Altamofen-10 Alpha Pharma

Nolvadex is a non-steroidal antiestrogenic agent that also has weak estrogenic properties. Its action is based on the ability to block estrogen receptors. Tamoxifen, as well as some of its metabolites, compete with estradiol at the site of binding to the cytoplasmic estrogen receptors in the tissues of the mammary gland, uterus, vagina, anterior pituitary gland and tumors with a high estrogen receptor content.

In contrast to the receptor complex of estrogen, the receptor complex of tamoxifen does not stimulate the synthesis of DNA in the nucleus, but inhibits cell division, which leads to regression of tumor cells and their death.

Pharmacodynamics

Nolvadex is a non-steroidal drug from the group of triphenylethylenes, which has a combined spectrum of the pharmacological action of both the antagonist and the estrogen agonist in various tissues. In patients with breast cancer in tumor cells, tamoxifen mainly manifests an anti-estrogenic effect, preventing the binding of estrogens to estrogen receptors.

Nolvadex, as well as some of its metabolites, compete with estradiol for binding sites to the cytoplasmic estrogen receptors in the tissues of the mammary gland, uterus, vagina, anterior pituitary gland and tumors with a high estrogen receptor content. In contrast to the receptor complex of estrogen, the receptor complex of tamoxifen does not stimulate DNA synthesis in the nucleus, but inhibits cell division, which leads to regression of tumor cells and their death.

In women with estrogen-positive / unspecified mammary tumors, adjuvant tamoxifen therapy significantly reduces recurrence of the disease and prolongs life expectancy to 10 years. A more pronounced effect is achieved with treatment for five years than with 1- or 2-year treatment and does not depend on age, climacteric status, dose of tamoxifen or adjuvant chemotherapy.

In approximately 10-20% of postmenopausal women, tamoxifen leads to a decrease in the concentration of total cholesterol and low-density lipoprotein in the blood plasma. In addition, there are reports that in women in the postmenopausal period tamoxifen retains bone mineral density. The variability of the clinical response to the use of tamoxifen may be related to polymorphism of the CYP2D6 isoenzyme. A low metabolic rate may be associated with a reduced therapeutic response. There are no recommendations for tamoxifen treatment of “slow” metabolizers of the CYP2D6 isoenzyme.

Indications for use

• Adjuvant therapy for early breast cancer with estrogen-positive receptors;
• Treatment of locally advanced or metastatic breast cancer with estrogen-positive receptors;
• Breast cancer (including men after castration).
• The drug can also be used in other solid tumors resistant to standard methods of treatment, in the presence of overexpression of estrogen receptors.