Exemestane

Exemestane (trade name Aromasin) is an oral estrogen-responsive) breast cancer in postmenopausal women. An aim in the treatment of hormone-receptor-positive patients in preventing recurrence is to lower estrogen levels that this breast cancer thrives on.

The main source of androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, the Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogens.

The estrogen suppression rate for exemestane varies from 85% for estradiol (E2) to 95% for estrone (E1).

References

• Extensive information, including trial statistics from the National Institutes of Health
• Aromasin official website
• Profile of exemestane for use as an anti-estrogen by athletes and bodybuilders
• Coombes RC et al. (2007). "Survival and safety of exemestane versus tamoxifen after 2–3 years' tamoxifen treatment (Intergroup Exemestane Study): a randomised controlled trial". Lancet 369 (9561): 559–70. doi:10.1016/S0140-6736(07)60200-1. PMID 17307102. Retrieved on 2007-07-22.