Leuprorelin/Leuprolide

Leuprorelin is a gonadotropin-releasing hormone analog and is a synthetic peptide. Initially, leuprorelin continuously stimulates gonadotropin-releasing hormone receptors in the anterior pituitary, causing a temporary rise in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, which in turn transiently increases testosterone in males or estrogen in females. With continued administration, prolonged receptor stimulation leads to desensitization and downregulation of gonadotropin-releasing hormone receptors, causing marked suppression of LH and FSH secretion from the pituitary. Ultimately, this can reduce testosterone in males to castration levels (chemical castration) and markedly lower estrogen levels in females.