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Exemestane, sold under the brand name Aromasin among others, is a medication used to treat breast cancer. It is a member of the class of antiestrogens known as aromatase inhibitors. Some breast cancers require estrogen to grow. Those cancers have estrogen receptors (ERs), and are called ER-positive. They may also be called estrogen-responsive ...
Exemestane went through clinical trials in the 1990s and received FDA approval in 1999, marketed as Aromasin. Indication for exemestane is advanced breast cancer in postmenopausal women, where the cancer has progressed following tamoxifen therapy. Exemestane is the first oral aromatase inactivator. [5]
Irreversible steroidal inhibitors, such as exemestane (Aromasin), forms a permanent and deactivating bond with the aromatase enzyme. Nonsteroidal inhibitors, such as the triazoles anastrozole (Arimidex) and letrozole (Femara), inhibit the synthesis of estrogen via reversible competition.
Non-Steroidal Aromatase Inhibitors (NSAIs) are one of two categories of aromatase inhibitors (AIs). 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.
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]
SERMs that have not been approved for medical use include arzoxifene, brilanestrant, clomifenoxide (clomiphene N-oxide; metabolite of clomifene), [3] droloxifene (3-hydroxytamoxifen), etacstil, fispemifene, GW-7604 (4-hydroxyetacstil; metabolite of etacstil), idoxifene (pyrrolidino-4-iodotamoxifen), levormeloxifene ((L)-ormeloxifene), miproxifene, nafoxidine, nitromifene (CI-628), NNC 45-0095 ...
Exemestane, aromasin, and by extension all estrogen-like compounds and aromatase inhibitors that mimic estrogen in function will be increased in effect, causing increased estrogen retention and increased drug retention. [72] Etoposide interferes with grapefruit, orange, and apple juices. [12]
Interim phase III trial results in 2011, showed that adding Afinitor (everolimus) to exemestane therapy against advanced breast cancer can significantly improve progression-free survival compared with exemestane therapy alone. [25] A study published in 2012, shows that everolimus sensitivity varies between patients depending on their tumor ...