Histrelin
Also known as: Histrelin acetate, Supprelin LA, Vantas
Histrelin acetate is a potent GnRH agonist delivered by a roughly year-long implant. Supprelin LA treats central precocious puberty; the former Vantas prostate-cancer implant has been discontinued.
Quick Facts
A sustained-release GnRH agonist
Histrelin is a synthetic nine-amino-acid analog of GnRH, also called LHRH. Modern products use a flexible subdermal implant that releases drug steadily for about 12 months, rather than the earlier daily injections. Placement and removal take place in a brief office procedure. Supprelin LA is the current US implant; Vantas was an adult prostate-cancer product.
An initial flare followed by suppression
Activation of pituitary GnRH receptors initially produces a short rise in LH and sex steroids. Continuous exposure then downregulates/desensitizes the receptors, suppressing gonadotropins and bringing sex hormones to prepubertal levels in children or castrate levels in men. In central precocious puberty, this interrupts early pubertal progression and bone maturation. In hormone-sensitive advanced prostate cancer, testosterone reduction removes a tumor-growth signal.
The pivotal pediatric study found stimulated peak LH fell from about 28 to under 1 mIU/mL after a single implant, with LH and sex-steroid suppression sustained for a year.
Supporting references: maintained.
Sources: [1]
Approval and market history
| Period | Event |
|---|---|
| Early 1990s | Approval of an earlier daily-injection form |
| 2004 | Vantas implant approved for advanced prostate cancer |
| 2007 | Supprelin LA implant approved for central precocious puberty |
| 2021 | Manufacturer discontinued Vantas |
Supporting references: approved; discontinued.
Current and former uses
Supprelin LA treats central precocious puberty in children. It is designed for removal and replacement after about 12 months. Vantas was used palliatively for advanced prostate cancer before its discontinuation and should not be described as a currently marketed US implant.
Implant and hormonal adverse effects
About half of children in Supprelin LA trials reported implantation-site reactions such as pain, bruising, soreness or swelling. Implant fracture or difficult removal can occur. The first-week hormone flare may briefly worsen symptoms. Mood/behavior changes include irritability, crying, anger and aggression. Other serious concerns include convulsions, pseudotumor cerebri with headache or visual changes, and severe skin reactions.
References and further reading
This reference draws on Superpower’s Peptide Library and the research linked below. Peptide Dossier’s editorial team adapted and integrated the material on .
- 10.1210/jc.2006-2479An initial flare followed by suppressionCited in: An initial flare followed by suppression
- endodocuments.comApproval and market historyCited in: Approval and market history
- mdedge.comApproval and market historyCited in: Approval and market history
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Disclaimer: This article is for informational and educational purposes only. It is not intended as medical advice. The information presented is based on published research and should not be used as a substitute for professional medical guidance. Always consult a qualified healthcare provider before starting any peptide protocol. Some peptides discussed may not be approved for human use by the FDA or equivalent regulatory bodies.