NCIt definition : The mesylate salt form of leuprolide, a synthetic nonapeptide analogue of gonadotropin-releasing
hormone (GnRH), with potential antineoplastic activity. Upon administration, leuprolide
binds to and activates the gonadotropin-releasing hormone receptor (GnRHR). The continuous
stimulation of GnRHR by leuprolide results in both the desensitization of pituitary
GnRHR and the inhibition of pituitary secretion of the gonadotropins follicle stimulating
hormone (FSH) and luteinizing hormone (LH). In males, this results in a significant
decline in testosterone production to castration levels and may inhibit androgen receptor-positive
tumor progression.;