Triptorelin

GnRH agonist approved for prostate cancer and early puberty; a single small dose is used off-label to trigger ovulation in IVF.

FDA-approved WADA prohibited A Evidence Approved drug or multiple human RCTs

Also called Trelstar, Triptodur, Decapeptyl, Gonapeptyl, Gonapeptyl Daily, Triptorelin pamoate, Triptorelin acetate, D-Trp6-LHRH

All peptides Last reviewed October 26, 2026
Legal status FDA-approved Banned in sport (WADA)
Evidence grade A Approved drug or multiple human RCTs
Human studies 250 published, approximate count
Half-life About 2.8 hours time for levels to halve
Route studied Intramuscular depot (Trelstar, Triptodur) plus subcutaneous daily injection (decapeptyl, gonapeptyl 0.1 mg)
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What it is

Triptorelin is a 10-amino-acid copy of GnRH, the brain hormone that tells the pituitary to release LH and FSH. Swapping one amino acid for D-tryptophan makes it far more potent and longer-lasting than natural GnRH. Like leuprolide, it works in two phases: one dose releases a burst of LH and FSH, while steady dosing shuts the pituitary down and drives testosterone or estrogen to very low levels.

In the US, Trelstar depots (every 4, 12 or 24 weeks) are approved for advanced prostate cancer, and Triptodur (every 24 weeks) for central precocious puberty in children 2 and older. In Europe, a 0.1 mg daily injection sold as Decapeptyl or Gonapeptyl is authorised to keep the pituitary quiet during IVF stimulation. IVF clinics also give a single 0.1 to 0.4 mg dose off-label to trigger final egg maturation instead of hCG; in a 131-woman study, 0.1 mg matured eggs as well as 0.2 or 0.4 mg.

Read the full overview 1 more

Some bodybuilders search for triptorelin as a one-shot way to restart testosterone after a steroid cycle. No published trial has tested that. What studies do show is a short LH and testosterone rise after a dose, and suppression when dosing continues. WADA bans triptorelin in male athletes, and a 2025 study found a triptorelin breakdown product in urine that anti-doping labs can test for.

Structure 10 residues
1. pGlu pGl 2. Histidine H 3. Tryptophan W 4. Serine S 5. Tyrosine Y 6. D-Tryptophan dW 7. Leucine L 8. Arginine R 9. Proline P 10. Glycine G N C
  • Hydrophobic
  • Polar
  • Positive charge
  • Gly / Pro / Cys
  • Non-standard
Sequence
pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
Length
10 amino acids
Molecular weight
1311.4 g/mol (free base, C64H82N18O13)
Origin
Synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) with D-tryptophan in place of glycine at position 6. Sold as the pamoate salt in long-acting depots (Trelstar, Triptodur) and as the acetate in daily injections (Decapeptyl, Gonapeptyl).

How Triptorelin works

What it binds to, and what happens inside the body after that, step by step.

Outside the cell Inside the cell
Target GnRH receptor on pituitary gonadotroph cells (agonist; continuous use causes desensitization)

Triptorelin binds GnRH receptors on the pituitary. A single dose releases LH and FSH, and in women at the end of IVF stimulation that LH surge finishes egg maturation, the way a natural mid-cycle surge does. Continuous exposure desensitizes the receptors, so LH, FSH and sex hormones fall to castrate or prepubertal levels; this is how the depots treat prostate cancer and early puberty.

  1. 1 Receptor binding Triptorelin binds pituitary GnRH receptors; in rat pituitary cells it was 100 times more active than natural GnRH at releasing LH.
  2. 2 LH and FSH burst One dose releases a burst of LH and FSH. Testosterone rises above baseline in the first week of depot treatment.
  3. 3 IVF trigger use In IVF cycles run with a GnRH antagonist, one 0.1 to 0.4 mg injection creates an LH surge that matures the eggs, with far less ovarian hyperstimulation risk than hCG.
  4. 4 Desensitization With continued exposure from a depot or daily dosing, the pituitary stops responding and LH and FSH fall.
  5. 5 Hormone shutdown Testosterone reached castrate levels (50 ng/dL or less) by day 29 in 91% to 98% of men on Trelstar, and LH stayed at prepubertal levels in at least 93% of children on Triptodur.

What the studies show

Human results and animal results are kept apart below. A result in rats tells you a mechanism is plausible. It does not tell you what happens in a person.

A Evidence

Triptorelin is an approved drug: Trelstar's label trials show castrate testosterone by day 29 in 91% to 98% of men, and Triptodur suppressed early puberty in at least 93% of 44 children. Its use as an IVF trigger rests on the GnRH agonist trigger trials and Cochrane review plus smaller dose studies, including a retrospective study of 131 women that found 0.1 mg as effective as 0.2 or 0.4 mg. Its use for testosterone recovery after steroids has no published human trial.

How far the evidence reaches Highest rung: Regulatory approval
  1. Cell studies In a dish None listed
  2. Animal studies Rodents and other models None listed
  3. Small human studies Open-label, case series 5 key studies below
  4. Randomized trials Placebo-controlled RCTs, meta-analyses 1 key study below
  5. Regulatory approval Approved as a medicine Yes
Preclinical: tells you a mechanism is plausible Human: tells you what happened in people (250 published studies, approx.)

In people 6

Case series 2019

Is oocyte maturation rate associated with triptorelin dose used for triggering final oocyte maturation in patients at high risk for severe ovarian hyperstimulation syndrome?

131 women at high risk of OHSS having ICSI with an antagonist protocol, retrospective

Egg maturation rates were 82.6%, 83.3% and 85.1% after 0.1, 0.2 and 0.4 mg triptorelin, with no significant difference.

Read the study
Meta-analysis 2014

Gonadotropin-releasing hormone agonist versus HCG for oocyte triggering in antagonist-assisted reproductive technology (Cochrane review)

17 RCTs, 1,847 women in IVF/ICSI

A GnRH agonist trigger cut OHSS (odds ratio 0.15) but lowered live birth in fresh transfers (odds ratio 0.47).

Read the study
Case series 2015

Gonadotropin-releasing hormone agonist triggering is effective, even at a low dose, for final oocyte maturation in ART cycles: case series

9 women given 0.1 mg triptorelin, compared with 14 matched women given 0.2 mg

Mature egg numbers and pregnancy rates did not differ between 0.1 mg and 0.2 mg, and no woman developed OHSS.

Read the study
Show all 6 studies
Human, open-label 2011

Comparison of human chorionic gonadotropin (Pregnyl 10,000 IU) versus GnRH agonist (triptorelin 0.2 mg) for final oocyte maturation in egg donors

Egg donors, each stimulated twice (hCG trigger, then triptorelin trigger)

Triptorelin 0.2 mg gave the same number of mature eggs as hCG (13.0 vs 12.6); one donor needed treatment for OHSS after hCG.

Read the study
Human, open-label 1981

Long-term effect of D-Trp6-luteinizing hormone-releasing hormone on testicular size and LH, FSH and testosterone levels in hypothalamic hypogonadotropic males

6 men aged 18 to 34 with hypothalamic hypogonadism, 6 months

10 mcg every other day raised the LH response at 1 month, but by 6 months it was back at baseline; the authors called this a paradoxical inhibitory response, probably from too high a dose.

Read the study
Case series 2025

The impact of triptorelin on hormone levels in human and its metabolite confirmation for doping control analysis

5 men with prostate cancer starting triptorelin, compared with leuprorelin

Triptorelin suppressed LH and testosterone more than leuprorelin, and its breakdown product triptorelin (5-10) was found in urine and blood.

Read the study

In animals and cells 0

No preclinical studies are listed as key studies here. The human data above carries the evidence.

New studies

When a new Triptorelin study in people is published, the daily email covers it.

What nobody has measured yet

These are questions the published research has not answered.

  1. 01 Whether one triptorelin injection speeds testosterone recovery after anabolic steroid use; no controlled human study exists.
  2. 02 The dose that would stimulate a man's pituitary without suppressing it; the only multi-week study in men (6 men, 1981) saw stimulation turn into suppression.
  3. 03 The best trigger dose in women who are not at high risk of OHSS; the 0.1 versus 0.4 mg data come from a retrospective high-risk group.
  4. 04 Bioavailability after subcutaneous injection is not stated on the US labels.

Triptorelin from discovery to today

1981202544 years of research history
  1. 1981Study in 6 men with hypogonadism shows D-Trp6-LHRH (triptorelin) first stimulates, then suppresses, LH.
  2. 1989Decapeptyl 0.1 mg authorised in the Netherlands for prostate cancer.
  3. 2000FDA approves Trelstar 3.75 mg for advanced prostate cancer.
  4. 2008Gonapeptyl 0.1 mg daily authorised in the Netherlands for down-regulation in IVF, later recognised in 12 more EU states.
  5. 2010FDA approves the 24-week Trelstar 22.5 mg depot.
  6. 2017FDA approves Triptodur for central precocious puberty.
  7. 2019Study of 131 women finds a 0.1 mg triptorelin trigger matures eggs as well as 0.2 or 0.4 mg.
  8. 2025Thai anti-doping lab confirms triptorelin (5-10) as a urine marker of triptorelin use.
Approval or regulatory milestoneResearch milestone
Regulatory · reviewed October 26, 2026

When the FDA or WADA changes Triptorelin's status, it's in the next morning's email.

How long it stays in the body

Half-life
About 2.8 hours
About 2.8 hours after an IV dose in healthy men; about 6.6 hours with moderate kidney impairment. Depots release drug over 4, 12 or 24 weeks.
Routes studied
Intramuscular depot (Trelstar, Triptodur), Subcutaneous daily injection (Decapeptyl, Gonapeptyl 0.1 mg)
Bioavailability
Not stated on the US labels, which cover intramuscular depots. Not active by mouth.
Notes
After 0.5 mg IV in 6 healthy men, 41.7% of the dose came out unchanged in urine. Elimination is by both liver and kidneys; clearance falls with kidney and especially liver impairment. Young men with high creatinine clearance cleared it twice as fast as patients with moderate kidney impairment.
Single-dose clearance

How much of Triptorelin is left after a single dose

50%left after 2.8 hours
100%50%25%12.5%2.8h5.6h8.4h11h14htime after dose100%50%25%2.8h8.4h14htime after dose
Half-lifeAbout 2.8 hours
About 97% cleared14 hours

Simple first-order model from the published half-life. Real clearance varies with dose, route, kidney and liver function and formulation. This is not a dosing schedule.

Doses used in published studies

This table records the doses that trials and approved labels used, with the source for each row. It is a record of research, not a recommendation, and it is open to free members.

Doses used in published research and approved labels5 rows
Checking membershipEach row names the trial or label, the dose, route, frequency, duration and a link to the source. Free account, no card.

Side effects, higher-risk groups and interactions

4Commonroughly 1 in 10 or more
2Uncommonroughly 1 in 100 to 1 in 10
1Rareunder 1 in 100
EffectCommonUncommonRareUnknown
Hot flushes58.6% of men on Trelstar 3.75 mg; also reported in children on Triptodur.Common
Erectile dysfunction, testicular shrinkage, skeletal pain, headacheAt least 5% on one or more Trelstar strengths.Common
Tumor flare or early puberty signs at the startTestosterone rises in the first week; in children, puberty signs and vaginal bleeding can briefly increase.Common
Injection site reactionsMost common reaction in Triptodur trials.Common
Mood changes and emotional labilityPost-marketing reports of crying, irritability, anger and aggression with GnRH agonists.Uncommon
High blood sugar, heart attack, stroke, QT prolongationClass warnings on the Trelstar label for men on androgen deprivation.Uncommon
Seizures, severe skin reactions (SJS/TEN, DRESS), anaphylaxis, pseudotumor cerebriPost-marketing reports; pseudotumor cerebri is reported in children.Rare
Groups with specific risks
  • Allergy to triptorelin, GnRH or other GnRH agonists
  • Pregnancy (may cause fetal harm)
Interactions
  • Drugs that prolong the QT interval: androgen deprivation can add to QT prolongation.
  • Drugs that raise prolactin: the Trelstar label says not to combine them, because high prolactin reduces pituitary GnRH receptors.
  • Tests of pituitary and gonadal function are unreliable during treatment and for a period after stopping.

Which symptoms are expected and which mean stop and get help: side effects and red flags.

What people say online, checked against the studies

Tap a claim to see what the studies found.

The claim"One triptorelin shot restarts natural testosterone after a steroid cycle."UntestedNobody has measured this in people

No published trial has given triptorelin to men coming off anabolic steroids. A dose does release LH briefly, but in 6 men given it every other day the LH response faded by 6 months, and continuous dosing is how the drug shuts testosterone down in prostate cancer.

The claim"A 0.1 mg trigger is too small to mature eggs."SupportedHuman evidence backs this

In 131 high-risk women, maturation rates were 82.6% with 0.1 mg vs 83.3% and 85.1% with 0.2 and 0.4 mg. That was a retrospective study, not a randomized trial.

The claim"A triptorelin trigger is safer than hCG with no trade-off."MixedSome studies agree, some do not

Agonist triggers sharply cut OHSS, but a Cochrane review found fewer live births when embryos are transferred fresh in the same cycle. The review authors suggest it for egg freezing, egg donors and freeze-all cycles, and the live-birth gap was seen mainly when luteal support had no LH activity.

The claim"Triptorelin cannot be detected in drug tests."Not supportedThe evidence does not back this

WADA lists it by name, and a 2025 study confirmed triptorelin (5-10), a breakdown product found in urine and blood, as a marker labs can test for.

Combinations people discuss

These pairings come up often. Almost none have been tested together in a trial, and the evidence note on each says so plainly.

Antagonist protocol with a triptorelin trigger

A GnRH antagonist blocks early ovulation during stimulation without taking the pituitary offline, so a single triptorelin dose can still release an LH surge to mature the eggs.

EvidenceSupported by the Cochrane review of 17 RCTs on agonist triggers: much less OHSS, fewer live births in fresh transfers. Off-label in the US.

Triptorelin as post-cycle therapy

Promoted online as a single injection to restart LH and testosterone after anabolic steroids.

EvidenceUntested. No study in men coming off steroids; continued dosing suppresses the pituitary, and WADA bans it in males.

Storage and stability

Dry powder (lyophilized)

Trelstar and Triptodur kits: 20 to 25°C (68 to 77°F); do not freeze.

Mixed with water (reconstituted)

Trelstar must be injected within 2 minutes of mixing; Triptodur settles fast and must be injected immediately after mixing.

Guide Reconstitution and storage, explainedMembers Bacteriostatic water, fridge vs freezer, and how fast peptides break down.

Related peptides

New Triptorelin research, explained when it is published

One email when a trial reads out, a label changes or the FDA acts on a peptide. Free, every source linked, unsubscribe any time.

Frequently asked questions
What is triptorelin used for?
In the US: advanced prostate cancer (Trelstar) and central precocious puberty (Triptodur). In Europe a 0.1 mg daily injection is approved to stop early ovulation during IVF. IVF clinics also use a single dose to trigger egg maturation, which is off-label in the US.
What does the 0.1 mg triptorelin trigger do?
In an IVF cycle run with a GnRH antagonist, one injection makes the pituitary release a burst of LH that finishes egg maturation before retrieval. It lowers the risk of ovarian hyperstimulation compared with hCG.
Does triptorelin raise testosterone in men?
Briefly. A dose releases LH and testosterone rises in the first days, but continued dosing shuts the pituitary down and testosterone falls to castrate levels within about 4 weeks. That is how it treats prostate cancer.
Is triptorelin banned in sport?
For men, yes. WADA's S2.2.1 names triptorelin among GnRH agonists prohibited in males at all times. Labs can detect a triptorelin breakdown product in urine.
What is the difference between Trelstar and Triptodur?
Both are triptorelin pamoate depots injected into muscle. Trelstar treats advanced prostate cancer every 4, 12 or 24 weeks. Triptodur is a 22.5 mg dose every 24 weeks for children 2 and older with central precocious puberty.