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Triptorelin

Also known as Triptorelin acetate, Triptorelin pamoate, Decapeptyl, Trelstar

A long-acting GnRH agonist decapeptide that initially surges then suppresses LH/FSH and sex hormones, used clinically in prostate cancer, endometriosis, and precocious puberty.

Molecular weight~1311.5 g/mol (peptide base; the pamoate depot salt is ~1699.9 g/mol)
Half-life~3–4 hours (immediate-release acetate); depot/pamoate formulations release over 1–6 months.
CategoryOther

Typical use cases

✓ Hormone suppression research✓ HPG-axis / reproductive research✓ Prostate cancer and endometriosis (approved clinical use)

Dosing guidelines

StartingResearch microdose protocols often cite single ~100 mcg subcutaneous doses; approved depot therapy uses far larger sustained-release doses (e.g. 3.75 mg IM monthly).
MaintenanceClinically delivered as depot injections (e.g. 3.75 mg/month, 11.25 mg/3 months, or 22.5 mg/6 months IM).
Max (studied)Approved depot strengths up to ~22.5 mg per 6-month injection; research microdosing is far smaller — context determines the meaningful range (hedge).

Titration

Not titrated in the usual sense — GnRH agonists cause an initial testosterone/estrogen 'flare' (weeks 1–2) before downregulation and sustained suppression; clinically a flare may be covered by an anti-androgen.

Reconstitution

2 mg research vial: ~2 mL bacteriostatic water yields ~1000 mcg/mL (0.1 mL = 100 mcg); clinical depot products use their own supplied diluents.

Injection sites

Subcutaneous for research acetate vials; approved depot formulations are intramuscular (rotate sites).

Storage & handling

Lyophilized: stable months cool/dark, longer frozen. Reconstituted: refrigerate (2–8 °C).

Side effects

  • Initial testosterone/estrogen 'flare' (can worsen hormone-sensitive disease) Severe · Common
  • Hot flashes Moderate · Common
  • Decreased libido / erectile dysfunction Moderate · Common
  • Reduced bone mineral density (prolonged use) Moderate · Common
  • Injection-site reaction Mild · Common

Research summary

Triptorelin is a synthetic decapeptide GnRH agonist whose D-tryptophan substitution at position 6 resists enzymatic breakdown, giving it a much longer action than native GnRH; like other GnRH agonists it first triggers a surge ('flare') of LH/FSH and sex hormones, after which receptor downregulation produces sustained suppression of testosterone or estrogen. It is an approved drug (e.g. Trelstar/Decapeptyl) for advanced prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and assisted-reproduction protocols. The flare can transiently worsen hormone-sensitive disease, and prolonged suppression carries effects such as hot flashes, sexual dysfunction, and reduced bone density. Educational only — not medical advice.

Key references

  • Trelstar (triptorelin pamoate) — FDA prescribing information
  • Triptorelin — DrugBank (DB06825): mechanism and flare effect

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Educational reference only — not medical advice. Dosing figures are commonly-cited ranges, not prescriptions. Consult a qualified clinician.

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