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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 ...
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
This page was last edited on 18 September 2023, at 00:24 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
[11] [4] In addition, it is described as a much more potent aromatase inhibitor than adrenal steroidogenesis inhibitor. [17] AG can inhibit aromatase by 74 to 92% and decrease circulating estradiol levels by 58 to 76% in men and postmenopausal women. [1] [7] AG is not an effective ovarian steroidogenesis inhibitor in premenopausal women. [17]
Type II aromatase inhibitors such as anastrozole and letrozole, by contrast, are not steroids and work by interfering with the aromatase's heme. [11] A study conducted on young adult males found that the estrogen suppression rate for exemestane varied from 35% for estradiol (E2) to 70% for estrone (E1). [13
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.
AIs are divided into two categories, steroidal aromatase inhibitors (SAIs, type 1 inhibitors) and non-steroidal aromatase inhibitors (type 2 inhibitors) that is based on their mechanism of action and structure. NSAIs are mainly used to treat breast cancer in women.
Fadrozole (INN Tooltip International Nonproprietary Name), sold under the brand name Afema (by Novartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer. [1] [2
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