Histrelin
Also known as: Supprelin LA, Vantas
A GnRH agonist delivered by a 12-month implant for central precocious puberty. FDA-approved as Supprelin LA; the Vantas prostate implant is discontinued.
Last updated
Mechanism of Action
Histrelin is a synthetic nonapeptide GnRH agonist that is substantially more potent than native GnRH. Continuous release from a hydrogel implant placed under the skin of the inner upper arm first stimulates, then desensitizes, pituitary GnRH receptors, suppressing LH and FSH and lowering sex steroids to prepubertal levels in children (or castrate levels in men). The implant releases drug at a nearly constant rate for about 12 months, and the effect reverses after it is removed.
- Half-life
- ~4 hours (drug released continuously from the implant)
- Administration Routes
- Subcutaneous implant
- Research Status
- Clinical
Reported Benefits
- Treatment of central precocious puberty in children aged 2 and older (Supprelin LA)
- Suppression of pubertal progression and slowing of bone age advancement
- Formerly used for palliative treatment of advanced prostate cancer (Vantas, discontinued)
Potential Side Effects
- Implant-site reactions: pain, bruising, swelling, infection
- Implant breakage or spontaneous extrusion
- Transient rise in sex hormones in the first weeks (e.g., vaginal bleeding)
- Psychiatric events such as mood changes (label warning)
- Seizures, reported with GnRH agonists in children (label warning)
Common Dosing
Supprelin LA is a single 50 mg implant inserted subdermally in the inner upper arm during a minor in-office surgical procedure under local anesthesia, and removed or replaced after 12 months. Response is monitored with hormone levels, growth and bone age. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Hypersensitivity to GnRH, GnRH agonists or any component
- Pregnancy
No documented stacking partners for Histrelin yet.
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Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial
2007
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An evaluation of the pharmacokinetics and pharmacodynamics of the histrelin implant for the palliative treatment of prostate cancer
2005
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Histrelin. A review of its pharmacological properties and therapeutic role in central precocious puberty
1993