The active pharmaceutical ingredient Of exemestane is an endocrine drug for the treatment of breast cancer. It is an aromatase inhibitor that inhibits the activity of aromatase to achieve the purpose of anti-tumor therapy. Exemestane tablets are currently clinically used It is suitable for the treatment of breast cancer patients with advanced hormone receptor-positive breast cancer after the application of tamoxifen.

Name: Exemestane

Chinese name: Exemestane

Cas Number: 107868-30-4

Source: India

Qualifications: USDMF/CEP

Filing status: Filing

The mechanism of action of the raw material exemestane

Research has confirmed that estrogen is closely related to the continuous growth of breast tumors, and endocrine therapy occupies a very important position. Endocrine therapy drugs include anti-estrogens, aromatase inhibitors, and luteinizing hormone releasing hormone analogs.

Exemestane is the second-generation aromatase inhibitor! Aromatase can catalyze the conversion of androgens to estrogen and is the main source of estrogen in postmenopausal women. Therefore, aromatase inhibitors inhibit the conversion of aromatase and reduce estrogen in the body. The growth of breast cancer cells depends on estrogen, and the occurrence and development of breast cancer are closely related to the effects of estrogen. Therefore, aromatase inhibitors can inhibit the production of estrogen in postmenopausal women and selectively treat postmenopausal hormone-dependent breast cancer.

Exemestane can irreversibly bind to aromatase to inactivate it, thereby preventing the biosynthesis of estrogen. Clinically, it is often used in adjuvant therapy for advanced breast cancer patients who have progressed after tamoxifen treatment and early breast cancer.

Exemestane is suitable for patients who are resistant to tamoxifen. The results of a long-term study showed that after 2-3 years of adjuvant treatment of breast cancer, it is more effective to switch from tamoxifen to exemestane than to continue taking tamoxifen. However, how to choose the medication should still follow the doctor's advice and should not change the medication without authorization.

The product advantages of the API Exemestane

Exemestane tablets are developed and produced by Pfizer. They were approved by the FDA in 1999 and entered the Chinese market on December 17, 2008. Exemestane is a third-generation new steroidal irreversible aromatase inhibitor with low side effects and convenient use. It can irreversibly bind to aromatase to inhibit the biosynthesis of estrogen in the body, thereby reducing circulation and tumor copy The level of estrogen at the site can inhibit the growth of breast cancer, and it has a significant effect on estrogen-dependent tumors such as endometrial cancer.

Because exemestane and non-steroidal aromatase inhibitors have different enzyme sites, they have no cross-resistance to each other, and this product may still be effective for patients who use other aromatase inhibitors that are not effective. Exemestane can effectively and selectively treat postmenopausal hormone-dependent breast cancer. Because it is well tolerated and has no obvious side effects, exemestane will gradually become the first-line treatment for advanced breast cancer. Compared with megestrol acetate, exemestane is better in terms of effectiveness, safety and side effects, especially in terms of tumor shrinkage, prolonged survival and stable disease; compared with similar drugs formestane Compared with exemestane, it can be taken orally and is convenient to use. The sales volume of Exemestane continued to grow after entering the Chinese market. In 2019, it exceeded 300 million yuan to 308 million yuan, a year-on-year increase of 9.61%.