Bottom line
Triptorelin is a synthetic decapeptide GnRH agonist available as long-acting depot Administered into a muscle. 定义来源: Neutral gloss; usage context: Routes, devices, and absorption primer · 术语表 injections. In the United States, Trelstar is approved for the palliative treatment of advanced prostate cancer and Triptodur is approved for central precocious puberty (CPP) in patients aged 2 years and older. Other triptorelin products have additional jurisdiction-specific indications. Depot strengths and products are not additive or interchangeable — each is formulated for a specific dosing interval. Initial testosterone surge (tumour flare) occurs; label warnings cover cardiovascular, metabolic, seizure, and hypersensitivity risks.
Identity and composition
| Field | Verified information |
|---|---|
| Preferred name | Triptorelin |
| Key aliases | Trelstar (US prostate cancer); Triptodur (US CPP); Decapeptyl (EU/ROW); triptorelin pamoate |
| Molecular/sequence identity | pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 (decapeptide) |
| Modifications/form | D-Trp at position 6; pamoate salt for depot formulation |
| Stable identifiers | The record number of a compound in PubChem, the atlas's primary structure-asset source. A registry record or depiction does not authenticate a commercial sample. 定义来源: Identity and structure assets methodology · 术语表 25074470; UNII 9081Y98W2V |
| Identity caveats | Not interchangeable with other GnRH agonists (leuprolide, goserelin). Trelstar depot strengths are not additive — each is designed for a specific dosing interval |
Development and approval status
| Jurisdiction | Status and indication | Product/source | As of |
|---|---|---|---|
| US (FDA) | Approved: advanced prostate cancer | Trelstar (Verity Pharmaceuticals) | 2000; label revised 03/2025 |
| US (FDA) | Approved: central precocious puberty (CPP) in patients aged ≥2 years | Triptodur (22.5 mg Administered into a muscle. 定义来源: Neutral gloss; usage context: Routes, devices, and absorption primer · 术语表 every 24 weeks) | Approved June 2017; label revised September 2025 |
| EU (EMA) | Approved: prostate cancer, CPP, endometriosis | Decapeptyl (Ipsen) | Ongoing |
| UK (MHRA) | Approved for multiple indications | Decapeptyl SR | Ongoing |
| Canada (Health Canada) | Approved for prostate cancer, CPP | Trelstar | Ongoing |
- UNITED STATES
- US (FDA): Approved: advanced prostate cancer; US (FDA): Approved: central precocious puberty (CPP) in patients aged ≥2 years
- EU/EEA
- EU (EMA): Approved: prostate cancer, CPP, endometriosis
- UNITED KINGDOM
- UK (MHRA): Approved for multiple indications
- OTHER DOCUMENTED
- Canada (Health Canada): Approved for prostate cancer, CPP
Sport status: WADA: Triptorelin is explicitly prohibited at all times in males under S2.2.1 as a GnRH agonist analogue. GnRH analogues are monitored, not prohibited on that basis, in female athletes under 18 in 2026.
Mechanism and pharmacology
GnRH agonist. Continuous depot exposure downregulates pituitary GnRH receptors, suppressing LH/FSH → testosterone castrate levels (less than 50 ng/dL). Initial LH/testosterone surge within 2-4 days. D-Trp substitution at position 6 provides higher potency and longer The time for the amount of a substance in the body to fall by half. 定义来源: Neutral gloss; usage context: Routes, devices, and absorption primer · 术语表 vs native GnRH. Biodegradable microgranule formulation provides sustained release over 4, 12, or 24 weeks.
Evidence by claim
| Claim/indication | Stage | Grade | Best human evidence | Main result | Important limitations |
|---|---|---|---|---|---|
| Advanced prostate cancer | Approved (FDA) | A | Phase 3 A study in which participants are assigned to the study material or a comparator by chance. 定义来源: Neutral gloss; usage context: Evidence grading methodology · 术语表 (Trelstar) | Castrate testosterone maintained in over 95%; equivalent to surgical castration | Tumour flare; no direct comparison with other GnRH agonists |
| Central precocious puberty | Approved (US Triptodur; other products/jurisdictions vary) | A | FDA-reviewed, A study in which participants and investigators know what is administered. 定义来源: Neutral gloss; usage context: Evidence grading methodology · 术语表 50-week pivotal study | Peak stimulated LH was suppressed to prepubertal levels in 93% at month 6 and 98% at month 12 | A study without a separate comparison group. 定义来源: Neutral gloss; usage context: Evidence grading methodology · 术语表 study; approval, formulation, age range, and schedule are product- and jurisdiction-specific |
| Endometriosis | Approved (EU) | A | RCTs | Pain reduction; lesion regression | Limited duration |
Text alternative for the claim-evidence diagram. Each grade is defined below:
- A — Established for a specific labeled use
- 3 claims: Advanced prostate cancer; Central precocious puberty; Endometriosis
- B — Moderate human evidence
- 0 claims
- C — Preliminary human evidence
- 0 claims
- D — Preclinical only
- 0 claims
- E — Anecdotal/marketing claim
- 0 claims
- X — Evidence contradicts or does not support the claim
- 0 claims
Key studies
| Study | Design/population | Exposure studied | Endpoints and result | Limitations |
|---|---|---|---|---|
| Trelstar phase 3 | A study in which participants and investigators know what is administered. 定义来源: Neutral gloss; usage context: Evidence grading methodology · 术语表; advanced PCa | Trelstar 3.75 mg Administered into a muscle. 定义来源: Neutral gloss; usage context: Routes, devices, and absorption primer · 术语表 q4w, 11.25 mg q12w, 22.5 mg q24w | Testosterone suppression less than 50 ng/dL: over 95% at Day 29; cumulative maintenance of castration over 90% | Open-label; no active comparator vs other GnRH agonists or antagonists |
Dose and administration evidence
Approved labeled regimen
The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.
Prostate cancer (US Trelstar):
Trelstar 3.75 mg Administered into a muscle. 定义来源: Neutral gloss; usage context: Routes, devices, and absorption primer · 术语表 q4 weeks
Trelstar 11.25 mg IM q12 weeks
Trelstar 22.5 mg IM q24 weeks
CPP (US Triptodur): 22.5 mg IM every 24 weeks in patients aged ≥2 years.
Route: Single intramuscular injection in either buttock
Note: Dosage strengths are not additive and are not interchangeable across products; select based on desired schedule and indication
Must be administered by a healthcare professional
What is not established
No established or recommended human dose for any unapproved indication.
Safety
Established label risks
Tumour flare (initial weeks) — worsening bone pain, neuropathy, hematuria, urinary obstruction.
Hypersensitivity reactions — anaphylactic shock, angioedema.
Metabolic syndrome — hyperglycemia, diabetes, hyperlipidemia; NAFLD including cirrhosis in post-marketing.
Cardiovascular — MI, sudden cardiac death, stroke risk increased.
Convulsions (post-marketing, including patients with seizure risk factors).
QT interval prolongation (class concern).
Injection site reactions.
Hot flashes.
Unknowns and product-quality risks
Long-term safety in non-oncology indications.
No direct comparative data with leuprolide or goserelin in prostate cancer.
Interactions and special populations
No dose adjustment for renal or hepatic impairment.
Pregnancy: Embryo-fetal toxicity — contraindicated if pregnancy possible.
Lactation: Not recommended.
Regulatory, compounding, and sport notes
US FDA: Prescription only.
The World Anti-Doping Agency; its Prohibited List classifies many peptides as prohibited substances in sport. 定义来源: WADA and sport regulation brief · 术语表: Triptorelin is explicitly prohibited at all times in males under S2.2.1 as a GnRH agonist analogue. GnRH analogues are monitored, not prohibited on that basis, in female athletes under 18 in 2026.
Compounding: Compounded triptorelin not equivalent to Trelstar depot.
Not interchangeable with other GnRH agonists.
Evidence gaps
Head-to-head comparisons with leuprolide, goserelin, and degarelix.
Safety of retreatment in endometriosis.
Optimal sequencing in castration-resistant prostate cancer.
Search notes
Databases and registries: DailyMed, Drugs@FDA, PubMed, EMA
Search terms: triptorelin, Trelstar, Triptodur, Decapeptyl, GnRH agonist, prostate cancer, central precocious puberty
Last searched: 2026-08-06
Inclusion emphasis: FDA label, phase 3 trials
Sources
Trelstar Prescribing Information (Verity, revised 03/2025). https://trelstar.com/wp-content/uploads/2025/03/Trelstar_PI_3-2025.pdf
DailyMed – TRELSTAR. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b1b84d62-a369-a4b7-5c41-dd1f553a18f3
FDA label (accessdata) — Trelstar 2025 update. https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/020715s050,021288s045,022437s025lbl.pdf
DailyMed. Triptodur (triptorelin) prescribing information, revised September 2025. https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=f41380e7-b830-432d-a5f5-a872932f107e
FDA CDER. Triptodur NDA 208956 clinical review (2017). https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208956Orig1s000MedR.pdf
EMA – Decapeptyl product information.
PubChem CID 25074470 (triptorelin). https://pubchem.ncbi.nlm.nih.gov/compound/25074470
