Histrelin

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Histrelin
Histrelin.svg
Systematic (IUPAC) name
5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-N5-(diaminomethylene)-L-ornithyl-N-ethyl-L-prolinamide
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a601146
Pregnancy cat. X (US)
Legal status -only (US)
Routes Subcutaneous implant
Pharmacokinetic data
Bioavailability 92%
Protein binding 70%
Metabolism Hepatic
Half-life 4.0 hours
Excretion Undetermined
Identifiers
CAS number 76712-82-8 N
ATC code L02AE05
PubChem CID 25077993
ChemSpider 10482012 YesY
UNII H50H3S3W74 YesY
KEGG D02369 YesY
ChEMBL CHEMBL1201255 N
Chemical data
Formula C66H86N18O12 
Mol. mass 1323.5 g/mol
 N (what is this?)  (verify)

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 Endo Pharmaceuticals under the brand names Vantas and Supprelin LA.

Pharmacology[edit]

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.

Indications[edit]

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 (since 2005 in the US, and since Jan 2010 in the UK[4]).

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.

References[edit]

  1. ^ Histrelin acetate (Vantas) - New Drug Bulletins
  2. ^ Histrelin consumer information
  3. ^ 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:10.1210/jc.2006-2479. PMID 17327379. Retrieved 2007-10-17. 
  4. ^ Daily Mail 6 April 2010, p48 "Implant ends the misery of prostate jabs"

External links[edit]