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Histrelin is a GnRH agonist found in subcutaneous implants used for the treatment of pediatric patients with central precocious puberty and the palliative treatment of advanced prostate cancer.
Histrelin is a GnRH agonist found in subcutaneous implants used for the treatment of pediatric patients with central precocious puberty and the palliative treatment of advanced prostate cancer.
Histrelin is a gonadotropin-releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin. GnRH binds to the GnRH receptor located on the pituitary gonadotrophs, and this leads to the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as the regulation of sexual maturation and reproductive function. When administered as an implant, histrelin is delivered in continuous therapeutic doses. As a GnRH agonist, this drug binds and, at first, activates the GnRH receptor. This increases the circulating levels of LH and FSH, leading to a transient increase in the concentration of gonadal steroids (testosterone and dihydrotestosterone in males and estrone and estradiol in premenopausal females). However, the continuous administration of histrelin induces the reversible down-regulation of the GnRH receptor and the desensitization of pituitary gonadotropes, which reduce LH and FSH levels. Pediatric patients with central precocious puberty (CPP) have a lower height potential. When treated with histrelin, LH levels in CPP are lowered, reducing the concentration of sex steroids. In adult males with advanced prostate cancer, histrelin reduces testosterone production to castration levels, hindering the growth of prostate cancer cells.
As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.
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