Routes Subcutaneous implant Bioavailability 92% Protein binding 70% Metabolism Hepatic Half-life 4 hours Excretion Undetermined
A nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency.
Acts on pituitary gland gonadotropin cells to release luteinizing hormone and follicle-stimulating hormone.
Considered a gonadotropin-releasing hormone agonist or GnRH agonist.
Marketed under the brand names Vantas and Supprelin LA.
By downregulation, daily stimulation of pituitary gonadotropes causes them to become desensitized to the effects of histrelin, decreasing the levels of LH and FSH fall after a short period of time.
Continual administration causes the levels of LH and FSH in the blood remain low.
This prolonged lowering of LH and FSH levels results in the decrease the sex steroids in the blood.
Used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women, and central precocious puberty in children.
It is available as a daily intramuscular injection, in a 12-month subcutaneous implant for the palliative treatment of advanced prostate cancer.