exemestane + goserelin + z-endoxifen

This drug combination consists of three agents used primarily in the treatment of hormone receptor-positive breast cancer in premenopausal women. - **Exemestane** is a third-generation aromatase inhibitor that irreversibly binds to and inhibits aromatase, the enzyme responsible for estrogen biosynthesis, thereby lowering estrogen levels and slowing growth of estrogen receptor-positive (ER+) cancers. - **Goserelin** is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function by downregulating pituitary release of luteinizing hormone, leading to decreased estrogen production in premenopausal women. - **(Z)-Endoxifen** is an active metabolite of tamoxifen and acts as a selective estrogen receptor modulator (SERM). It competitively inhibits binding of estrogen to the estrogen receptor on cancer cells, blocking proliferative signaling. It may be effective even when tamoxifen metabolism is impaired. The combination aims to provide comprehensive hormonal blockade by reducing systemic estrogen production via exemestane and goserelin while directly antagonizing ER signaling with z-endoxifen. This regimen is under investigation as neoadjuvant therapy for ER+/HER2- breast cancer in premenopausal women, with clinical trials such as EVANGELINE evaluating its efficacy compared to standard exemestane plus goserelin therapy[1][3][5][6].

Other names

(Z)-endoxifen(Z)-4-hydroxy-N-desmethyltamoxifen