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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 ...
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]
Scientists have found that the hormone therapy - called anastrozole - can p revent women from developing breast cancer and that the protective effect lasts for years after the treatment has ended.
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 ...
Third-generation, anastrozole and letrozole are very selective, they only inhibit the aromatase enzyme and do not have an effect on other steroidogenic pathways. [21] Mechanism of NSAIs is a reversible binding process where NSAIs binds to the aromatase enzyme through non-covalent interactions. [22] NSAIs do not destroy the enzyme like SAIs do.
Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, [6] [7] aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues.
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.