Peptide LibraryHistrelin
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
- Evidence level
- FDA Approved
- Human dose established
- Yes
- Administration Route
- Subcutaneous implant
- Frequency
- One implant every 12 months
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 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.
Research evidence
- Regulatory review (FDA label)1 reviewed source
- Controlled human trials1 reviewed source
- Early or uncontrolled human studies1 reviewed source
- Lab & animal studiesNone in reviewed sources
How it works
Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess.
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.
Histrelin dosage evidence
Histrelin has an FDA-approved human dosage for children with central precocious puberty. SUPPRELIN LA is one 50 mg histrelin acetate implant placed under the skin of the inner upper arm every 12 months; it releases about 65 mcg a day. VANTAS, a once-yearly histrelin implant used in advanced prostate cancer, has no current listing on DailyMed, so prostate-cancer use is covered here only by trial reports.
| Human dosing established | Yes |
|---|---|
| Studied dose range | One 50 mg implant every 12 months (SUPPRELIN LA, central precocious puberty) |
| Route | Subcutaneous implant |
| Frequency | One implant every 12 months |
| Duration studied | Continued until the appropriate age for puberty; a new implant may be placed when the old one is removed |
| Evidence level | FDA Approved |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| FDA label — SUPPRELIN LA, central precocious pubertyFDA-approved label · FDA prescribing information | Children with central precocious puberty | One implant containing 50 mg histrelin acetate, releasing about 65 mcg a day | Subcutaneous implant in the inner upper arm | Every 12 months | Removed after 12 months; another implant may be inserted to continue. Stopping is considered at about 11 years for girls and 12 years for boys | Suppression of LH, FSH and sex steroids | SUPPRELIN LA (histrelin acetate) subcutaneous implant — FDA prescribing information (Endo), DailyMed |
| Phase 3 long-term extension (Silverman et al., 2015)Clinical trial · Phase 3 open-label study | Children with central precocious puberty (n=36; 20 treatment-naive, 16 previously treated) | One 12-month histrelin implant, replaced by a new implant at removal | Subcutaneous implant | Yearly | Up to 6 years of treatment and up to 1 year of follow-up | Hormonal suppression maintained; predicted adult height in girls rose from 151.9 cm to 166.5 cm at month 60 (n=6) | Silverman LA et al. 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. 2015. |
| Prostate cancer — open-label extension of a pivotal study (Shore et al., 2012)Clinical trial · Open-label extension study | Men with advanced prostate cancer who had responded to 52 weeks of the histrelin implant (n=104) | One histrelin implant placed each year; the strength is not stated in the indexed abstract | Subcutaneous implant | Yearly | Over 70% received three consecutive implants; the longest single treatment period was over 4 years | Serum testosterone stayed below 50 ng/dL in all patients; hot flashes in 64.4% | Shore N, Cookson MS, Gittelman MC. Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU Int. 2012. |
Where sources disagree
- The implant is not a dose that can be divided or repeated more often. It releases histrelin continuously for 12 months, and the label sets a single regimen: one implant a year.
- The SUPPRELIN LA label warns of an initial rise in gonadotropins and sex steroids in the first weeks, implant breakage, psychiatric events, convulsions, severe skin reactions and pseudotumor cerebri. It calls for LH, FSH and estradiol or testosterone checks 1 month after insertion and every 6 months after that.
- VANTAS, the once-yearly histrelin implant for advanced prostate cancer named in Djavan et al. (Can J Urol, 2010), has no DailyMed listing today. The prostate-cancer row above comes from a trial report, not a current US label.
Sequence & 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
Research statistics
124 PubMed publications · 58.2% human clinical research · 8 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
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 |
How FDA approval, compounding and research-only status differ
Benefits
—
Histrelin side effects
No side effects listed yet for this entry.
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
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 Nov 7, 2026 · Version 2
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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