Triptorelin
moderate riskAlso: Trelstar · Decapeptyl · GnRH agonist
Triptorelin is an FDA-approved GnRH agonist that paradoxically causes chemical castration through pituitary desensitization with continuous dosing. Approved for prostate cancer, endometriosis, and precocious puberty. Also used off-label post-cycle in performance enhancement contexts.
Reported Benefits
Prostate cancer (androgen suppression)
FDA-approved standard of care for advanced prostate cancer; achieves castrate testosterone levels.
Endometriosis
Reduces endometriosis lesion size and pain scores via estrogen suppression.
PCT (off-label)
Used in performance enhancement PCT to restart HPG axis; limited formal study but mechanistically rational.
Mechanism of Action
Long-acting GnRH agonist — initial stimulation followed by sustained pituitary GnRH receptor downregulation, profoundly suppressing LH, FSH, testosterone/estrogen to castrate levels.
Key Clinical Studies
Crawford et al. (1989)
Phase III RCT · n=244
Castrate testosterone levels in advanced prostate cancer; comparable to orchiectomy
Paradoxical Mechanism
GnRH agonists cause hypogonadism by flooding the pituitary with continuous stimulation — the opposite of pulsatile physiologic GnRH. This downregulation is the therapeutic mechanism in prostate cancer and endometriosis.
Off-Label PCT Use
In performance enhancement contexts, triptorelin has been used to rapidly restart the HPG axis post-anabolic steroid cycle. This use is not FDA-approved and carries significant risk due to the biphasic agonist/antagonist nature of the compound.
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Regulatory Status
FDA ApprovedFDA approved (Trelstar) for prostate cancer and other indications
Safety Profile
Side Effects
- •Hot flashes
- •Bone density loss
- •Sexual dysfunction
- •Fatigue
- •Initial testosterone surge ('flare effect')
Contraindications
- •Pregnancy
- •Hormone-sensitive conditions not being treated
Drug Interactions
- •QT-prolonging drugs
- •Sex steroid supplements
Primary Uses
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