Summary
Triptorelin is a long-acting GnRH agonist. After an initial surge in LH and testosterone, continuous exposure desensitizes the pituitary and suppresses sex hormones to castrate levels, which is how it treats prostate cancer and early puberty. In IVF it is also used as a single trigger dose.
Structure
pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2. D-Trp at position 6 slows breakdown and increases receptor affinity.
How it works
Sustained GnRH receptor occupancy downregulates and uncouples pituitary receptors, reducing LH and FSH output after about two to four weeks.
Research use cases
Areas where Triptorelin has been studied. Inclusion here does not mean it works for that purpose.
- Advanced prostate cancer
- Central precocious puberty
- Endometriosis and fibroids (outside the US)
- IVF oocyte maturation trigger
What the research found
Class mechanism
The paradoxical suppression by continuous GnRH agonists is well established and forms the basis for their use in hormone-sensitive cancers.1
Safety and open questions
Hot flushes, loss of libido, bone density loss with long-term suppression, and an initial flare of symptoms in prostate cancer.
Regulatory status
FDA-approved for advanced prostate cancer (Trelstar) and central precocious puberty (Triptodur). Prescription only.
Status was accurate when this page was last reviewed on October 26, 2026. Regulations change; check with the relevant authority before relying on it.
Triptorelin: common questions
Does triptorelin raise or lower testosterone?
Both, in sequence. A single dose raises it briefly. Ongoing exposure suppresses it.
Is Triptorelin approved for human use?
FDA-approved for advanced prostate cancer (Trelstar) and central precocious puberty (Triptodur). Prescription only.
References
- Conn PM, Crowley WF Jr. (1994). Gonadotropin-releasing hormone and its analogs. Annual Review of Medicine.
Links open a PubMed search for the exact title, or the original source where one is given.