Quick summary
Histrelin (Supprelin LA/Vantas) is an FDA-approved GnRH agonist delivered via a subcutaneous hydrogel implant providing continuous hormone suppression for 12 months. It is indicated for central precocious puberty in children and advanced prostate cancer, offering a once-yearly dosing advantage.
Overview
Histrelin is a potent synthetic GnRH agonist nonapeptide delivered via a subcutaneous hydrogel implant providing continuous hormone release for 12 months. FDA-approved as Supprelin LA for central precocious puberty (CPP) in children and as Vantas for advanced prostate cancer, it offers a once-yearly dosing advantage over daily injections or frequent depot formulations. The implant is inserted subdermally in the inner upper arm under local anesthesia.
Mechanism of action
Histrelin is a highly potent GnRH receptor agonist. The subcutaneous implant continuously releases approximately 65 mcg histrelin acetate per day, producing non-pulsatile GnRH receptor stimulation. This continuous exposure causes pituitary GnRH receptor downregulation and gonadotroph desensitization, reversibly suppressing LH and FSH secretion. Within 1 month, LH and FSH levels decline to prepubertal levels in CPP patients, and testosterone falls to castrate levels (<50 ng/dL) in prostate cancer patients. The hydrogel polymer matrix controls diffusion for consistent plasma concentrations over 52 weeks, avoiding peak-trough variation seen with periodic depot injections.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| Central precocious puberty (children) | subcutaneous | 50–50 mg | one implant every 12 months | Implant delivers ~65 mcg/day. Insert subdermally in inner upper arm under local anesthesia. Remove and replace at 12 months. Monitor LH, FSH, and sex steroids at 1 month, then every 6 months. |
| Advanced prostate cancer — ADT | subcutaneous | 50–50 mg | one implant every 12 months | Same implant system as Supprelin LA but marketed as Vantas. Add antiandrogen for first 4 weeks to cover initial flare. |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
The pivotal Supprelin LA trial (n=36 CPP patients) demonstrated profound HPG-axis suppression within 1 month, with mean LH suppressed to prepubertal levels and maintained for 12 months. Height velocity and bone age advancement decelerated, with final adult height outcomes comparable to other GnRH agonists. For prostate cancer (Vantas), phase III data confirmed castrate testosterone (<50 ng/dL) in 92–97% of patients at month 12. Patient and caregiver preference studies show strong preference for annual implant over monthly injections, with significant improvements in quality of life and treatment adherence.[1][2][3][4]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with Histrelin for synergistic effects.
Legal status
FDA-approved as Supprelin LA (NDA 022058, 2007) for central precocious puberty in children and as Vantas (NDA 021732, 2004) for palliative treatment of advanced prostate cancer. Prescription-only; implant insertion and removal performed by trained clinicians.
Sourcing & access
Prescription required
Histrelin is an FDA-approved prescription medication available through licensed healthcare providers, telehealth platforms, and 503A/503B compounding pharmacies.
Frequently asked questions
Histrelin is an FDA-approved GnRH agonist delivered via a subcutaneous hydrogel implant providing 12 months of continuous drug release. It is approved under two brand names: Supprelin LA for central precocious puberty (CPP) in children and Vantas for palliative treatment of advanced prostate cancer. The implant format allows once-yearly treatment rather than monthly injections.
The histrelin implant releases approximately 65 micrograms per day at a continuous, non-pulsatile rate. This sustained non-pulsatile GnRH receptor stimulation desensitizes pituitary gonadotroph cells, suppressing LH and FSH secretion within one month. In children with CPP, this halts premature puberty. In prostate cancer, testosterone is suppressed to castrate levels, slowing androgen-dependent tumor growth.
The implant is placed subdermally in the inner upper arm under local anesthesia via a minor outpatient procedure. A small incision is made, the implant inserted, and the wound closed without sutures in most cases. It is replaced at 12 months. Studies in pediatric patients with CPP show strong preference over monthly injectable formulations due to reduced injection burden and consistent hormonal control.
Implant site reactions including pain, bruising, and scar formation are the most common local effects, with rare implant extrusion. Systemic effects reflect induced hypogonadism: hot flashes, sexual dysfunction, and bone mineral density loss with long-term use. An initial disease flare lasting 1 to 2 weeks may occur at treatment initiation due to transient LH surge before desensitization takes effect, which can worsen prostate cancer symptoms temporarily.
Research references
- Histrelin subcutaneous implant for central precocious puberty: pharmacokineticsPubMed
- GnRH agonist histrelin in advanced prostate cancer: long-term efficacyPubMed
- Histrelin acetate implant for testosterone suppression in prostate cancerPubMed
- Long-term testosterone suppression with histrelin implant in malesPubMed