Leuprolide is a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to, and activates, GnRH / LHRH receptors. In males, Luteinizing hormone and follicle-stimulating hormone release from the anterior pituitary transiently increases testosterone concentration. However, continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production. It reduces testosterone production to castration levels (medical castration) and usually inhibits androgen receptor-positive tumor progression.
In females, Gonadotropin release from the anterior pituitary transiently increases estrone and estradiol concentrations. However, continuous, prolonged administration results in a decrease in estrogens to postmenopausal levels, leading to inhibition of estrogen-dependent cancers. In the treatment of endometriosis, as a consequence of suppression of ovarian function, both normal and ectopic endometrial tissues become inactive and atrophic. As a result, amenorrhea occurs.
Packaging: glass vials
Storage conditions: Preserve in tight containers. Store at a temperature not higher than 30°.