|Trade names||Vantas, Supprelin LA, others|
|Other names||Histrelin acetate|
|Drug class||GnRH agonist; Antigonadotropin|
|Main uses||Prostate cancer|
|Side effects||Pain at the site of injection, hot flashes, breast enlargement, sexual dysfunction, tiredness, kidney problems, constipation, weight loss, trouble sleeping|
|Elimination half-life||4.0 hours|
|Chemical and physical data|
|Molar mass||1323.528 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Histrelin, sold under the brand names Vantas among others, is a medication used to treat advanced prostate cancer. It may also be used for precocious puberty and in transgender children. It is given by injection under the skin.
Common side effects include pain at the site of injection, hot flashes, breast enlargement, sexual dysfunction, tiredness, kidney problems, constipation, weight loss, and trouble sleeping. Other side effects may include osteoporosis, high blood sugar, liver problems, anaphylaxis, and pituitary apoplexy. Use in pregnancy may harm the baby. It acts similar to gonadotropin-releasing hormone (GnRH), resulting in increased luteinizing hormone (LH) and follicle stimulating hormone (FSH), and therefore decreased testosterone and estrogen.
Histrelin was approved for medical use in the United States in 1991. It is available as a generic medication. In the United States an implant costs about 5,100 USD per year as of 2021. Since 2014 it is no longer commercially available in the United Kingdom.
Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children.
Histrelin can be part of the primary care protocol in transgender children/youth, which is an off-label use in the USA and the UK, and is used in suppressing cis-sex puberty, until the patient is ready to begin cross-sex hormonal therapy. It is also sometimes prescribed to transgender adults who benefit from having their sex hormone production halted.
It is often used as a 50 mg implant, once per year.
It is available as a daily intramuscular injection. Histrelin is also available in a 12-month subcutaneous implant (Vantas) for the palliative treatment of advanced prostate cancer, since 2005 in the US, and since Jan 2010 in the UK. A 12-month subcutaneous implant (Supprelin LA) for central precocious puberty (CPP) was approved on May 3, 2007 by the U.S. Food and Drug Administration.
It acts on particular cells of the pituitary gland called gonadotropes. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist.
In a process known as downregulation, daily stimulation of pituitary gonadotropes causes them to become desensitized to the effects of histrelin. As a consequence, levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) fall after a short period of time. From that point forward, as long as histrelin is administered, the levels of LH and FSH in the blood remain low.
This prolonged lowering of LH and FSH levels is the rationale for therapy using GnRH agonists. Since LH and FSH stimulate the gonads to produce estrogens and androgens in females and males respectively, histrelin can effectively be used to decrease the sex steroids in the blood of patients.
In the United States a 50 mg implant for prostate cancer costs about 5,100 USD per year as of 2021. The implant for precocious puberty, despite being the same 50 mg dose costs about 45,000 USD as of 2021. The first medication releases 50 micrograms per day while the second releases 65 micrograms per day, which is likely of no importance.
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- "Supprelin LA Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 10 December 2021.
- "Hormone Blocker Sticker Shock: Kids Drug Costs 8 Times More Than One For Adults". NPR.org. Retrieved 10 December 2021.