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
Key takeaways
- Histrelin is a GnRH agonist delivered through a subcutaneous implant, marketed as Supprelin LA.
- It is approved to treat central precocious puberty (CPP) in children.
- Chronic use desensitizes the pituitary gland, reducing ovarian and testicular steroidogenesis.
- Supprelin LA does not carry a boxed warning.
- Reported issues to the FDA include device breakage, procedural complications, and injection site rash, reported as counts rather than confirmed causes.
What Histrelin Is
Histrelin is a GnRH agonist, a type of hormone therapy that works by altering signals between the brain and the gonads. Delivered continuously from a subcutaneous implant, it first stimulates then suppresses the pituitary gland's release of gonadotropins. This suppression lowers steroid hormone production from the ovaries or testes. The implant delivers approximately 65 mcg of histrelin acetate per day.
What Histrelin Is Approved For
Histrelin, sold as Supprelin LA, is approved to treat central precocious puberty in children. CPP causes early onset of secondary sexual characteristics, before age 8 in females and age 9 in males, along with accelerated bone age that can reduce adult height. Diagnosis typically requires blood testing for sex steroids, LH, and FSH after GnRH analog stimulation, along with bone age assessment. Supprelin LA's label does not carry a boxed warning.
What the Evidence Shows
Histrelin has been studied across 16 registered clinical trials. A completed Phase 3 trial evaluated the histrelin subcutaneous implant specifically in children with central precocious puberty. A separate completed Phase 3 trial examined a histrelin subdermal implant in patients with prostate cancer, reflecting the compound's broader hormone-suppressing mechanism. A trial on markers of pubertal suppression during CPP therapy was terminated.
Reported Side Effects
FDA Adverse Event Reporting System data for histrelin reflects reports, not confirmed incidence or causation. The most frequently reported issues relate to treatment and device performance: drug ineffectiveness (138 reports), device breakage (117), and procedural complications (83). Administration-related reports, including incorrect drug or product administration duration, were also common (65 and 60 reports, respectively). Skin reactions were reported as well, including rash (46) and implant site rash (41), along with headache (39).
FAQ
What is histrelin used for?
Histrelin, sold as Supprelin LA, is approved to treat central precocious puberty in children. It works by suppressing the pituitary gland's hormone signals after an initial stimulatory phase. This helps slow the early onset of secondary sexual characteristics and associated bone age advancement.
How does histrelin work in the body?
Histrelin is a GnRH agonist delivered continuously through a subcutaneous implant. With chronic exposure, it desensitizes pituitary gonadotropin responsiveness, which reduces ovarian and testicular steroid hormone production. The implant releases approximately 65 mcg of histrelin acetate per day.
Does histrelin have a boxed warning?
No, the Supprelin LA label for histrelin does not carry a boxed warning according to the available labeling data.
What are the most commonly reported side effects of histrelin?
FDA adverse event reports for histrelin most often mention drug ineffectiveness, device breakage, and procedural complications related to the implant. Administration duration errors and skin reactions, including rash at the implant site, were also frequently reported. These are reported counts, not confirmed rates or proof of causation.
What clinical evidence supports histrelin's use?
Histrelin has been evaluated in 16 registered clinical trials. A completed Phase 3 trial studied the histrelin subcutaneous implant specifically in children with central precocious puberty. Another completed Phase 3 trial examined a histrelin implant in patients with prostate cancer, reflecting its hormone-suppressing mechanism.
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Sources: FDA label (Supprelin LA) ClinicalTrials.gov FDA FAERS PubChem
Updated 2026-11-07