Therapeutic review: deslorelin acetate subcutaneous implant.

摘要

Deslorelin is a synthetic analog of endogenously occurring gonadotropin-releasing hormone (GnRH) that is believed to be 10 times more potent than the naturally occurring compound.1 The synthetic analog differs from natural GnRH in amino acid sequence by D-tryptophan at position 6 rather than glycine and terminating at position 9 with proethylamide rather than glycine-amide.2 and 3 Deslorelin acts similarly to GnRH by stimulating pituitary secretion of the gonadotropins luteinizing hormone and follicle-stimulating hormone, resulting in estrus and ovulation, as well as stimulating production of GnRH receptors on cell membranes.4 and 5 However, continuous secretion of GnRH or chronic administration of its analogs stimulates the GnRH receptors, causing down-regulation and reduction in gonadotropin release and decreased production and circulation of estrogen, progesterone, and testosterone.