Drug intelligence / Profile preview

ribociclib + goserelin + non-steroidal aromatase inhibitor

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

A combination therapy consisting of **ribociclib** (a selective cyclin-dependent kinase 4/6 [CDK4/6] inhibitor), **goserelin** (a gonadotropin-releasing hormone [GnRH] agonist), and a **non-steroidal aromatase inhibitor** (NSAI, typically either letrozole or anastrozole). Ribociclib inhibits CDK4 and CDK6 to block cell cycle progression in hormone receptor-positive (HR+), HER2-negative breast cancer cells. Goserelin suppresses ovarian estrogen production in premenopausal and perimenopausal patients by downregulating pituitary secretion of luteinizing hormone, leading to ovarian suppression. The NSAI (letrozole or anastrozole) inhibits aromatase, the enzyme responsible for conversion of androgens to estrogens, further reducing estrogen levels. This combination is used to treat HR+/HER2- advanced or early breast cancer, particularly in premenopausal and perimenopausal women, and has demonstrated significant improvements in progression-free and invasive disease-free survival compared to endocrine therapy alone or chemotherapy, while having a favorable tolerability profile[1][2][3][4][5][6][7].

Brand names
Kisqali + non-steroidal aromatase inhibitor + ovarian function suppression
Other names
ribociclib + NSAI + OFS
02

Targets

CYP19A1 (Aromatase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)GnRHR (Gonadotropin-releasing hormone receptor)

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