Triptorelin (Trelstar)

Peptide

Triptorelin is a synthetic decapeptide GnRH agonist. FDA-approved in 2000, available as 1-month (3.75mg), 3-month (11.25mg), and 6-month (22.5mg) formulations. Clinical trials show 97.5% achieve castrate testosterone by day 29 with 6-month formulation. 9-month survival significantly higher than leuprolide (97.0% vs 90.5%, p=0.033). Also approved for adjuvant breast cancer treatment.

Quick Answer

What it is

Triptorelin is a synthetic decapeptide GnRH agonist. FDA-approved in 2000, available as 1-month (3.75mg), 3-month (11.25mg), and 6-month (22.5mg) formulations.

Key findings

  • Grade A: Testosterone Suppression (Prostate Cancer)
  • Grade A: PSA Suppression (Prostate Cancer)
  • Grade A: Overall Survival (Prostate Cancer)

Safety

No specific caution or interaction language was detected in the current summary/outcome notes.

⚠️ Research Notice

This peptide information is for educational and research purposes only. Peptides may not be FDA-approved for human use and may only be legally available for research purposes. Consult qualified healthcare professionals before considering any peptide compounds.

ℹ️ Quick Facts: Triptorelin (Trelstar)

Quick Facts: Triptorelin (Trelstar)

  • Best Evidence:Grade A
  • Conditions Studied:2
  • Research Outcomes:10
  • Grade A Findings:6
  • Grade B Findings:2
  • Key Effect:Prostate Cancer
A6
B2
C1
D1
2 conditions · 10 outcomes

Detailed Outcomes

|
A
Testosterone Suppression
97.5% achieve castrate testosterone by day 29. Mean T of 12.8 ng/dL from month 2-12. Most potent GnRH agonist with lowest mean testosterone levels.
largeImproves
A
PSA Suppression
Median PSA reduced by 96.4% at 12 months. Real-world data shows reduction from 117.9 to 8.5 ng/mL at 6 months.
largeImproves
A
Overall Survival
9-month survival significantly higher than leuprolide (97.0% vs 90.5%; p=0.033). Low nadir testosterone associated with improved OS (p<0.001).
largeImproves
A
Ovarian Function Suppression
Used in TEXT and SOFT trials for premenopausal breast cancer. Approved in EU and US for adjuvant treatment with tamoxifen or AI.
largeImproves
A
Disease-Free Survival (Breast)
SOFT/TEXT trials showed OFS plus tamoxifen provides significant DFS benefit in premenopausal patients. HOBOE trial validated efficacy.
moderateImproves
A
Ovarian Preservation
GIM/PROMISE-GIM6 study: reduces chemotherapy-induced early menopause. Enables fertility preservation in young breast cancer patients.
moderateImproves
B
Anti-Cancer Activity
16 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
moderateImproves
B
Safety/Tolerability
5 human trials support this finding. Human clinical trial data available.
smallImproves
C
Reproductive Outcomes
10 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
moderateImproves
D
Hormone Levels
2 human trials support this finding. Human clinical trial data available.
smallImproves

Research Citations (42)

Efficacy of Triptorelin Combined with Recombinant Human Growth Hormone (rhGH) on Serum Sex Hormones, Bone Age, and Clinical Outcomes in Girls with Precocious Puberty.
(2025)
PMID: 39998154
Testosterone nadir and clinical outcomes in patients with advanced prostate cancer: Post hoc analysis of triptorelin pamoate Phase III studies
(2024)
PMID: 38481666
PRIORITI: Phase 4 study of triptorelin or active surveillance in high-risk prostate cancer
(2024)
PMID: 38958195
GnRH analogue triptorelin acetate induces ovulation in jennies during oestrus.
(2024)
PMID: 38546114
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.
(2024)
PMID: 39412628
Triptorelin nanoparticle-loaded microneedles for use in assisted reproductive technology.
(2023)
PMID: 37387211
The efficacy and safety of triptorelin-therapy following conservative surgery for deep infiltrating endometriosis: A multicenter, prospective, non-interventional study in China.
(2022)
PMID: 35119037
Assessment of Two Formulations of Triptorelin in Chinese Patients with Endometriosis: A Phase 3, Randomized Controlled Trial.
(2022)
PMID: 35947347
Single injection of triptorelin or buserelin acetate in saline solution induces ovulation in mares the same as a single injection of hCG.
(2020)
PMID: 31930759
Spotlight on triptorelin in the treatment of premenopausal women with early-stage breast cancer
(2018)
PMID: 29551913

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