The third generation aromatase inhibitors, used in the treatment of metastatic breast cancer and used as aid in the treatment of early breast cancer.Many breast cancers are stimulated to grow by the female sex hormones oestrogen and progesterone. These breast cancers are called hormone sensitive or hormone receptor positive and can be treated with drugs that block the effects of these hormones.In women who have had their menopause, oestrogen is mainly produced by changing androgens (sex hormones produced by the adrenal glands) into oestrogens. This process is called aromatisation and happens mainly in the fatty tissues, muscle and the skin. It needs a particular enzyme called aromatase.Exemestane blocks the process of aromatisation. So it lowers the amount of oestrogen in the body. In early breast cancer, taking exemestane can help to stop breast cancer coming back. In advanced breast cancer the cancer cells may grow more slowly or stop growing completely.
Exemestane (trade name Aromasin) is a drug used to treat breast cancer. It is a member of the class of drugs 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,hormonally-responsive, hormone-receptor-positive. Aromatase is an enzyme that synthesizes estrogen. Aromatase inhibitors block the synthesis of estrogen. This lowers the estrogen level, and slows the growth of cancers.
1. Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women.
2. Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione.
3. 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."
4. By being structurally similar to enzyme targets, Exemestane permanently binds to the enzymes, preventing them from converting androgen into estrogen
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