Drug intelligence / Profile preview

formestane + triptorelin

Development stage
Preclinical
Lead developer
Debiopharm
Modality
Peptides, Small Molecules
Administration
Intramuscular, Subcutaneous
01

Overview

Formestane + triptorelin is a combination therapy used primarily in clinical research for premenopausal women with advanced or metastatic, estrogen receptor-positive breast cancer. Formestane is a second-generation, irreversible steroidal aromatase inhibitor that blocks the conversion of androgens to estrogens, thereby reducing estrogen production. Triptorelin is a synthetic decapeptide agonist analog of gonadotropin-releasing hormone (GnRH), which suppresses pituitary secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased ovarian steroidogenesis. The rationale for combining these agents is to achieve more complete suppression of circulating estrogens than with either agent alone, potentially enhancing anti-tumor efficacy by creating a more profound hypoestrogenic state[1][2]. This approach has been shown in small studies to result in greater reductions in estradiol, estrone, and estrone sulfate compared to GnRH analog monotherapy[1][2].

Other names
4-hydroxyandrostenedione + triptorelin4-OHA + triptorelin
02

Targets

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

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