Histrelin
Histrelin is an FDA-approved GnRH receptor agonist implant. Histrelin is a nonapeptide GnRH agonist released continuously from a hydrogel implant over about twelve months. Sustained, non-pulsatile receptor occupancy desensitises pituitary gonadotrophs, suppressing luteinising and follicle-stimulating hormone and consequently gonadal steroid production, after a transient initial stimulation.
For research use only.
Key Facts
- CAS
- 76712-82-8
- Molecular Weight (MW)
- 1323.5 g/mol
- Half-life
- —
- FDA status
- Approved
- Administration Route
- subcutaneous
- Frequency
- —
- Last updated
- Aug 30, 2026
- Reviewed
- Aug 30, 2026
Research summary
GnRH receptor agonist delivered from a subcutaneous implant, approved for central precocious puberty in children and for palliative treatment of advanced prostate cancer.
Peptide Library's Histrelin profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Protocol
- Dosage Range
- —
- Frequency
- —
- Cycle
- —
- Administration Route
- subcutaneous
- Reconstitution Guide
- —
Not yet checked against primary sources
These figures are compiled from earlier reference material. They have not been verified against FDA labelling, registered trials or published literature, no citation is attached to them, and none of them is a recommended dose. Histrelin is queued for dosage evidence review.
Compare reported doses across the whole librarySequence & molecular data
| Molecular formula | C66H86N18O12 |
|---|---|
| Molecular weight | 1323.5 g/mol |
| CAS number | 76712-82-8 |
| PubChem CID | 25077993 |
| FDA UNII | H50H3S3W74 |
| ChEMBL | CHEMBL1201255 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Histrelin is a nonapeptide GnRH agonist released continuously from a hydrogel implant over about twelve months. Sustained, non-pulsatile receptor occupancy desensitises pituitary gonadotrophs, suppressing luteinising and follicle-stimulating hormone and consequently gonadal steroid production, after a transient initial stimulation.
Studies
- Long-Term Continuous Suppression With Once-Yearly Histrelin Subcutaneous Implants for the Treatment of Central Precocious Puberty: A Final Report of a Phase 3 Multicenter Trial
- Comparative Cardiovascular Safety of Gonadotropin-releasing Hormone Antagonists and Agonists Among Patients Diagnosed with Prostate Cancer: A Systematic Review and Meta-analysis of Real-world Evidence Studies
- Association of Surgical Risk With Exogenous Hormone Use in Transgender Patients: A Systematic Review
- Experience with the Histrelin Implant in Pediatric Patients
- The histrelin implant: a novel treatment for central precocious puberty
Regulatory & research status
Histrelin is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Research status | Approved product (see FDA status) |
| Availability | Prescription-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | FDA-Approved |
Benefits
—
Potential Side Effects
No side effects listed yet for this entry.
Storage & stability
Lyophilized (freeze-dried) peptide powder is far more stable than the reconstituted solution. Keep sealed vials cold, dry and away from light; long-term storage is typically frozen, with short-term refrigeration for vials in use.
Once reconstituted in bacteriostatic water, keep the solution refrigerated, avoid repeated freeze–thaw cycles and agitation, and label the vial with the reconstitution date and concentration. Discard any solution that turns cloudy or shows particulates.
Degradation rates differ by sequence: peptides containing methionine, cysteine, asparagine or glutamine are more prone to oxidation and deamidation, so shelf life after reconstitution is compound-specific rather than universal.
Read the full guide: how to store peptides before and after reconstitution →
Source: Manning MC, Chou DK, Murphy BM, Payne RW, Katayama DS. Stability of protein pharmaceuticals: an update. Pharm Res. 2010;27(4):544–575. (PMID 20143256). General guidance for research handling; not product-specific instructions.
Histrelin: frequently asked questions
What is Histrelin?
GnRH receptor agonist delivered from a subcutaneous implant, approved for central precocious puberty in children and for palliative treatment of advanced prostate cancer.
How does Histrelin work?
Histrelin is a nonapeptide GnRH agonist released continuously from a hydrogel implant over about twelve months. Sustained, non-pulsatile receptor occupancy desensitises pituitary gonadotrophs, suppressing luteinising and follicle-stimulating hormone and consequently gonadal steroid production, after a transient initial stimulation.
Is Histrelin FDA approved?
Yes. Histrelin is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
What peptides are similar to Histrelin?
Compounds most often compared with Histrelin include Leuprolide, Goserelin, Triptorelin and Nafarelin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Long-Term Continuous Suppression With Once-Yearly Histrelin Subcutaneous Implants for the Treatment of Central Precocious Puberty: A Final Report of a Phase 3 Multicenter Trial — J Clin Endocrinol Metab, 2015External reference
- Comparative Cardiovascular Safety of Gonadotropin-releasing Hormone Antagonists and Agonists Among Patients Diagnosed with Prostate Cancer: A Systematic Review and Meta-analysis of Real-world Evidence Studies — Eur Urol Oncol, 2025External reference
- Association of Surgical Risk With Exogenous Hormone Use in Transgender Patients: A Systematic Review — JAMA Surg, 2019External reference
- Experience with the Histrelin Implant in Pediatric Patients — Endocr Dev, 2016External reference
- The histrelin implant: a novel treatment for central precocious puberty — Pediatrics, 2005External reference
Related research, comparisons & guides
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Aug 30, 2026 · Version 1
This Histrelin profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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