Triptorelin

AApproved (Rx)Reproductive and neuroendocrine hormones →TrelstarTriptodurDecapeptyl
In one paragraphTriptorelin is a synthetic ten-amino-acid analogue of gonadotropin-releasing hormone, approved since the 1980s and sold as Trelstar for advanced prostate cancer and Triptodur for central precocious puberty. Given continuously it shuts the reproductive axis down after an initial surge. Its grey-market reputation is the opposite use — a single low dose to restart testosterone production after anabolic steroids — and that rests on one published case report of one man, not on any trial.
Schematic 3D structure of Triptorelin
10 residues · GnRH decapeptide with D-Trp at position 6 · schematic
Overall gradeA Established
Human trialsApproval programme; the grey-market use rests on 1 case report
Outcomes graded4
Last reviewed29 October 2026
EvidenceWhat it isHow it worksUnknownsMolecule & PKRegulationQuestionsReferences

What the human research shows

Two pages' worth of evidence under one name. The licensed uses are grade A: decades of use, large approval programmes, three depot intervals on the label. The "HPTA restart" use that brings people to this page is grade D — one case report, n=1, and a mechanism that cuts the other way if the dose is wrong.

MetabolicCardioMuscleHealingNeuroImmuneSexualSkinAgeing

Evidence profile0–5

  • Metabolic & weight—0.0
  • Cardiovascular—0.0
  • Muscle & growth—0.0
  • Healing & repair—0.0
  • Neuro & sleep—0.0
  • Immune & inflammation—0.0
  • Sexual & hormonalA5.0
  • Skin & appearance—0.0
  • Ageing & longevity—0.0
Each score is confidence × effect size, taken from the best-evidenced benefit in that domain: the grade (A–D) sets the confidence, the measured effect sets the size. Hover a domain to see the outcomes behind it. Adverse effects are excluded and listed separately below.
OutcomeGradeEffect sizeHuman studiesWhere the evidence comes from
Testosterone suppression in advanced prostate cancerAEstablishedLargeApproval programme; decades of useThe licensed indication. Continuous GnRH receptor occupancy desensitises the pituitary, and after a transient surge testosterone falls to castrate levels. The Trelstar label carries three depot intervals for this use and the effect is the basis of forty years of androgen-deprivation therapy.1
Central precocious pubertyAEstablishedLargeApproval programmeTriptodur is approved for central precocious puberty in children aged two and above, as a single depot injection repeated every 24 weeks — the same axis shutdown used to halt premature puberty.2
Restarting testosterone after anabolic steroidsDNo human evidenceNot measurable1 case report (n=1)A 2010 Italian case report describes one man with hypogonadism after anabolic steroid use who was given a single 100 μg dose of triptorelin; testosterone was in the normal range within a month. One patient, no control, no replication in sixteen years. Forum protocols built on this report also ignore the dose relationship: the licensed depot products use the same molecule to switch the axis off.3
Initial testosterone surge ("flare")adverseAEstablishedModerateApproval programmeThe first days after a depot injection bring a rise in testosterone before suppression — clinically important in prostate cancer because it can transiently worsen symptoms, and the reason anti-androgen cover is used.1
AMultiple good human trials, consistentBSome human trials, mostly consistentCFew or weak human studiesDAnimal or anecdotal onlyeffect size · red = adverse

Literature searched to 29 October 2026. Human studies only; animal and cell work informs the mechanism section and nothing else.

Registered trials

ClinicalTrials.gov lists 110+ interventional studies naming Triptorelin as an intervention — 50 completed, 12 recruiting, and 24 with results posted to the registry.

A registration is not a result. Anyone can register a study, and many never report — so this list shows what has been attempted, not what has been shown. The graded evidence above is the answer to whether something works.

StudyPhaseStatusParticipantsSponsorResults
A Study of Immediate 9 Months Adjuvant Hormone Therapy With Triptorelin 11.25 mg Versus Active Surveillance After Radical Prostatectomy in High Risk Prostate Cancer Patients.NCT01753297 · started Dec 2012Phase 4Completed226IpsenPosted
Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue AdministrationNCT01161563 · started Jul 2010Phase 4Completed118Watson PharmaceuticalsPosted
Suppression of Ovarian Function With Either Tamoxifen or Exemestane Compared With Tamoxifen Alone in Treating Premenopausal Women With Hormone-Responsive Breast CancerNCT00066690 · started Dec 2003Phase 3Completed3,066ETOP IBCSG Partners FoundationPosted
Triptorelin With Either Exemestane or Tamoxifen in Treating Premenopausal Women With Hormone-Responsive Breast CancerNCT00066703 · started Nov 2003Phase 3Completed2,672ETOP IBCSG Partners FoundationPosted
Effect of Triptorelin (Decapeptyl®) 22.5 mg on Two Biomarkers in Patients With Advanced Prostate CancerNCT01020448 · started Nov 2009Phase 3Completed339IpsenPosted
Study to Compare the Oestradiol Suppression, Clinical Efficacy and Safety of Two Formulations of Triptorelin (Triptorelin Pamoate PR 3-month and Triptorelin Acetate PR 1-month) in Chinese Subjects With EndometriosisNCT03232281 · started Jul 2017Phase 3Completed300IpsenPosted
A Study to Assess the Efficacy and Safety of Ganirelix (Orgalutran®) Treatment in Chinese Women Undergoing Controlled Ovarian Stimulation for in Vitro Fertilization (IVF) or Intra Cytoplasmatic Sperm Injection (ICSI) (Study 38651)(P05703)NCT00725491 · started May 2007Phase 3Completed259Organon and CoPosted
Effects of Triptorelin Pamoate 6-month When Given to Adult Chinese Participants With Advanced Cancer in the ProstateNCT05590793 · started Nov 2022Phase 3Completed195IpsenPosted

102 further studies are registered. Participant counts marked * are the sponsor's estimate, not a final enrolment. Source: ClinicalTrials.gov, read directly from the registry and refreshed weekly.

What it is

Triptorelin is GnRH with one substitution: the glycine at position six is replaced by D-tryptophan, which resists the enzymes that destroy the natural hormone in minutes. The Trelstar label gives the structure as a synthetic decapeptide. The result is a molecule that occupies the receptor long enough to desensitise it — the same trick leuprolide uses, from the same era.

It is supplied as a depot suspension for intramuscular injection in several intervals. The grey-market product sold as a single-use vial for "restart" protocols is a different preparation from the licensed depots, and in most of LYO's regions selling it for human use without authorisation is unlawful.

How it is thought to work

Pulsed GnRH keeps the pituitary releasing LH and FSH; GnRH present continuously desensitises the receptor and stops them. Triptorelin's long action makes it a continuous signal, which is why it suppresses. The restart idea uses the opposite end of the curve: a single small dose as one artificial pulse, intended to prompt one burst of LH and FSH and so restart a suppressed axis. The pharmacology of that is coherent; the human evidence for it is one man.

What is still unknown

  • Whether a single low dose restarts the axis in anyone other than the one reported patient — no trial has tested it.
  • What dose, if any, produces a pulse rather than the beginning of suppression.
  • Whether the case report's outcome would have occurred spontaneously, as post-steroid hypogonadism often resolves without treatment.

The molecule and how long it lasts

Identity
Formula
C64H82N18O13
Molecular weight
1311.4 g/mol
CAS number
57773-63-4
PubChem
CID 25074470
Sequence
[pGlu]HWSY[D-Trp]LRPG-NH2

Matches the decapeptide structure given in the Trelstar label.

PubChem record, read 29 October 2026; the sequence was derived from that record's own structure and checked against the product label where one exists.

Pharmacokinetics
Route
Intramuscular depot injection
Half-life
About 6 minutes, 45 minutes and 3 hours in a three-compartment model
Licensed regimen (Trelstar)
Depot injection repeated every 4, 12 or 24 weeks depending on the strength used, for advanced prostate cancer; Triptodur is a 24-week depot for central precocious puberty

From the approved product's prescribing information: Trelstar prescribing information (DailyMed) The regimen is the label's own wording, reproduced as a regulatory fact.

Regulatory status

European Union
Approved, prescription-only

Authorised nationally across member states (Decapeptyl and others) for prostate cancer, endometriosis, uterine fibroids, precocious puberty and in assisted reproduction.

United States
Approved, prescription-only

Trelstar for advanced prostate cancer; Triptodur for central precocious puberty. Vials sold online for "restart" protocols are unapproved drugs.

United Kingdom
Licensed, prescription-only

Decapeptyl SR licensed by the MHRA.

Australia
Registered, Schedule 4

Diphereline / Decapeptyl registered on the ARTG.

Canada
Authorised, prescription-only

Trelstar authorised with a Drug Identification Number.

Sport (WADA)
Prohibited for males at all times

GnRH agonists are S2 (peptide hormones, growth factors and related substances) for male athletes.

Questions people actually ask

Does a single triptorelin shot restart testosterone after a steroid cycle?
One published case report, of one man, says his testosterone normalised within a month of a single 100 μg dose. That is the entire evidence base, and post-cycle hypogonadism also resolves on its own. The same molecule in its licensed form is used to shut the axis down.
Is triptorelin the same as leuprolide?
Both are GnRH agonists from the same generation that suppress the axis through continuous receptor occupancy. They differ in the substituted residues and in which depot products are licensed where.
Is triptorelin banned in sport?
Yes, for male athletes — GnRH agonists sit in S2 of the Prohibited List, prohibited at all times.

One page per claimed effect

References

  1. 1
    Trelstar (triptorelin pamoate) prescribing information.DailyMed, read 29 Oct 2026Advanced prostate cancer; three depot intervals; pharmacokinetics and the decapeptide structure.
  2. 2
    Triptodur (triptorelin) prescribing information.DailyMed, read 29 Oct 2026Central precocious puberty in children aged 2 and above; 24-week depot.
  3. 3
    Pirola I, Cappelli C, Delbarba A, et al. Anabolic steroids purchased on the Internet as a cause of prolonged hypogonadotropic hypogonadism.Fertil Steril, 2010;94:2331–2332Case report, n=1. The origin of the "triptorelin restart" protocol.

Change log

  • 2026-10-29Initial publication. Grade A for the licensed uses; the grey-market restart row graded D on a single case report.