Library · Reproductive · Treatment of hormone-dependent cancers and reproductive disorders
Triptorelin
Decapeptyl, Diphereline, Gonapeptyl, AY-25650
A synthetic GnRH agonist decapeptide, first developed in the 1970s, that initially raises then suppresses sex hormones with continued use. An established treatment for prostate cancer, endometriosis, precocious puberty, and assisted reproduction, under several brand names.
Research score 95/100. Reference only, not a dose.
- Hormone Regulation
- Anti-cancer
- Fertility Enhancement
- GnRH Agonist
- US status
- Prescription Only
- Approval
- FDA + EMA Approved
- Evidence
- FDA-approved GnRH agonist (Trelstar). Standard of care for advanced prostate cancer (androgen deprivation therapy), endometriosis, and central precocious puberty.
- Research score
- 95 / 100
- Indication
- Multiple Approved Indications
- Origin
- France
- Source category
- Reproductive System
- Status group
- Approved / prescription
Mechanism
Initially stimulates FSH and LH release, but continuous use downregulates and desensitizes GnRH receptors, suppressing gonadal hormone output to castration levels within one to two weeks after an initial 'flare,' through prolonged receptor binding, calcium mobilization, and protein kinase C activation.
Safety file
Common effects include hot flashes, reduced libido, and injection-site pain; serious risks include an initial tumor flare, metabolic effects, bone density loss, and rare seizure risk; contraindicated in pregnancy.
- Hot flashes
- Mood changes
- Decreased libido
- Initial testosterone surge
- Injection site reactions