Drug intelligence / Profile preview

leuprolide

Development stage
Approved
Lead developer
Takeda
Modality
Peptides, Small Molecules
Administration
Intramuscular, Subcutaneous, Implant
01

Overview

Leuprolide (also known as leuprorelin, Chinese name: 亮丙瑞林) is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH). It acts as a GnRH receptor agonist, initially stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which leads to increased levels of sex hormones. However, with continuous administration, it causes downregulation and desensitization of pituitary GnRH receptors, resulting in decreased LH and FSH secretion and subsequent suppression of testosterone and estradiol production. This mechanism underlies its use in treating advanced prostate cancer, breast cancer, endometriosis, uterine fibroids-related anemia, central precocious puberty in children, as part of transgender hormone therapy regimens for puberty suppression or chemical castration[1][2][5]. Leuprolide is administered by subcutaneous or intramuscular injection; long-term depot formulations are available.

Brand names
LupronLupron DepotEligardFensolviViadurCamcevi
Other names
leuprorelinleuprolide acetateEnantone (regional brand)Leuprolide Monoacetate
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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