Drug intelligence / Profile preview

anastrozole + degarelix

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

Overview

Anastrozole + degarelix is a combination of two pharmaceutical agents used primarily in hormone-dependent cancers. Anastrozole is a non-steroidal aromatase inhibitor that blocks the conversion of androgens to estrogens by inhibiting the enzyme aromatase, thereby reducing estrogen levels in the body. This mechanism is particularly relevant for treating estrogen receptor-positive breast cancer, especially in postmenopausal women[5]. Degarelix is a synthetic peptide and gonadotropin-releasing hormone (GnRH) receptor antagonist that binds competitively to GnRH receptors in the pituitary gland, leading to rapid suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which results in decreased testosterone production[1][5]. Degarelix is approved for advanced prostate cancer but has also been studied as an ovarian function suppressor in premenopausal women with breast cancer when combined with aromatase inhibitors such as letrozole[2][6]. The combination of anastrozole and degarelix would theoretically provide dual suppression of both estrogen synthesis (via aromatase inhibition) and ovarian androgen/estrogen production (via GnRH antagonism), potentially useful for certain endocrine-responsive cancers.

02

Targets

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

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