What is exemestane?

Exemestane is a hormone therapy drug used to treat breast cancer in women who have gone through a natural menopause (when periods stop). It can also be used in premenopausal women having ovarian suppression (treatment to stop the ovaries working).

You may also hear it called Aromasin, which is its best-known brand name. There are a number of other brands of exemestane, all of which contain the same dose of the drug.

Men with breast cancer may be given exemestane, although another drug called tamoxifen is more commonly used

How exemestane works

Aromatase works by reducing the amount of oestrogen made in the body.

Some breast cancers use oestrogen in the body to help them to grow. These are known as oestrogen receptor positive or ER+ breast cancers.

Exemestane belongs to a group of drugs called  aromatase inhibitors.

Who might be offered exemestane?

Exemestane is suitable for women who have been through the menopause and whose breast cancer is oestrogen receptor positive.

Sometimes exemestane is given alongside ovarian suppression to women who haven’t yet been through the menopause.

If your cancer is hormone receptor negative, then exemestane will not be of any benefit.

Androgenic steroids are ergogenic drugs enhancing the muscular mass and strength in both male and female athletes. Consequently, androgens are banned for usage in sports by the World Anti-Doping Agency (WADA).

To circumvent the imposed ban, several strategies have been developed; for instance, the use of aromatase inhibitors. Aromatase inhibitors are widely used in clinical settings and are of 2 types: steroids and nonsteroids.

Exemestane is the representative of steroidal aromatase inhibitors in the clinic. Aminoglutethimide, letrozole, and anastrozole are the most commonly available nonsteroid aromatase inhibitors.

Aromatase (estrogen synthetase) is omnipresent in several human tissues, and it catalyzes the conversion of androgens to estrogens. In addition, it converts the adrenally generated androstenedione into estrone and testosterone into estradiol in peripheral tissues, as well as in tumors. Aromatase inhibitors can suppress the aromatase activity by competitively binding to the heme of its cytochrome P450 subunit. They are commonly employed for the treatment of postmenopausal women with hormone-sensitive breast cancer. After oral administration, increased serum testosterone levels have been observed. Hence, male athletes use aromatase inhibitors to improve athletic performance and treat the adverse effects of an extensive abuse of anabolic androgenic steroids (gynecomastia).




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