects use.
Aromatase inhibitors affect the ability of estrogens production from androgens by inhibiting the aromatase enzyme activity which is a part of the estrogen pathway. [13] The two categories of AIs are based on their mechanism of action and structure.
Although aromatase inhibitors and antigonadotropins can be considered antiestrogens by some definitions, they are often treated as distinct classes. [9] Aromatase inhibitors and antigonadotropins reduce the production of estrogen, while the term "antiestrogen" is often reserved for agents reducing the response to estrogen. [10]
A group of drugs called aromatase inhibitors are commonly prescribed to postmenopausal women who test positive for hormone receptor-positive cancer. Aromatase in fat and muscle can circulate estrogen in postmenopausal women. [12] Aromatase in highly estrogen-sensitive tissues, such as the breast, uterus, vagina, bone, and blood vessels ...
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