Histrelin
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Histrelin
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | H01 |
| PubChem | ? |
| Chemical data | |
| Formula | C66H86N18O12 |
| Mol. mass | 1323.5 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 92% |
| Protein binding | 70% |
| Metabolism | Hepatic |
| Half life | 4 hours |
| Excretion | Undetermined |
| Therapeutic considerations | |
| Pregnancy cat. |
X(US) |
| Legal status | |
| Routes | Subcutaneous implant |
Histrelin acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency.[1] When present in the bloodstream, 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.
Histrelin is marketed by Indevus Pharmaceuticals under the brand names Vantas and Supprelin LA.
[edit] Pharmacology
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 LH and 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.
[edit] Indications
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.[2][3]
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. 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.
[edit] References
- ^ Histrelin acetate (Vantas) - New Drug Bulletins
- ^ Histrelin consumer information
- ^ Eugster, Erica A.; William Clarke, et. al (2007). "Efficacy and Safety of Histrelin Subdermal Implant in Children with Central Precocious Puberty: A Multicenter Trial". J Clin Endocrinol Metab 92 (5): 1697–1704. doi:.
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