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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 ...
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.
1,4,6-Androstatriene-3,17-dione (ATD) is a potent irreversible aromatase inhibitor that inhibits estrogen biosynthesis by permanently binding and inactivating aromatase in adipose and peripheral tissue. [1] It is used to control estrogen synthesis. [2]
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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
Atamestane (developmental code name SH-489), also known as metandroden, as well as 1-methylandrosta-1,4-diene-3,17-dione, is a steroidal aromatase inhibitor that was studied in the treatment of cancer. [2] It blocks the production of estrogen in the body. The drug is selective, competitive, and irreversible in its inhibition of aromatase.
Although it is most potent in inhibiting aromatase among the enzymes it targets, AG is described nonetheless as a relatively weak aromatase inhibitor. [11] [4] In addition, it is described as a much more potent aromatase inhibitor than adrenal steroidogenesis inhibitor. [17]
CYP19A1 (aromatase) CYP21A2 (steroid 21-hydroxylase) CYP24A1 (1,25-dihydroxyvitamin D3 24-hydroxylase) CYP27A1 (sterol 27-hydroxylase) CYP27B1 (25-hydroxyvitamin D3 1α-hydroxylase) CYP39A1 (oxysterol 7α-hydroxylase 2) CYP46A1 (cholesterol 24-hydroxylase) CYP51A1 (lanosterol 14α-demethylase)
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