Drug intelligence / Profile preview

letrozole + anastrozole + goserelin acetate

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

This is a combination therapy consisting of two aromatase inhibitors, letrozole and anastrozole, together with the gonadotropin-releasing hormone (GnRH) agonist goserelin acetate. Letrozole and anastrozole both inhibit the enzyme aromatase, which is responsible for converting androgens to estrogens in peripheral tissues. Goserelin acetate suppresses ovarian function by downregulating pituitary secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased estrogen production from the ovaries. This combination aims to achieve profound estrogen suppression in premenopausal women with hormone receptor-positive breast cancer. While combinations of goserelin with either letrozole or anastrozole are established as effective endocrine therapies for premenopausal women with advanced or metastatic breast cancer, there is no evidence supporting the routine clinical use of all three agents together as a single regimen[1][2][3][4][5][6]. The rationale would be maximal estrogen deprivation; however, this specific triple combination has not been reported in clinical trials or guidelines.

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CYP19A1 (Aromatase)

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