Peptide LibraryTriptorelin
Also known as: Trelstar, Decapeptyl, GnRH agonist
Triptorelin (also called Trelstar or Decapeptyl) is an FDA-approved depot GnRH agonist. Triptorelin is a GnRH agonist decapeptide with a D-tryptophan substitution at position six that increases receptor affinity and resists enzymatic degradation.
For research use only.
Key Facts
- CAS
- 57773-63-4
- Molecular Weight (MW)
- 1311.4 g/mol
- Half-life
- Depot: weeks to months
- FDA status
- Approved
- Evidence level
- FDA Approved
- Human dose established
- Yes
- Administration Route
- Intramuscular
- Frequency
- Every 4, 12 or 24 weeks by strength
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
- Targets
- GnRH receptor
Research summary
FDA-approved depot GnRH agonist (Trelstar) for advanced prostate cancer. Causes flare then downregulation of LH/testosterone. WADA S2.
Research evidence
- Regulatory review (FDA label)2 reviewed sources
- Controlled human trials1 reviewed source
- Early or uncontrolled human studiesNone in reviewed sources
- 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 Triptorelin 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.
Triptorelin dosage evidence
Triptorelin has FDA-approved human dosages given as an intramuscular injection. For advanced prostate cancer, TRELSTAR is 3.75 mg every 4 weeks, 11.25 mg every 12 weeks or 22.5 mg every 24 weeks. For central precocious puberty in children aged 2 and over, TRIPTODUR is 22.5 mg every 24 weeks.
| Human dosing established | Yes |
|---|---|
| Route | Intramuscular |
| Frequency | Every 4, 12 or 24 weeks by strength |
| Duration studied | Long-term for prostate cancer; until the age of puberty for central precocious puberty |
| 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 — TRELSTAR, advanced prostate cancerFDA-approved label · FDA prescribing information | Men with advanced prostate cancer | 3.75 mg every 4 weeks, 11.25 mg every 12 weeks or 22.5 mg every 24 weeks | Intramuscular, either buttock | Every 4, 12 or 24 weeks by strength | Long-term | Treatment of advanced prostate cancer | TRELSTAR (triptorelin pamoate for injectable suspension) — FDA prescribing information (Verity), DailyMed |
| FDA label — TRIPTODUR, central precocious pubertyFDA-approved label · FDA prescribing information | Children aged 2 and over with central precocious puberty | 22.5 mg | Intramuscular | Once every 24 weeks | Stopped at the appropriate age for the onset of puberty | Suppression of LH and sex steroids | TRIPTODUR (triptorelin) for extended-release injectable suspension — FDA prescribing information (Azurity), DailyMed |
| Phase 3 trial of the 6-month formulation in Chinese children (Yu et al., 2024)Clinical trial · Phase 3 open-label single-arm trial (NCT05029622) | Chinese children with central precocious puberty (girls under 9, boys under 10; 66 completed) | Triptorelin pamoate 22.5 mg on day 1 and at month 6 | Not stated in the indexed abstract | Every 6 months | 12 months | All patients had LH suppression (stimulated peak LH 5 IU/L or less) at month 6; 98.5% at month 12 | Yu X et al. A Phase 3, Open-Label, Single-Arm Trial of the Efficacy and Safety of Triptorelin 6-Month Formulation in Chinese Children with Central Precocious Puberty. Adv Ther. 2024. |
Where sources disagree
- The TRELSTAR strengths have different release characteristics: the label says they are not additive and must be chosen by the dosing schedule wanted.
- The TRELSTAR label warns of hypersensitivity reactions including anaphylactic shock, tumor flare in the first weeks, and metabolic changes such as hyperglycemia and diabetes. The TRIPTODUR label also warns of pseudotumor cerebri.
- OvuGel, also listed on DailyMed under triptorelin, is a veterinary gel for sows. It is not a human product and contributes no dosing here.
Handling & administration
- Injection Sites
- Gluteal
- Timing Notes
- Educational catalog only — not medical advice
Sequence & molecular data
| Molecular formula | C64H82N18O13 |
|---|---|
| Molecular weight | 1311.4 g/mol |
| CAS number | 57773-63-4 |
| Half-life | Depot: weeks to months |
| Appearance | Lyophilized powder for depot injection |
| Formulation | Lyophilized Powder |
| PubChem CID | 25074470 |
| FDA UNII | 9081Y98W2V |
| ChEMBL | CHEMBL1201334 |
| DrugBank | DB06825 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Triptorelin is a GnRH agonist decapeptide with a D-tryptophan substitution at position six that increases receptor affinity and resists enzymatic degradation. Given as a depot it provides continuous rather than pulsatile receptor occupancy, which first stimulates and then desensitises pituitary gonadotrophs: luteinising and follicle-stimulating hormone rise transiently, then fall as the receptor is downregulated, and gonadal steroid production declines to castrate concentrations over roughly two to four weeks. The same initial flare seen with other GnRH agonists occurs, and formulations are available giving one, three or six months of suppression.
Origin
Synthetic decapeptide GnRH analog.
Targets
Studies
- A Phase 3, Open-Label, Single-Arm Trial of the Efficacy and Safety of Triptorelin 6-Month Formulation in Chinese Children with Central Precocious Puberty
- Adolescent Gender Dysphoria in Italy: Reflections on Triptorelin, Consent, and Care
- Triptorelin: The Need for Legal Protection Aimed at the Full Political and Social Integration of Gender Variant youth. A Comparison of Different Global realities
- GnRH agonist treatment before total laparoscopic hysterectomy for large uteri
- Spotlight on triptorelin in the treatment of premenopausal women with early-stage breast cancer
Research statistics
1,670 PubMed publications · 69.6% human clinical research · 200 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
Triptorelin 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 |
| WADA (sport) | Banned in Sport |
| Library classification | FDA-Approved |
How FDA approval, compounding and research-only status differ
Benefits
Triptorelin side effects
The effects below are drawn from Triptorelin's prescribing information, which lists the full adverse-reaction data.
Side Effects
- Hot flashes
- Bone loss
- Tumor flare
- Injection-site reactions
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.
Triptorelin: frequently asked questions
What is Triptorelin?
FDA-approved depot GnRH agonist (Trelstar) for advanced prostate cancer. Causes flare then downregulation of LH/testosterone. WADA S2.
How does Triptorelin work?
Triptorelin is a GnRH agonist decapeptide with a D-tryptophan substitution at position six that increases receptor affinity and resists enzymatic degradation. Given as a depot it provides continuous rather than pulsatile receptor occupancy, which first stimulates and then desensitises pituitary gonadotrophs: luteinising and follicle-stimulating hormone rise transiently, then fall as the receptor is downregulated, and gonadal steroid production declines to castrate concentrations over roughly two to four weeks.
Is Triptorelin FDA approved?
Yes. Triptorelin 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 is the half-life of Triptorelin?
Reported half-life for Triptorelin is Depot: weeks to months. Half-life describes how long the compound persists in circulation, not how long any effect lasts, and published figures vary with route of administration, formulation and the population studied.
Is Triptorelin banned in sport?
Triptorelin is recorded here as prohibited in sport. Athletes subject to anti-doping rules should check the current WADA Prohibited List directly, since it is revised annually and classifications change.
What peptides are similar to Triptorelin?
Compounds most often compared with Triptorelin include Leuprolide, Goserelin, Nafarelin and Histrelin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Trelstar labelExternal reference
- WADA Prohibited List 2026External reference
- A Phase 3, Open-Label, Single-Arm Trial of the Efficacy and Safety of Triptorelin 6-Month Formulation in Chinese Children with Central Precocious Puberty — Adv Ther, 2024External reference
- Adolescent Gender Dysphoria in Italy: Reflections on Triptorelin, Consent, and Care — Clin Ter, 2025External reference
- Triptorelin: The Need for Legal Protection Aimed at the Full Political and Social Integration of Gender Variant youth. A Comparison of Different Global realities — Clin Ter, 2025External reference
- GnRH agonist treatment before total laparoscopic hysterectomy for large uteri — J Am Assoc Gynecol Laparosc, 2003External reference
- Spotlight on triptorelin in the treatment of premenopausal women with early-stage breast cancer — Breast Cancer (Dove Med Press), 2018External reference
Related research, comparisons & guides
Related peptides
Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Triptorelin 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
Track Triptorelin research, inventory and reconstitution in the free Peptide Library app. Get the app for iOS or Android →