Drug intelligence / Profile preview

leuprorelin + goserelin + buserelin + triptorelin

Development stage
Unknown
Lead developer
Takeda
Modality
Peptides
Administration
Intramuscular, Subcutaneous, Intranasal, Implant
01

Overview

Leuprorelin, goserelin, buserelin, and triptorelin are synthetic analogues of gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH). These drugs act as GnRH receptor agonists. Initially, they stimulate the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a temporary increase in sex hormones such as testosterone and estradiol. However, with continuous administration, they desensitize pituitary GnRH receptors, resulting in decreased LH and FSH secretion and subsequent suppression of gonadal steroidogenesis. This leads to hypogonadism with reduced levels of testosterone or estrogen. They are primarily used for androgen deprivation therapy in advanced prostate cancer but are also indicated for breast cancer, endometriosis, uterine fibroids, central precocious puberty, infertility treatments requiring ovarian suppression or stimulation protocols, and delaying puberty in transgender youth[4][5][6][8].

Brand names
LupronFensolviCamceviViadur
Other names
leuprolide (for leuprorelin)LHRH agonists (class name)GnRH agonists (class name)
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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