Drug intelligence / Profile preview

fulvestrant + goserelin

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Peptides, Small Molecules
Administration
Intramuscular, Subcutaneous
01

Overview

Fulvestrant + goserelin is a combination hormone therapy used primarily for premenopausal women with hormone receptor-positive (HR+), HER2-negative metastatic breast cancer. Fulvestrant is a pure estrogen receptor antagonist that blocks and degrades estrogen receptors, while goserelin is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function, reducing estrogen production in premenopausal women. This combination effectively creates a dual blockade of estrogen signaling, which can help stop the growth of estrogen-dependent breast cancer cells. Clinical studies have shown promising results for this combination, particularly in premenopausal women with tamoxifen-pretreated metastatic breast cancer. In one phase II study, fulvestrant plus goserelin demonstrated improved time to progression compared to goserelin alone (16.5 months vs 13.5 months)[1]. The combination has shown clinical benefit rates of approximately 58% in some studies[2]. This therapy is typically administered as fulvestrant 500 mg via intramuscular injection and goserelin 3.6 mg subcutaneously every 4 weeks. The combination may also be used with CDK4/6 inhibitors like ribociclib or palbociclib for enhanced efficacy in advanced breast cancer settings[3][9].

02

Targets

ESR1 (ERα)GnRHR (Gonadotropin-releasing hormone receptor)

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