Drug intelligence / Profile preview

ribociclib + fulvestrant + triptorelin

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules, Peptides
Administration
Oral, Intramuscular
01

Overview

This is a combination regimen consisting of three drugs—ribociclib, fulvestrant, and triptorelin—used primarily for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. Ribociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks proteins involved in cell cycle progression, thereby slowing or stopping cancer cell growth[1][5][6]. Fulvestrant is an estrogen receptor antagonist that binds to and degrades the estrogen receptor, inhibiting estrogen-driven tumor growth. Triptorelin is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function and reduces circulating estrogen levels. This combination targets both the hormonal drivers of breast cancer and key cell cycle regulators to provide comprehensive endocrine-based therapy for premenopausal or perimenopausal women with HR-positive/HER2-negative disease[5]. The regimen may be used as initial endocrine-based therapy or after progression on prior endocrine treatments.

Other names
Ribociclib + Fulvestrant + TriptorelinRibociclib plus endocrine therapy plus GnRH agonist
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)ESR2 (ERβ)GnRHR (Gonadotropin-releasing hormone receptor)

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