Histrelin 50mg implant with device
Histrelin is a gonadotropin-releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant delivering continuous therapeutic doses.
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Suspected adverse reactions reported for Histrelin
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1 branded products available
WHO defined daily dose (DDD)
137 microgram
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
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Codes for healthcare professionals and prescribing systems
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 7 · Trials: 1 · 1993–2025
Showing the 50 most relevant studies, sorted by most relevant.
Viktoriya Tulchinskaya, Rula V. Kanj, Emery Lu
Journal of Pediatric and Adolescent Gynecology, 2023
Erica A. Eugster, William L. Clarke, Gad B. Kletter, et al.
The Journal of Clinical Endocrinology & Metabolism, 2007
- Age Determination by Skeleton
- Bone and Bones
- Breast
Silverman LA, Han X, Huang H, et al.
2021
- Subcutaneous Tissue
- Puberty, Precocious
- Leuprolide
ObjectivesGonadotropin-releasing hormone analogs are the treatment of choice for central precocious puberty (CPP). This study characterizes patients treated with histrelin implant or leuprolide injection.MethodsA US claims database was used to identify patients aged ≤20 years with ≥1 histrelin or leuprolide claim (index treatment) between April 2010 and November 2017 and continuous enrollment ≥3 months before and ≥12 months after the index treatment date.ResultsOverall, 4,217 patients (histrelin, n=1,001; leuprolide, n=3,216) were identified. The percentage of patients with CPP diagnosis was greater in the histrelin (96.5%) vs. leuprolide (68.8%; p50% of patients aged 6-9 years. Mean treatment duration was significantly longer for histrelin (26.7 ± 14.8 months) vs. leuprolide (14.1 ± 12.1 months; pConclusionsPatients with CPP treated with histrelin had a longer duration of treatment, lower rates of index treatment discontinuation, and lower annual treatment costs vs. those treated with leuprolide.
Abstract licence: CC BY 4.0
Peter N. Schlegel
British Journal of Urology, 2009
- Absorption
- Biological Availability
- Delayed-Action Preparations
Ellis Barrera, Rachel Locks, Jessica Kremen, et al.
Journal of Pediatric Urology, 2023
- Gonadotropin-Releasing Hormone
- Sperm Retrieval
- Sex Reassignment Surgery
Lauren A. Ray, George J. Eckert, Erica A. Eugster
Journal of Pediatric Endocrinology and Metabolism, 2023
- Puberty, Precocious
- Drug Implants
- Gonadotropin-Releasing Hormone
Mak A, Hwang R, Nace G Jr, et al.
2023
- Puberty, Precocious
- Gonadotropin-Releasing Hormone
- Drug Implants
Sarah Pilcher, Jeremi M. Carswell, Michael P. Kurtz, et al.
Transgender Health, 2024
Ian Marpuri, Mitchell E. Geffner, Lily C. Chao
Hormone Research in Paediatrics, 2025
N. Cazales, Florencia Pereyra, Sthefanía Icatt, et al.
Journal of Equine Veterinary Science, 2023
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
1.01 hr
Mechanism
Histrelin is a gonadotropin-releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin.
Food interactions
None known
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
0.375 ng/mL
Half-life
1.01 hr
[L41715]
Protein binding
29.5%
[L41715]
Volume of distribution
7.86 L
Metabolism
Elimination
[L41715]
Clearance
56.5 mL/min
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Initially, histrelin implants were developed to reduce testosterone to castration levels in patients with advanced prostate cancer.[L41715] The Vantas product was approved by the FDA in October 2004 for the palliative treatment of this condition.[L41715] Vantas was later discontinued by Endo Pharmaceuticals Inc. on September 21, 2021.[L41710]
GnRH agonists are the first line of treatment for children with central precocious puberty (CPP) due to their capacity to reduce LH levels and the concentration of sex steroids. As the product Supprelin LA, histrelin is indicated for the treatment of CPP in children (approved by the FDA in May 2007).[L41700]
[L41700]
As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.
[L41715]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 477 interactions
[L41715]
Patients receiving one, two or four histrelin implants (Vantas, Endo Pharmaceuticals) had similar adverse event profiles.
[L41715]
No overdose cases were reported in the clinical trials of the histrelin product Supprelin LA (Vantas, Endo Pharmaceuticals). The administration of high doses of histrelin in animal studies was associated with the expected pharmacological effects.
[L41700]
Since both products of histrelin are administered using implants that deliver a constant dose, accidental or intentional overdose is unlikely.
When administered as an implant, histrelin is delivered in continuous therapeutic doses.[L41700][L41715] 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).[L41700][L41715] 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.[L41700][L41715]
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.[A7088][L41700] In adult males with advanced prostate cancer, histrelin reduces testosterone production to castration levels, hindering the growth of prostate cancer cells.[A18505][A18506][L41715]
Both histrelin products (Vantas and Supprelin LA from Endo Pharmaceuticals) cause a transient increase in serum concentrations of estradiol in females and testosterone in both sexes during the first week of treatment.[L41700][L41715] Laboratory tests are also recommended in order to monitor hormone levels. For pediatric patients with central precocious puberty (CPP) using histrelin (Supprelin LA, Endo Pharmaceuticals), LH, follicle-stimulating hormone and estradiol or testosterone should be monitored.[L41700] In patients with advanced prostate cancer using histrelin (Vantas, Endo Pharmaceuticals), testosterone and prostate-specific antigen should be measured periodically.[L41715] Issues such as breakage during insertion and difficulty locating and removing implants have been reported.[L41700][L41715]
The Supprelin LA (Endo Pharmaceuticals) product label alerts users about psychiatric events, convulsions and cases of pseudotumor cerebri (idiopathic intracranial hypertension) that have been reported in patients receiving GnRH agonists.[L41700] The Vantas (Endo Pharmaceuticals) product label alerts users about cases of spinal cord compression and urinary tract obstruction, and an increased risk of hyperglycemia/diabetes and cardiovascular disease in men receiving GnRH agonists.[L41715]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L41715]
The continuous subcutaneous release of the histrelin implant was confirmed, as serum levels were sustained throughout the 52-week dosing period. At the end of the 52-week period, the mean serum histrelin concentration was 0.13 ± 0.065 ng/mL.
[L41715]
In patients that received a second implant at the end of the 52-week period, the serum histrelin concentration in the first eight weeks was similar to the one detected with the first implant. On average, the residual drug content of 41 histrelin implants (Vantas, Endo Pharmaceuticals) was 56.7 ± 7.71 mcg/day over 52 weeks.
[L41715]
Compared to healthy male volunteers that received a subcutaneous bolus dose, the relative bioavailability of histrelin in patients with prostate cancer and normal renal and hepatic function was 92%.
[L41715]
In children with central precocious puberty (CPP, n=47) that received a subcutaneous histrelin implant (Supprelin LA, Endo Pharmaceuticals), the median maximum serum histrelin concentration over the study period was 0.43 ng/mL, which is expected to maintain gonadotropins at prepubertal levels.
[L41700]
There were no pharmacokinetic differences between patients previously treated with luteinizing hormone-releasing hormone (LHRH) agonists and those that had not.
[L41700]
Food-drug interaction studies have not been performed for histrelin products.
[L41715][L41700]
Serum histrelin concentrations are 50% higher in prostate cancer patients with mild to severe renal impairment compared to those with no renal or hepatic impairment; however, this difference is not considered clinically relevant.
[L41715]
[L41715]
[L41715]
[L41715]
[L41715]
In an in vitro drug metabolism study using human hepatocytes, a single histrelin metabolite resulting from C-terminal dealkylation was identified.
[L41715]
[L41715]
[L41715]
Proteins and enzymes this drug interacts with in the body
ATC L02AE05
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Histrelin
Additional database identifiers
Drugs Product Database (DPD)
18561
ChemSpider
26606349
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4421
GenAtlas
GNRHR
GeneCards
GNRHR
GenBank Gene Database
L03380
GenBank Protein Database
183422
Guide to Pharmacology
256
UniProt Accession
GNRHR_HUMAN
DrugBank citations
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q5871149), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication. WHO INN from the World Health Organization.