WhatPeptide

Triptorelin

A synthetic GnRH agonist 131× more potent than native GnRH due to D-Trp⁶ substitution. FDA-approved as Trelstar (NDA 020715, 2000) for advanced prostate cancer and as Triptodur for central precocious puberty. Available in 1-, 3-, and 6-month depot formulations.

Strong evidence FDA Approved GnRH Analog

Written by WhatPeptide Editorial Team · Last updated 2026-03-18

Half-life

IV: ~6 min (distribution), ~45 min (intermediate), ~3 hours (terminal). Depot: sustained release over 1-6 months

Dosage range

Prostate cancer: 3.75 mg IM monthly, 11.25 mg IM q12wk, or 22.5 mg IM q24wk. PCT (single case report): 100 mcg single dose (PMID 20416868)

Administration

Intramuscular injection

Research level

Strong

How Triptorelin works

Binds GnRH receptors on pituitary gonadotropes. Initial administration produces a transient LH/FSH/testosterone surge (flare effect). Continuous exposure from depot formulations causes receptor downregulation and desensitization, achieving castrate testosterone levels (≤50 ng/dL) within 2-4 weeks.

Also known as: Triptorelin pamoate, Triptorelin acetate, D-Trp⁶-LHRH, AY-25650, Trelstar, Triptodur, Decapeptyl, Gonapeptyl, Diphereline

Research relevance

Sexual Health
Some relevance 30

Side effects & safety

Hot flashes (most common) Erectile dysfunction and decreased libido Bone mineral density loss with chronic use Tumor flare (initial testosterone surge) Cardiovascular risk with androgen deprivation Injection-site reactions

Contraindications

Pregnancy (Category X — causes fetal harm)
Hypersensitivity to triptorelin, other GnRH agonists, or GnRH

Consult a healthcare provider before use if any of these apply to you.

FAQ

What is Triptorelin? +
A synthetic GnRH agonist 131× more potent than native GnRH due to D-Trp⁶ substitution. FDA-approved as Trelstar (NDA 020715, 2000) for advanced prostate cancer and as Triptodur for central precocious puberty. Available in 1-, 3-, and 6-month depot formulations. Its mechanism of action is supported by robust clinical evidence.
What is Triptorelin researched for? +
Triptorelin has the strongest research relevance for Sexual Health. Evidence is supported by robust clinical evidence.
What are the side effects of Triptorelin? +
Reported side effects include Hot flashes (most common), Erectile dysfunction and decreased libido, Bone mineral density loss with chronic use, Tumor flare (initial testosterone surge), Cardiovascular risk with androgen deprivation, Injection-site reactions. Key contraindications: Pregnancy (Category X — causes fetal harm); Hypersensitivity to triptorelin, other GnRH agonists, or GnRH.
Is Triptorelin FDA approved? +
Yes, Triptorelin has FDA approval for specific indications. Always consult a healthcare provider for appropriate use.
How is Triptorelin administered? +
Triptorelin is typically administered via intramuscular route. Researched dosage range: Prostate cancer: 3.75 mg IM monthly, 11.25 mg IM q12wk, or 22.5 mg IM q24wk. PCT (single case report): 100 mcg single dose (PMID 20416868). Half-life: IV: ~6 min (distribution), ~45 min (intermediate), ~3 hours (terminal). Depot: sustained release over 1-6 months.

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