Histrelin
Also known as: Supprelin LA, Vantas
Histrelin is a GnRH receptor agonist that initially stimulates and then, through continuous implant delivery, downregulates pituitary GnRH receptors to suppress LH, FSH and sex steroid production.
- Drug class
- GnRH agonist (gonadotropin-releasing hormone agonist)
- Primary targets
- GnRH receptor, Pituitary gonadotrophs, LH/FSH secretion
- Dose reference
- Reference (not a recommendation): one 50 mg subcutaneous implant per 12 months, delivering roughly 50-65 mcg histrelin per day per FDA labels.
- Half-life
- Continuous release for ~12 months from the implant; terminal half-life of the peptide is ~3.9 hours (clearance ~179 mL/min) after the implant is removed.
- Developer / origin
- Valera Pharmaceuticals / Indevus / Endo (Supprelin LA marketed by Endo)
- Reference year
- 1991
- Evidence score
- 4/5 - Approved with phase 3 label-backed evidence
Approved uses
- Central precocious puberty in children (Supprelin LA)
- Palliative treatment of advanced prostate cancer (Vantas, discontinued 2021)
Approved with phase 3 label-backed evidence
Histrelin is FDA approved as a 12-month subcutaneous implant, with phase 3 trial and prescribing-information support for central precocious puberty (Supprelin LA) and, historically, advanced prostate cancer (Vantas, discontinued in 2021).
Investigational compound with human randomized or phase 2/3 evidence.
Evidence basis
- Phase 3 multicenter trial in children with CPP showed rapid, sustained LH and sex-steroid suppression over 12 months (Eugster, JCEM 2007)
- Phase 3 prostate cancer trial showed ~100% castrate testosterone by week 4 maintained through 52 weeks with PSA decline (Schlegel, J Urol 2006)
- FDA/DailyMed labels for Supprelin LA and Vantas establish mechanism, dosing and safety
- Pharmacokinetic data (terminal half-life ~3.9 h, clearance ~179 mL/min) from FDA labels
Key references
- DailyMedSupprelin LA (histrelin acetate) implant prescribing information
- FDAVantas (histrelin implant) prescribing information
- PubMedEfficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial
- PubMedEfficacy and safety of histrelin subdermal implant in patients with advanced prostate cancer
How to read this entry
Dose references and half-life values are pulled from trial protocols, labels, reviews, or published summaries where available. They are context for research and comparison, not a personal dosing recommendation.
Status matters: approved drugs have regulated indications; investigational compounds are still being studied; research-only peptides do not have established human dosing, safety, or efficacy for consumer use.
Histrelin guides
Read the matching guide or adjacent research pages for more context.
Peptide calculators
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Triptorelin is a potent GnRH-receptor agonist that first transiently stimulates LH and FSH release, then, with continuous exposure, downregulates and desensitizes pituitary GnRH receptors to suppress gonadotropins and sex steroids.
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Goserelin is a synthetic decapeptide GnRH agonist that first stimulates and then, with continuous depot exposure, downregulates pituitary GnRH receptors to suppress LH, FSH and downstream sex steroids toward castrate or postmenopausal levels.
Buserelin
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Buserelin is a GnRH receptor superagonist that initially stimulates and then, with continuous non-pulsatile exposure, desensitizes pituitary gonadotrophs to suppress LH, FSH and downstream testosterone or estradiol production.
Nafarelin
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Nafarelin is a potent GnRH receptor agonist that initially stimulates pituitary LH and FSH release but with continued dosing downregulates the receptor, suppressing gonadotropins and sex steroid production.