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Histrelin (Vantas/Supprelin)

Peptide

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.

Quick Answer

What it is

Histrelin is a nonapeptide GnRH agonist. FDA-approved 1991 (daily), 2004 (implant for prostate cancer), 2007 (implant for CPP).

Key findings

  • Grade A: Testosterone Suppression (Prostate Cancer)
  • Grade A: PSA Suppression (Prostate Cancer)
  • Grade A: Long-term Castration (Prostate Cancer)

Safety

No specific caution or interaction language was detected in the current summary/outcome notes.

⚠ī¸ Research Notice

This peptide information is for educational and research purposes only. Peptides may not be FDA-approved for human use and may only be legally available for research purposes. Consult qualified healthcare professionals before considering any peptide compounds.

ℹī¸ Quick Facts: Histrelin (Vantas/Supprelin)

Quick Facts: Histrelin (Vantas/Supprelin)

  • Best Evidence:Grade A
  • Conditions Studied:2
  • Research Outcomes:9
  • Grade A Findings:5
  • Grade B Findings:2
  • Key Effect:Prostate Cancer
A5
B2
C2
D0
2 conditions ¡ 9 outcomes

Detailed Outcomes

|
A
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.
large↓Improves
A
PSA Suppression
PSA decreased 90% from baseline (83.6 ng/mL) by week 16 (p=0.0001). Sustained suppression over multiple treatment cycles.
large↓Improves
A
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.
large↑Improves
A
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.
large↓Improves
A
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.
moderate↑Improves
B
Anti-Cancer Activity
13 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
moderate↑Improves
B
Hormone Levels
7 human trials support this finding. Human clinical trial data available.
small↑Improves
C
Reproductive Outcomes
6 preclinical studies support this finding. Primarily preclinical evidence.
small↑Improves
C
Safety/Tolerability
3 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
small↑Improves

Research Citations (31)

Periovulatory anticoagulant therapy enhances embryo recovery rates in superovulated mares.
(2025)
PMID: 39490086
Adverse event profile differences among long-acting gonadotropin-releasing hormone analogs: A real-world, pharmacovigilance study.
(2025)
PMID: 40644420
Review of drug-drug interactions in patients with prostate cancer.
(2024)
PMID: 38720547
Long-term experience with the use of a single histrelin implant beyond one year in patients with central precocious puberty
(2023)
PMID: 36625262
Fertility preservation in transfeminine adolescents using TESE at the time of Histrelin Acetate subcutaneous implant placement: A Case Series.
(2023)
PMID: 37770134
Case Report: Ovulation Induction in Greater One-Horned Rhinoceros (Rhinoceros unicornis).
(2021)
PMID: 34277752
Effects of GnRH agonists on testosterone and testosterone-stimulated parameters for contraception and aggression reduction in male lion-tailed Macaques (Macaca silenus).
(2021)
PMID: 34224162
Comparative Efficacy of Histrelin Acetate and hCG for Inducing Ovulation in Brazilian Northeastern Jennies (Equus africanus asinus).
(2020)
PMID: 32797776
Histrelin acetate-induced ovulation in Brazilian Northeastern jennies (Equus asinus) with different follicle diameters.
(2019)
PMID: 31254727
Association of Surgical Risk With Exogenous Hormone Use in Transgender Patients: A Systematic Review.
(2019)
PMID: 30516808

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