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Leuprorelin acetate (also known as leuprolide acetate) is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH). This specific 11.25 mg 3-month depot formulation, developed by Takeda and marketed as LUPRON DEPOT-PED, is indicated for the treatment of children with central precocious puberty (CPP). As a potent GnRH receptor agonist, it initially stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). However, continuous and sustained administration leads to the downregulation and desensitization of GnRH receptors. This paradoxically results in the suppression of gonadotropin secretion, subsequently reducing sex steroid levels (testosterone in males and estradiol in females) to prepubertal ranges. This suppression effectively halts or reverses the progression of secondary sexual characteristics, slows bone age advancement, and improves predicted adult height in children with CPP.
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