--- title: "Histrelin" canonical_url: https://peptidelibrary.app/library/histrelin description: "GnRH receptor agonist delivered from a subcutaneous implant, approved for central precocious puberty in children and for palliative treatment of advanced prostate cancer." updated: 2026-11-07 publisher: Peptide Library notice: "Research and educational use only. Not medical advice." --- # 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. GnRH receptor agonist delivered from a subcutaneous implant, approved for central precocious puberty in children and for palliative treatment of advanced prostate cancer. ## Classification - Type: FDA-approved GnRH receptor agonist implant - Mechanism class: GnRH Modulator - Development stage: Approved product - Regulatory class: FDA-approved medicine ## Mechanism 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. ## Properties - Molecular formula: C66H86N18O12 - Molecular weight: 1,323.5 g/mol - CAS number: 76712-82-8 - Studied routes: Subcutaneous ## Evidence - Evidence level: FDA Approved - Highest documented: Regulatory review (FDA label) - Human trials: 2 - Controlled human trials: 1 - Preclinical sources: 0 - Latest source: 2015 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. ### Studies 1. SUPPRELIN LA (histrelin acetate) subcutaneous implant — FDA prescribing information (Endo), DailyMed. Regulatory label (FDA), human. Population: Children with central precocious puberty. Suppression of LH, FSH and sex steroids [Source](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d8fb000e-3cc9-4803-b71d-2cc597661977) 2. 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. 2015. Controlled human trial. Population: Children with central precocious puberty (n=36; 20 treatment-naive, 16 previously treated). Hormonal suppression maintained; predicted adult height in girls rose from 151.9 cm to 166.5 cm at month 60 (n=6) [Source](https://pubmed.ncbi.nlm.nih.gov/25803268/) 3. 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. 2012. Human study (early or uncontrolled). Population: Men with advanced prostate cancer who had responded to 52 weeks of the histrelin implant (n=104). Serum testosterone stayed below 50 ng/dL in all patients; hot flashes in 64.4% [Source](https://pubmed.ncbi.nlm.nih.gov/21851539/) ## Safety Human safety basis: FDA prescribing information ## Regulatory 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 - Availability: Prescription-Only ## 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, 2015](https://pubmed.ncbi.nlm.nih.gov/25803268/) - [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, 2025](https://pubmed.ncbi.nlm.nih.gov/39343637/) - [Association of Surgical Risk With Exogenous Hormone Use in Transgender Patients: A Systematic Review — JAMA Surg, 2019](https://pubmed.ncbi.nlm.nih.gov/30516808/) - [Experience with the Histrelin Implant in Pediatric Patients — Endocr Dev, 2016](https://pubmed.ncbi.nlm.nih.gov/26683629/) - [The histrelin implant: a novel treatment for central precocious puberty — Pediatrics, 2005](https://pubmed.ncbi.nlm.nih.gov/16322137/)