March 30, 2022
Exemestane drug description
An aromatase inhibitor, an antitumor agent, is structurally similar to androstenedione, a natural steroid hormone.
An irreversible steroidal aromatase inhibitor similar in structure to androstenedione, a natural substance. In postmenopausal women, estrogen is mainly produced by the conversion of androgens to estrogen by the action of aromatase enzymes in peripheral tissues. Blocking estrogen production by inhibiting aromatase is an effective and selective treatment for hormone-dependent breast cancer in postmenopausal women. The mechanism of action of exemestane is due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation. In postmenopausal women, exemestane significantly reduces serum estrogen levels starting at a dose of 5 mg. Maximum reduction (>90%) is achieved with doses of 10-25 mg.
Exemestane for Women
In postmenopausal women, estrogen is produced primarily by the conversion of androgens to estrogen by the action of the enzyme aromatase in peripheral tissues. The action of exemestane is based on the irreversible binding of the active fraction of plant aromatase, resulting in enzyme inactivation.
Exemestane has no progesterone and estrogenic activity. When used in high doses, low androgenic activity is observed. It does not affect the biosynthesis of cortisol and aldosterone in the adrenal glands.
Even low doses of exemestane have been shown to slightly increase serum levels of LH and FSH. However, this effect is unusual for drugs of this pharmacological group. It probably develops according to reaction theory at the pituitary level. A decrease in estrogen levels stimulates the secretion of gonadotropins from the pituitary gland, even in postmenopausal women.