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Peptide

Histrelin (Vantas/Supprelin)

Histrelin is a nonapeptide GnRH agonist. FDA-approved 1991 (daily), 2004 (implant for prostate cancer), 2007 (implant for CPP). Once-yearly subcutaneous implant releases 65 mcg/day. Phase III trials show 100% achieve testosterone ≤50 ng/dL within 4 weeks. Mean testosterone 13.1 ng/dL maintained through repeated cycles. PSA decreased 90% from baseline. Also approved for central precocious puberty.

Research notice. This page is for education and research. Peptides may not be FDA-approved for human use and may only be legally available for research. Talk to a qualified clinician before considering any peptide.

Best evidence
Grade A
Conditions studied
2
Outcomes
9
Graded outcomes
5220

Evidence by condition

  • Strong
  • Moderate
  • Limited
  • Very limited

2 conditions, plus general outcomes

Early-Onset Puberty

Early-Onset Puberty: outcomes studied for Histrelin (Vantas/Supprelin)
GradeOutcomeEffectSizeStudiesPeopleStudies list
LH Suppression (CPP)

Phase III: maintained excellent suppression of peak LH for 1 year. Long-term extension showed sustained suppression for up to 6 years.

Improves (the measure goes down)Large effect10 studies

Studies that measured lh suppression (cpp)

Predicted Adult Height

In treatment-naive girls, predicted adult height increased from 151.9 to 166.5 cm (10.7 cm gain) over 60 months.

Improves (the measure goes up)Moderate effect3 studies

Studies that measured predicted adult height

Prostate Cancer

Prostate Cancer: outcomes studied for Histrelin (Vantas/Supprelin)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Testosterone Suppression

100% achieve T ≤50 ng/dL by week 4. Mean testosterone 13.1 ng/dL sustained over multiple years. 99-100% maintain castrate levels for 52 weeks.

Improves (the measure goes down)Large effect9 studies

Studies that measured testosterone suppression

PSA Suppression

PSA decreased 90% from baseline (83.6 ng/mL) by week 16 (p=0.0001). Sustained suppression over multiple treatment cycles.

Improves (the measure goes down)Large effect9 studies

Studies that measured psa suppression

Long-term Castration

T <30 ng/dL maintained in 96% at 2 years, 100% at 3-5 years. Single implant maintains castration for up to 30 months.

Improves (the measure goes up)Large effect9 studies

Studies that measured long-term castration

General

General: outcomes studied for Histrelin (Vantas/Supprelin)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Anti-Cancer Activity

13 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Moderate effect10 studies

Studies that measured anti-cancer activity

Hormone Levels

7 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Small effect8 studies

Studies that measured hormone levels

Reproductive Outcomes

6 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect7 studies

Studies that measured reproductive outcomes

Safety/Tolerability

3 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Small effect2 studies

Studies that measured safety/tolerability

Key findings

  • LH Suppression (CPP)Early-Onset PubertyImproves (the measure goes down)
  • Testosterone SuppressionProstate CancerImproves (the measure goes down)
  • PSA SuppressionProstate CancerImproves (the measure goes down)

Studies cited

31 studies from PubMed

  1. Periovulatory anticoagulant therapy enhances embryo recovery rates in superovulated mares.Theriogenology, 2025 · PMID 39490086
  2. Adverse event profile differences among long-acting gonadotropin-releasing hormone analogs: A real-world, pharmacovigilance study.PloS one, 2025 · PMID 40644420
  3. Review of drug-drug interactions in patients with prostate cancer.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, 2024 · PMID 38720547
  4. Long-term experience with the use of a single histrelin implant beyond one year in patients with central precocious pubertyJ Pediatr Endocrinol Metab, 2023 · PMID 36625262
  5. Fertility preservation in transfeminine adolescents using TESE at the time of Histrelin Acetate subcutaneous implant placement: A Case Series.Journal of pediatric urology, 2023 · PMID 37770134
  6. Case Report: Ovulation Induction in Greater One-Horned Rhinoceros (Rhinoceros unicornis).Frontiers in veterinary science, 2021 · PMID 34277752
  7. Effects of GnRH agonists on testosterone and testosterone-stimulated parameters for contraception and aggression reduction in male lion-tailed Macaques (Macaca silenus).Zoo biology, 2021 · PMID 34224162
  8. Comparative Efficacy of Histrelin Acetate and hCG for Inducing Ovulation in Brazilian Northeastern Jennies (Equus africanus asinus).Journal of equine veterinary science, 2020 · PMID 32797776
  9. Histrelin acetate-induced ovulation in Brazilian Northeastern jennies (Equus asinus) with different follicle diameters.Theriogenology, 2019 · PMID 31254727
  10. Association of Surgical Risk With Exogenous Hormone Use in Transgender Patients: A Systematic Review.JAMA surgery, 2019 · PMID 30516808
  11. Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancerBJU Int, 2015 · PMID 25548680
  12. Long-Term Continuous Suppression With Once-Yearly Histrelin Subcutaneous Implants for the Treatment of Central Precocious Puberty: A Final Report of a Phase 3 Multicenter TrialJ Clin Endocrinol Metab, 2015 · PMID 25803268
  13. A single histrelin implant is effective for 2 years for treatment of central precocious pubertyJ Pediatr, 2015 · PMID 23809043
  14. Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancerBJU Int, 2012 · PMID 21851539
  15. Histrelin: in advanced prostate cancerDrugs, 2010 · PMID 20329807
  16. Relationships between FSH, inhibin B, anti-Mullerian hormone, and testosterone during long-term treatment with the GnRH-agonist histrelin in patients with prostate cancer.European journal of endocrinology, 2010 · PMID 19820037
  17. Analysis of testosterone suppression in men receiving histrelin, a novel GnRH agonist for the treatment of prostate cancer.The Canadian journal of urology, 2010 · PMID 20735905
  18. A review of the pharmacokinetic and pharmacological properties of a once-yearly administered histrelin acetate implant in the treatment of prostate cancer.BJU international, 2009 · PMID 19228147
  19. A review of the use of histrelin acetate in the treatment of prostate cancer.BJU international, 2009 · PMID 19228148
  20. Increased risk of metabolic syndrome, diabetes mellitus, and cardiovascular disease in men receiving androgen deprivation therapy for prostate cancer.Pharmacotherapy, 2008 · PMID 19025432
  21. Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trialJ Clin Endocrinol Metab, 2007 · PMID 17327379
  22. Efficacy and safety of histrelin subdermal implant in patients with advanced prostate cancerJ Urol, 2006 · PMID 16515997
  23. The histrelin implant: a novel treatment for central precocious pubertyPediatrics, 2005 · PMID 16322137
  24. Reversibility of androgen deprivation therapy in patients with prostate cancer.The Journal of urology, 2005 · PMID 15711270
  25. An evaluation of the pharmacokinetics and pharmacodynamics of the histrelin implant for the palliative treatment of prostate cancer.Journal of clinical pharmacology, 2005 · PMID 16239357
  26. Comparison of single-agent androgen suppression for advanced prostate cancer.Reviews in urology, 2005 · PMID 16985882
  27. Effective long-term androgen suppression in men with prostate cancer using a hydrogel implant with the GnRH agonist histrelinUrology, 2001 · PMID 11597543
  28. An implant releasing the gonadotropin hormone-releasing hormone agonist histrelin maintains medical castration for up to 30 months in metastatic prostate cancerJ Urol, 2000 · PMID 10687989
  29. A review of drug-induced Leydig cell hyperplasia and neoplasia in the rat and some comparisons with man.Human & experimental toxicology, 1995 · PMID 7576816
  30. Histrelin. A review of its pharmacological properties and therapeutic role in central precocious pubertyDrugs, 1993 · PMID 7684676
  31. Lack of correlation between fertility and sperm numbers in male rats treated with histrelin, a potent LHRH agonist.Journal of andrology, 1986 · PMID 3522515