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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.
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