NCIt synonyms : SR PT105; Leuprorelin Acetate Sustained-release Microspheres PT105;
NCIt definition : A sustained-release (SR) injectable microsphere formulation composed of the acetate
salt of leuprolide, a synthetic, long-acting nonapeptide analog of the endogenous
hormone 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 females, prolonged administration results in a decrease in estradiol production
and suppression of ovarian function. Leuprolide also reduces testosterone production
to castration levels and may inhibit androgen receptor-positive tumor progression.;