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Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer.
Pages in category "Aromatase inhibitors" The following 76 pages are in this category, out of 76 total. This list may not reflect recent changes. ...
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]
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.
[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]
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, provides estrogen locally, so aromatase inhibitors work by reducing this estrogen production.
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]
Exemestane is known chemically as 6-methylideneandrosta-1,4-diene-3,17-dione. Like the aromatase inhibitors formestane and atamestane, exemestane is a steroid that is structurally similar to 4-androstenedione, the natural substrate of aromatase. It is distinguished from the natural substance only by the methylidene group in position 6 and an ...
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