Overview
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In plain language
Histrelin is a GnRH agonist delivered in a remarkable way: a tiny implant placed under the skin of the upper arm that releases medicine continuously for a full year. It is sold as Supprelin LA for children with central precocious puberty.
The year-long implant means a child gets continuous treatment without daily pills or monthly injections, and the implant is removed and replaced after 12 months. A version for prostate cancer (Vantas) was discontinued in 2021, but the puberty implant remains available through specialty pharmacies.
For students
Histrelin is [D-His(Bzl)6, Pro9-NHEt]GnRH (about 1,323 Da), among the most potent GnRH agonists per milligram. The Supprelin LA implant is a 50 mg hydrogel cylinder that releases roughly 65 mcg/day for a year, providing continuous downregulation of the reproductive axis.
The implant's continuous, zero-order release makes histrelin pharmacologically distinctive: rather than depot peaks and troughs, it delivers a flat signal that maintains desensitization without breaks, an advantage for compliance in a pediatric population. Vantas, the prostate cancer implant, was discontinued by Endo in 2021 after manufacturing problems, and generic leuprolide and triptorelin depots now cover most of that indication.
For researchers and instructors
Biochemistry. The D-His(Bzl)6 substitution combined with an ethylamide at position 9-10 increases potency several-fold over native GnRH; the hydrogel implant cross-links to release drug by diffusion-controlled zero-order kinetics.
Pharmacology. Year-long duration is unmatched among GnRH products; LH and sex steroid suppression is continuous rather than pulsatile, with no injection or daily dosing burden; removal is an office procedure.
Human evidence. Open-label studies in central precocious puberty showed sustained suppression of LH response to stimulation and appropriate pubertal pause; the Vantas prostate program had equivalent testosterone suppression to other agonists.
Teaching point. Teaches how formulation innovation (a year-long implant) can differentiate a molecule whose receptor pharmacology is commodity.
Molecular identity
- Amino acids
- 9 (nonapeptide)
- Molecular weight
- ~1,323 Da
- Formula
- C₆₆H₈₆N₁₈O₁₂
- Sequence
- GnRH with D-His(Bzl)6 and Pro-NHEt at 9-10
Origin and history
Histrelin is a potent GnRH agonist. Its modern form is remarkable: a 50 mg hydrogel implant placed under the skin of the upper arm that releases drug for a full year, approved for central precocious puberty in children (Supprelin LA, 2007).
An identical implant for prostate cancer (Vantas, 2004) was discontinued by Endo in 2021 after manufacturing problems; the puberty implant remains available through specialty pharmacies.
Key people
- Endo PharmaceuticalsDeveloped the year-long implant
Timeline
- 1991
Daily-injection form approved
- 2004
Vantas implant approved
- 2007
Supprelin LA approved
- 2021
Vantas discontinued
See every peptide on one history timeline.
Human evidence
Open-label studies showed year-long suppression of puberty hormones with the implant; the prostate program included Phase 3 evidence.
Registration and enrollment are not proof of benefit; check study results directly.
Explore original publications and distinguish preclinical findings from controlled human evidence.
Safety and regulatory status
See every compound on the regulatory tracker.
FDA-approved (Supprelin LA). The prostate-cancer implant (Vantas) was discontinued in 2021.
This profile is educational and does not provide treatment, dosing or sourcing guidance.
Sources
- PubMed literature search: Histrelin
- PubChem compound search: Histrelin
- DailyMed (FDA label search): Histrelin
- UniProt search: Histrelin
- ClinicalTrials.gov search: Histrelin
Hernandez Gener, E. (November 8, 2026). Histrelin: molecular data, research history and evidence. VALREXA Biosciences. https://valrexa.com/peptides/histrelin.html
APA style · Last reviewed November 8, 2026 · Our editorial standardsLast reviewed November 8, 2026. Trial and regulatory status can change; confirm in the linked registries. This profile is educational and is not medical advice, a treatment recommendation, or dosing or sourcing guidance. Report an error · Corrections policy