Drug intelligence / Profile preview

goserelin + histrelin + leuprolide + triptorelin

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

Overview

This is a combination of four gonadotropin-releasing hormone (GnRH) agonists—goserelin, histrelin, leuprolide, and triptorelin. Each of these agents acts as a synthetic analog of GnRH (also known as luteinizing hormone-releasing hormone, LHRH), binding to the GnRH receptor in the pituitary gland. After an initial stimulation that increases luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion—and thus sex steroid production—chronic administration leads to downregulation of the GnRH receptor. This results in decreased LH and FSH release and subsequent suppression of gonadal steroidogenesis (testosterone in males, estrogen in females). These drugs are primarily used for androgen deprivation therapy in advanced prostate cancer but are also indicated for breast cancer, endometriosis, central precocious puberty, uterine fibroids/bleeding disorders depending on the specific agent[1][2][3][6][8][9].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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