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ribociclib + tamoxifen + goserelin
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous
01
Overview
This is a **triple-drug combination** of ribociclib (a selective cyclin-dependent kinase 4/6 inhibitor), tamoxifen (a selective estrogen receptor modulator), and goserelin (a gonadotropin-releasing hormone agonist). This regimen is studied primarily in **premenopausal or perimenopausal women with advanced or metastatic, hormone receptor-positive (HR+), HER2-negative breast cancer**. Ribociclib inhibits CDK4/6, blocking cell cycle progression in tumor cells. Tamoxifen blocks estrogen's effect on breast tissue, while goserelin suppresses ovarian estrogen production via downregulation of the pituitary-gonadal axis. The triple therapy was investigated in the MONALEESA-7 trial, showing improved progression-free survival versus placebo plus endocrine therapy, but ribociclib is *not indicated with tamoxifen* due to an increased risk of QT prolongation and possible liver toxicity; regulatory approvals focus on ribociclib with aromatase inhibitors plus goserelin[1][2][3][5].
- Other names
- ribociclib + tamoxifen + goserelin
02
Targets
ER (Estrogen receptor)GnRHR (Gonadotropin-releasing hormone receptor)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)
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