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.
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.
Where to get it
Prescription required
Histrelin is a prescription medication. Consult your healthcare provider or a licensed telehealth platform for access.