Sexual & reproductive GnRH agonist
Histrelin
Regulatory status
Status at a glance
503A compounding status
Not nominated
We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.
- FDA approval
- An FDA-approved product contains this peptide
- 503B outsourcing
- Not determined
- Anti-doping (WADA)
- Not on the WADA Prohibited List
- DEA schedule
- Not a controlled substance
About peptide status
Most peptides discussed here are not FDA-approved for any use, and products labeled “research use only” are not for human use. Removal from Category 2 does not authorize compounding. PCAC votes are non-binding recommendations; FDA and HHS make the final decisions.
This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information. Talk with a licensed clinician before using any peptide.
If you think you are having a medical emergency, call 911.
Key takeaway
Histrelin (histrelin acetate, sold as Supprelin LA and formerly as Vantas) is a synthetic nonapeptide agonist of gonadotropin-releasing hormone delivered as a small implant that releases drug for about a year. It suppresses the pituitary and the sex hormones it controls, and is used for central precocious puberty in children; a second implant for advanced prostate cancer in adults was discontinued in 2021. The implant products have been FDA-approved in the U.S. since the mid-2000s, and one implant lasts roughly 12 months.
At a glance
- What it is
- A GnRH (LHRH) receptor agonist peptide delivered as a 12-month subdermal implant
- Approved for
- Central precocious puberty (Supprelin LA); the advanced prostate cancer implant (Vantas) was discontinued in 2021
- Key fact
- A single 50 mg implant drove stimulated luteinizing hormone down and held it suppressed for a year in children with precocious puberty
- Route
- Subdermal implant placed in the inner upper arm
- Evidence strength
- FDA approved
Summary
Histrelin is an FDA-approved GnRH agonist implant for central precocious puberty. Learn how it works, its side effects, and the evidence behind it.
What is histrelin?
Histrelin, known generically as histrelin acetate and sold under the brand Supprelin LA and formerly as Vantas, is a synthetic nine-amino-acid analog of gonadotropin-releasing hormone (GnRH, also called LHRH). It is one of the more potent GnRH agonists and is delivered from a flexible implant that sits under the skin and releases drug steadily for about 12 months, so a child or patient needs only one placement per year rather than repeated injections. Earlier forms of histrelin were given as daily injections; the modern products are implants.
How does histrelin work?
Histrelin binds the GnRH receptor on the pituitary. As with other agonists in its class, an initial dose briefly stimulates the gland, producing a short rise in luteinizing hormone and sex steroids, the flare. Because the implant then delivers the drug continuously, the receptors downregulate and desensitize, and gonadotropin output falls. Sex-hormone levels drop to prepubertal levels in children or castrate levels in men.
In central precocious puberty, that suppression stops the premature pubertal cascade, pausing bone maturation and breast or testicular development until a more appropriate age; in advanced prostate cancer, it removes the testosterone that hormone-sensitive tumors rely on. In the pivotal pediatric study, a single subdermal implant lowered peak stimulated luteinizing hormone from about 28 to under 1 mIU/mL and maintained suppression of luteinizing hormone and sex steroids for a full year.
Is it FDA-approved?
Editor’s note
Status: Yes. Histrelin's U.S. approval and market history: Year | Event Early 1990s | An earlier daily-injection form of histrelin was approved 2004 | Vantas implant approved for advanced prostate cancer 2007 | Supprelin LA implant approved for central precocious puberty 2021 | Vantas discontinued by its manufacturer Supprelin LA is now the only histrelin implant sold in the U.S. Each implant is designed to deliver drug for about 12 months and is then removed and replaced.
Category: FDA-approved · Primary body area: Sexual & reproductive
Yes. Histrelin's U.S. approval and market history:
| Year | Event |
|---|---|
| Early 1990s | An earlier daily-injection form of histrelin was approved |
| 2004 | Vantas implant approved for advanced prostate cancer |
| 2007 | Supprelin LA implant approved for central precocious puberty |
| 2021 | Vantas discontinued by its manufacturer |
Supprelin LA is now the only histrelin implant sold in the U.S. Each implant is designed to deliver drug for about 12 months and is then removed and replaced.
What is histrelin prescribed for?
Histrelin is prescribed for central precocious puberty in children (Supprelin LA). It was also used as palliative treatment of advanced prostate cancer in adults (Vantas) until that implant was discontinued. The implant is placed and removed in a brief in-office procedure.
What are the side effects?
According to the Supprelin LA label, the most common side effect is a reaction at the implant site, reported in about half of children in clinical trials:
- Pain, bruising, soreness, or swelling where the implant is placed
More serious considerations include:
- Implant breakage or difficult removal
- A brief rise in sex hormones in the first week, which can temporarily worsen symptoms
- Mood and behavior changes such as irritability, crying, anger, or aggression
- Convulsions
- Raised pressure around the brain (pseudotumor cerebri), with symptoms such as headache and vision changes
- Severe skin reactions
Sources: FDA prescribing information for Supprelin LA; KFF Health News reporting on the discontinuation of Vantas; the pediatric implant trial (Eugster et al., Journal of Clinical Endocrinology and Metabolism, 2007, DOI: 10.1210/jc.2006-2479), indexed on PubMed. This document is educational and does not constitute medical advice.
Registered human trials
0 registered human trials on ClinicalTrials.gov that we reviewed
Sources
- [1]
- [2]
- [3]
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