Overview
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In plain language
Triptorelin is a GnRH agonist given as a monthly or three-monthly intramuscular injection, sold as Trelstar. It is used for advanced prostate cancer and for central precocious puberty in young children.
Like other drugs in its class, it first raises then permanently switches off the body's production of sex hormones. In men this lowers testosterone to castrate levels to treat prostate cancer; in children with early puberty it pauses the premature activation of puberty until an appropriate age.
For students
Triptorelin is [D-Trp6]GnRH (about 1,311 Da), a single-substitution decapeptide developed by Debiopharm and marketed by Ipsen. The D-tryptophan at position 6 resists proteolysis and increases receptor affinity, and the drug is formulated as a biodegradable microgranule or polymer depot given every 1, 3 or 6 months.
In central precocious puberty (CPP), the same downregulation strategy pauses the hypothalamic-pituitary-gonadal axis, halting bone-age advancement and allowing normal adult height, a use approved in the U.S. in 2011 after long European experience. The drug's central role in the classic 2009 E2503 adjuvant breast cancer trial era is a footnote; its main evidence base is prostate cancer and CPP.
For researchers and instructors
Biochemistry. The D-Trp6 substitution is shared with leuprolide's D-Leu6, illustrating how different position-6 residues tune potency and duration; the peptide otherwise retains the native pyroGlu1 and Gly10-NH2.
Pharmacology. Intramuscular depot every 4, 12 or 24 weeks; testosterone suppression equivalent to surgical castration; in CPP, LH response to stimulation testing is the monitoring endpoint.
Human evidence. Pivotal trials in advanced prostate cancer (versus orchiectomy) and randomized CPP studies showing improved adult height prediction support its approved uses.
Teaching point. One molecule, two opposite-seeming uses (sex hormone excess in cancer, sex hormone timing in children), unified by the same receptor-downregulation mechanism.
Molecular identity
- Amino acids
- 10 (decapeptide)
- Molecular weight
- ~1,311 Da
- Formula
- C₆₄H₈₂N₁₈O₁₃
- Sequence
- GnRH with D-Trp6
Origin and history
Triptorelin replaces the glycine at position 6 of GnRH with D-tryptophan, slowing breakdown. Developed by Debiopharm and marketed by Ipsen and others, it was approved in the U.S.
in 2000 as a monthly (and later three-monthly) intramuscular depot for advanced prostate cancer, and later for central precocious puberty in children.
Key people
- Debiopharm research teamDeveloped triptorelin
Timeline
- 2000
Trelstar approved by the FDA
See every peptide on one history timeline.
Human evidence
Randomized trials established castrate-level testosterone suppression and its use in precocious puberty.
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. Causes an initial hormone surge; long-term use thins bones and causes hot flashes.
This profile is educational and does not provide treatment, dosing or sourcing guidance.
Sources
- PubMed literature search: Triptorelin
- PubChem compound search: Triptorelin
- DailyMed (FDA label search): Triptorelin
- UniProt search: Triptorelin
- ClinicalTrials.gov search: Triptorelin
Hernandez Gener, E. (November 8, 2026). Triptorelin: molecular data, research history and evidence. VALREXA Biosciences. https://valrexa.com/peptides/triptorelin.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