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Is exemestane a form of chemotherapy?

Exemestane is an irreversible steroid aromatase inhibitor with a structure similar to its natural androstenedione substrate. Estrogen deprivation by inhibiting aromatase is an effective and optional method for the treatment of hormone-dependent breast cancer in postmenopausal women. It is used for advanced breast cancer in natural or artificial postmenopausal women whose condition has not progressed after tamoxifen treatment.

Exemestano


What is the pharmacological study of this product?

Exemestane is an irreversible steroid aromatase inhibitor, and its structure is similar to that of natural androstenedione substrate. Estrogen in postmenopausal women is mainly converted by androgens through the action of aromatase in peripheral tissues. Inhibiting aromatase to block the production of estrogen in patients is an effective and selective treatment for postmenopausal hormone-dependent breast cancer. Exemestane 5 mg can significantly reduce the serum estrogen level of postmenopausal women, and the dose of 10-25 Mg can reduce the estrogen level to the greatest extent (>90%). In postmenopausal patients with breast cancer, exemestane 25 mg daily reduced the overall aromatization by 98%.

Exemestane does not have progesterone and estrogen-like effects but has a slight androgen-like effect, which may be related to the structure of 17 hydroxy derivatives, and this androgen-like effect is mainly visible at high doses. In the study of repeated daily administration of exemestane, whether stimulated by ACTH or not, exemestane had no effect on the biosynthesis of cortisone and aldosterone, proving that exemestane had a selective effect on steroid metabolic enzymes.

Therefore, patients receiving exemestane do not need glucocorticoid or mineralocorticoid replacement therapy. When exemestane was applied at low doses, there was a slight dose-independent increase in serum LH and FSH levels. This effect is expected to be related to its pharmacological characteristics, which may be caused by the feedback of pituitary levels caused by the decline of estrogen levels. The decrease of estrogen levels in the body will stimulate the pituitary gland to secrete gonadotropin, and the same is true for postmenopausal women.


What is the purpose of this product?

Exemestane and tamoxifen are adjuvants for the treatment of advanced breast cancer and ovarian cancer. They are not adjuvants to chemotherapy, but one of the rehabilitation drugs after chemotherapy.

Clinically, tamoxifen is used to treat advanced breast cancer and ovarian cancer. Exemestane is a substitute player. It is used for the adjuvant treatment of early invasive stellar breast cancer in postmenopausal women with estrogen receptor-positive after 2-3 years of tamoxifen adjuvant treatment (at this time, the effect of tamoxifen is no longer obvious), until the completion of a total of 5 years of adjuvant endocrine therapy.

This product is also used for advanced breast cancer in natural or artificial postmenopausal women whose condition is still progressing after tamoxifen treatment.

The efficacy of this product in estrogen receptor-negative patients is not clear.


Clinical evaluation of this product

Exemestane is a highly effective irreversible steroid aromatase inhibitor. For tamoxifen-resistant patients, exemestane 25mg/d can obtain an objective effective rate of 15% - 28% and a median duration of 69-76 weeks. Exemestane is superior to megestrol and can prolong the time of disease progression. Exemestane can still achieve an objective effective rate of 11% - 13% in patients with deterioration after megestrol treatment. Exemestane 25mg/d had an objective effective rate of 6.6% in patients who failed to receive treatment with nonsteroidal aromatase inhibitors. There was no cross-resistance between the two drugs.


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