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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 ...
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 ...
Letrozole Exemestane is an irreversible "aromatase inactivator" which is superior to megestrol acetate for treatment of tamoxifen -refractory metastatic breast cancer, and does not appear to have the osteoporosis -promoting side effects of other drugs in this class.
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 ...
There are azole derivatives containing imidazole ring such as fadrozole and liarozole together with derivatives containing 1,2,4 triazole ring such as letrozole, anastrozole and vorozole. [30] The effect of 1,2,3-triazole instead of 1,2,4-triazole has been examined in the letrozole structure. [31]
Anastrozole was patented in 1987 and was approved for medical use in 1995. [8] [9] It is on the World Health Organization's List of Essential Medicines. [10] Anastrozole is available as a generic medication. [7] In 2022, it was the 179th most commonly prescribed medication in the United States, with more than 2 million prescriptions. [11] [12]
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 ]
Inhibitors that are in current clinical use include anastrozole, exemestane, and letrozole. Aromatase inhibitors are also beginning to be prescribed to men on testosterone replacement therapy as a way to keep estrogen levels from spiking once doses of testosterone are introduced to their systems.