Source: FDA label
| Molecular formula | C66H86N18O12 |
|---|---|
| Molecular weight | 1323.5 g/mol |
| Registered trials | 16 |
| PubChem CID | 25077993 |
| Brand names | SUPPRELIN LA |
Mechanism of Action
12.1 Mechanism of Action SUPPRELIN LA is a GnRH agonist and an inhibitor of gonadotropin secretion when given continuously. It delivers approximately 65 mcg histrelin acetate per day. Both animal and human studies indicate that following an initial stimulatory phase, chronic, subcutaneous administration of histrelin acetate desensitizes responsiveness of the pituitary gonadotropin which, in turn causes a reduction in ovarian and testicular steroidogenesis. In humans, administration of histrelin
Intro
Parents exploring treatment for a child diagnosed with early puberty often want to understand how the medication works before committing to it. Histrelin is a long-acting hormone therapy delivered through a small implant placed under the skin.
Key takeaways
- Histrelin acetate is marketed as SUPPRELIN LA, a subcutaneous implant for central precocious puberty (CPP).
- It is a GnRH agonist that gradually reduces the body's own sex hormone production.
- Diagnosis of CPP requires hormone testing and a bone age assessment before treatment starts.
- At least 16 trials have studied histrelin, including a completed phase 3 study in children with CPP.
- Reported side effects lean heavily toward device and administration issues rather than systemic reactions.
What histrelin is
Histrelin is a synthetic hormone analog belonging to the GnRH agonist class. Given continuously, it first stimulates and then suppresses the pituitary gland's release of gonadotropins. That suppression lowers ovarian and testicular hormone production over time. The compound is identified in chemical databases under PubChem CID 25077993.
What histrelin is approved for
SUPPRELIN LA is approved for children with central precocious puberty, whether the cause is neurogenic or idiopathic. This condition involves early signs of puberty, before age 8 in girls and age 9 in boys, along with bone age that outpaces chronological age. Diagnosis requires blood hormone testing after GnRH analog stimulation and a bone age evaluation. The label does not carry a boxed warning.
What the evidence shows
Histrelin has been studied across 16 registered trials. A completed phase 3 trial evaluated the subcutaneous implant specifically in children with central precocious puberty. Separate research, including an active phase 3 study, has examined histrelin implants in prostate cancer settings, though that use falls outside the CPP-specific label discussed here.
Reported side effects
The most frequently reported issues center on the implant and its administration rather than the drug's hormonal action: drug ineffective (138 reports), device breakage (117), procedural complications (83), and incorrect drug or product administration duration (65 and 60). Skin reactions also appear, including rash (46) and implant site rash (41), along with headache (39). These figures reflect submitted reports, not confirmed rates or proof of a causal link.
FAQ
What is histrelin used for?
Histrelin, sold as SUPPRELIN LA, is an implant approved to treat central precocious puberty in children. It is used when a child shows early signs of puberty along with bone age that is advancing faster than expected. Diagnosis is confirmed with hormone testing before treatment begins.
How does histrelin work in the body?
Histrelin is a GnRH agonist that, when delivered continuously, first stimulates and then desensitizes the pituitary gland's hormone signaling. This process reduces the ovaries' or testes' production of sex hormones over time. The effect builds gradually rather than acting immediately.
Does histrelin carry a boxed warning?
No. According to the label data reviewed, SUPPRELIN LA does not carry a boxed warning.
What are the most commonly reported side effects of histrelin?
Reported cases most often involve device breakage, procedural complications, and issues with administration duration rather than typical drug side effects. Rash, including rash at the implant site, and headache are also reported. These counts come from adverse event reports and do not establish incidence or cause.
Has histrelin been studied in clinical trials?
Yes. Histrelin has been evaluated in at least 16 registered trials, including a completed phase 3 study in children with central precocious puberty. Other trials have examined histrelin implants in different medical contexts, such as prostate cancer research.
This page is an editorial information resource. It does not sell, prescribe, or recommend any medication.
Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: DailyMed label (SUPPRELIN LA) ClinicalTrials.gov FAERS PubChem
Updated 2026-08-04