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Delivered as a 12-month subcutaneous implant for continuous GnRH receptor activation.
Also known as: Supprelin LA · Vantas · GnRH agonist
Part of the Foundational & therapeutic peptides cluster
Overview
Histrelin is a synthetic GnRH agonist peptide administered as a subcutaneous implant that releases drug continuously over about a year. It is an approved prescription medicine for central precocious puberty in children and for hormone-sensitive prostate cancer in adults. This page is educational and is not medical advice.
Source & context
Biological / chemical source: Synthetic GnRH analog
Primary research or clinical context: Approved medicine for central precocious puberty and hormone-sensitive prostate cancer, delivered by subcutaneous implant (prescription)
Implant delivery
Rather than repeated injections, histrelin is placed in a small hydrogel implant under the skin of the upper arm. Continuous release maintains receptor desensitization, suppressing gonadotropins and sex hormones until the implant is removed or replaced.
Peptide design
Histrelin is a nonapeptide GnRH analog with a D-histidine substitution and an ethylamide C-terminus. These modifications increase potency and metabolic stability relative to native GnRH, supporting the long-duration implant format.
Sequence
One-letter sequence commonly cited for Histrelin (educational; isoforms and modifications may differ):
XHWSYHLRP
X = non-canonical residue (N-terminal residue is pyroglutamic acid; histadine residue is phenylmethyl-histidine). X marks a non-canonical residue — see the structure block below. (Plotted as alanine on the wheel.)
Residues plotted ~100° apart around an α-helix — clustering of one color reveals an amphipathic face.
Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
Reference values are taken from the cited molecular record or curated profile. A database match is not independent laboratory verification; modifications, counter-ions, and formulations can change the measured mass.
- Molecular form
- Histrelin (source record; form not independently established)
- Species
- Not established by this molecular identity audit
- Termini (N / C)
- Not specified / Not specified
Average reference mass
Reference policy updated: 2026-10-05
- IUPHAR/BPS source snapshot · 2026-10-01
- PubChem molecular record · 2026-10-01
- Molecular formula
- C66H86N18O12
- Average reference mass
- ≈ 1,323.5
- Status
- Approved medicine in at least one jurisdiction (IUPHAR record)
N-terminal residue is pyroglutamic acid; histadine residue is phenylmethyl-histidine
- PubChem CID: 25077993
- IUPHAR ligand: 3884
- ChEMBL: CHEMBL1201255
- CAS RN: 76712-82-8
- UNII: H50H3S3W74
Chemistry values: IUPHAR/BPS Guide to Pharmacology, PubChem · fetched 2026-10-01.
Clinical development snapshot
ClinicalTrials.gov lists 15 registered studies with “Histrelin” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT04513717 | Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low | Phase 3 | active not recruiting | 2026-08-17 |
| NCT05050084 | Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for | Phase 3 | active not recruiting | 2026-08-17 |
| NCT06378866 | Stereotactic Body Radiation Therapy Plus Immediate or Delayed Androgen Receptor Pathway Inhibitor and Androgen | Phase 2 | recruiting | 2026-07-20 |
| NCT04787744 | Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-direc | Phase 3 | recruiting | 2026-04-08 |
| NCT04203381 | Skeletal Health and Bone Marrow Composition Among Youth | Not applicable | terminated | 2026-04-03 |
| NCT03678025 | Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prosta | Phase 3 | recruiting | 2025-09-11 |
Histrelin — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Histrelin (source record; form not independently established)Average reference mass: 1,323.5 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
FAQ about Histrelin
What is Histrelin?+
Histrelin is a synthetic GnRH agonist peptide administered as a subcutaneous implant that releases drug continuously over about a year. It is an approved prescription medicine for central precocious puberty in children and for hormone-sensitive prostate cancer in adults. This page is educational and is not medical advice.
What Canadian product status is recorded for Histrelin?+
Canadian product status for Histrelin has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the typical length of Histrelin?+
Histrelin is commonly described as approximately 9 amino acids (GnRH agonist (nonapeptide analog)).
Related peptides
References & further reading
- 1.Deeks (2010). Histrelin: in advanced prostate cancer. Drugs
- 2.Mak et al. (2023). Trends in Histrelin Implantation at a Pediatric Tertiary Care Center. J Surg Res
- 3.Barradell et al. (1993). Histrelin. A review of its pharmacological properties and therapeutic role in central precocious puberty. Drugs
- 4.Silverman et al. (2021). Clinical characteristics and treatment patterns with histrelin acetate subcutaneous implants vs. leuprolide injections in children with precocious puberty: a real-world study using a US claims database. J Pediatr Endocrinol Metab
- 5.Olson-Kennedy et al. (2021). Histrelin Implants for Suppression of Puberty in Youth with Gender Dysphoria: A Comparison of 50 mcg/Day (Vantas) and 65 mcg/Day (SupprelinLA). Transgend Health
- 6.Krishna et al. (2021). Optimizing pediatric histrelin implantation to improve success rates in clinic without sedation. J Pediatr Endocrinol Metab
- 7.Klein et al. (2020). Treatment patterns, health resource utilization and costs among central precocious puberty patients treated with leuprolide or histrelin: an examination of the commercial and Medicaid populations. J Med Econ
- 8.Eugster et al. (2007). Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial. J Clin Endocrinol Metab
- 9.PubChem — compound summary for Histrelin (CID 25077993)
- 10.Wikipedia — Histrelin