Pharmacological action

Irreversible steroidal aromatase inhibitor, similar in structure to the natural substance androstenedione.

In postmenopausal women, estrogens are produced primarily by converting androgens to estrogens under the action of the aromatase enzyme in peripheral tissues. Blocking the formation of estrogen by inhibiting aromatase is an effective and selective method for treating hormone-dependent breast cancer in postmenopausal women. The mechanism of action of the drug Aromazin® is due to the fact that it binds irreversibly to the active fragment of the enzyme, causing its inactivation. In postmenopausal women, Aromazin® significantly reduces serum estrogen concentration, starting at a dose of 5 mg, with a maximum reduction (> 90%) achieved with doses of 10-25 mg. In postmenopausal patients diagnosed with breast cancer who received 25 mg of the drug daily, the total level of the aromatase enzyme in the body decreased by 98%.

Exemestane does not possess progestagenic and estrogenic activity. Only minor androgenic activity is revealed, mainly when used in high doses.

Aromazin® does not affect the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids.

When using the drug even in low doses, a slight increase in the content of LH and FSH in the blood serum is observed, which is characteristic for the preparations of this pharmacological group and is likely to develop on the basis of feedback at the pituitary level: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also women in postmenopausal women.

Indications

- common breast cancer in women in natural or induced postmenopausal women with progression of the disease against the background of anti-estrogen therapy, as well as with the progression of the disease after repeated use of various types of hormone therapy;

- adjuvant therapy for early breast cancer in postmenopausal women with estrogen-positive receptors or with an unknown receptor status after completion of 2-3 years of initial adjuvant tamoxifen therapy to reduce the risk of relapse (distant or regional) and contralateral breast cancer glands.