PEPTOKING
EN

Gonadorelin

Gonadotrophin-releasing hormone (synthetic GnRH)

Status

Approved

Authorised in France as Lutrelef (since 1985) for pulsatile ovulation induction, while its US human products, Factrel (approved 1982) and Lutrepulse (1989), are both discontinued; it is prohibited for male athletes.

Evidence

Moderate

Pulsatile GnRH has decades of clinical use with high ovulation rates in hypothalamic amenorrhoea, but the evidence comes mainly from clinical series rather than large randomized trials.

In sport

WADAProhibited (WADA)

Gonadorelin is a synthetic copy of gonadotrophin-releasing hormone (GnRH), the brain signal that starts the reproductive hormone cascade. Given in pulses by a small pump, it can restore ovulation in women whose brain does not release enough GnRH.

Structure

10 residues

Point at a bead, or focus the chain and use the arrow keys, to name it. Pick a chemistry to highlight it.

Sequence as text
pGlu-H-W-S-Y-G-L-R-P-G-NH2

What it is used for

  • Inducing ovulation in women with infertility from hypothalamic GnRH deficiency, by pulsatile pump (approved)
  • Diagnostic testing of pituitary gonadotrophin function, the indication of the discontinued US product Factrel (approved)
  • Inducing sperm production in men with GnRH deficiency (studied)

How it works

Gonadorelin is identical to natural GnRH. It binds GnRH receptors on pituitary gonadotroph cells, releasing LH and FSH, which drive ovulation, sperm production and sex hormone production. The pattern of delivery is critical: pulses roughly every 60 to 90 minutes restore normal pituitary output, whereas continuous exposure desensitises the receptors and shuts the system down, the principle behind long-acting GnRH agonists such as leuprolide.

How strong the evidence is

ModerateAt least one good randomised trial, or consistent smaller human trials.

Classic primate experiments showed that hourly GnRH pulses restored gonadotrophin secretion after hypothalamic damage, while continuous infusion failed to sustain it and caused desensitisation (Belchetz 1978, Science). A clinical review by Martin and colleagues (1990) concluded that physiological pulsatile GnRH replacement gives high rates of ovulation and conception in women with hypothalamic amenorrhoea and complete GnRH deficiency, with lower rates in polycystic ovary syndrome. The French Lutrelef label notes that ovarian hyperstimulation is uncommon with pulsatile GnRH compared with other ovulation induction methods.

Risks and side effects

  • Injection-site pain, inflammation, infection or superficial thrombophlebitis at the pump needle
  • Headache, nausea, abdominal pain and heavy periods
  • Multiple follicles, multiple pregnancy and, uncommonly, ovarian hyperstimulation syndrome
  • Allergic reactions, occasionally severe
  • Pituitary apoplexy (bleeding) reported in people with pituitary tumours given diagnostic doses
  • Prohibited for male athletes at all times (WADA S2)

Label dosing

Label (Lutrelef, France): 10 to 20 micrograms per pulse given under the skin every 90 minutes by a portable pump.

Summarised from the official prescribing information. Not a recommendation: dosing is decided with a prescriber.

Regulatory status

RegionYearApproved for
USFDA1982Evaluating the gonadotrophin-releasing capacity of the anterior pituitary (product discontinued)
EUANSM (France, national authorisation)1985Ovulation induction for infertility caused by hypothalamic anovulation

Status by country

JurisdictionStatusSource
USUnited StatesWithdrawnSource 2
EUEuropean UnionAuthorised in some member statesSource 1
UKUnited KingdomAuthorised medicineSource 10
AUAustraliaNo authorised medicineSource 11
CACanadaAuthorised medicineSource 12
Whether a medicine containing it is authorised, checked in each regulator’s records on Oct 1, 2026.

Status of every peptide by country

Trials of Gonadorelin to watch

  1. Phase 2, Phase 3Recruiting

    Pulsatile GnRH in Down syndrome(opens the source in a new tab)

    GnRH Therapy on Cognition in Down Syndrome

    Primary completion expected December 202856 participantsSponsor: Nelly PitteloudNCT04390646

All trials to watch

Timeline

  1. 2028

    1. Pulsatile GnRH in Down syndrome

  2. 1985

    1. Approved, EU (ANSM (France, national authorisation))Ovulation induction for infertility caused by hypothalamic anovulation

  3. 1982

    1. Approved, US (FDA)Evaluating the gonadotrophin-releasing capacity of the anterior pituitary (product discontinued)

Sources

  1. 01LUTRELEF 3,2 mg: summary of product characteristics and patient leaflet(opens the source in a new tab) Base de Donnees Publique des Medicaments (ANSM, France), 2019
  2. 02FACTREL (gonadorelin hydrochloride) NDA 018123: product history(opens the source in a new tab) Drugs@FDA, U.S. Food and Drug Administration, 2026
  3. 03LUTREPULSE (gonadorelin acetate) NDA 019687: product history(opens the source in a new tab) Drugs@FDA, U.S. Food and Drug Administration, 2026
  4. 04Gonadorelin (CID 638793)(opens the source in a new tab) PubChem, NCBI, 2026
  5. 05Progonadoliberin-1 (human GnRH precursor) (P01148)(opens the source in a new tab) UniProt, 2026
  6. 06Hypophysial responses to continuous and intermittent delivery of hypothalamic gonadotropin-releasing hormone(opens the source in a new tab) Science, 1978
  7. 07Clinical review 15: Management of ovulatory disorders with pulsatile gonadotropin-releasing hormone(opens the source in a new tab) J Clin Endocrinol Metab, 1990
  8. 08Our products: LUTREPULSE / LUTRELEF (gonadorelin acetate)(opens the source in a new tab) Ferring Pharmaceuticals, 2026
  9. 09World Anti-Doping Code International Standard: Prohibited List 2026(opens the source in a new tab) World Anti-Doping Agency, 2025
  10. 10Gonadorelin 100 micrograms powder for solution for injection: Summary of Product Characteristics(opens the source in a new tab) electronic medicines compendium (emc), 2022
  11. 11Australian Register of Therapeutic Goods (ARTG)(opens the source in a new tab) Therapeutic Goods Administration
  12. 12Drug Product Database: Lutrepulse (DIN 02046202)(opens the source in a new tab) Health Canada, 2026
  1. In clinical trialsKisspeptinKISS1 receptor (GPR54) agonist, natural neuropeptide54 WADA banned
  2. ApprovedLeuprolideGnRH receptor agonist9 WADA banned
  3. ApprovedOxytocinOxytocin receptor agonist (posterior pituitary hormone)9

Educational information, not medical advice. Talk to a licensed clinician before starting, stopping or changing any medicine.