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Exemestane is an irreversible steroid aromatase inhibitor. Its structure is similar to that of aromatase’s natural substrate, androstenedione, and acts as a pseudosubstrate. Postmenopausal women’s estrogen is mainly converted from androgen (produced by the adrenal cortex) by aromatase in the surrounding tissue. This drug irreversibly binds with the active site on aromatase to deactivate it, thus dramatically lower estrogen levels in the blood circulation of postmenopausal women. By inhibiting aromatase to lower estrogen levels, it can be used to treat hormone-dependent breast cancer in postmenopausal women.
Exemestane is suitable for treating advanced breast cancer in naturally or artificially postmenopausal women that has not responded well to tamoxifen treatment. It is also suitable for treating estrogen and progesterone receptor positive postmenopausal advanced breast cancer, and it can also be used to treat metastasized breast cancer and as adjuvant therapy for 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.
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