Vial Guide
Approved drugGnRH (the natural pituitary signal)

Gonadorelin

GnRH, LHRH, gonadorelin acetate or hydrochloride; formerly Factrel and Lutrepulse in the US

Common dose
100–200 mcg, 2–3× weekly
Cycle
Continuous
Vial sizes
2, 5 mg
Typical draw
10 units2 mg with 2 mL, 100 mcg

The ten-amino-acid hormone the hypothalamus releases in pulses to tell the pituitary to make LH and FSH, which in turn drive the testes or ovaries. Given in pulses it stimulates; given continuously it does the opposite and shuts the pituitary down.

Evidence. A copy of the body’s own GnRH, approved for decades. Both US products are gone: Factrel (1982) and Lutrepulse (1989) are listed as discontinued. Approved products remain in Europe, including the Lutrelef pump for hypothalamic amenorrhea and a 100 mcg diagnostic injection in the UK. Pump therapy has good evidence in fertility; the popular use alongside testosterone therapy has no controlled trial.

Status

Approval
No gonadorelin medicine is approved and marketed in the US today. Factrel (gonadorelin hydrochloride, approved September 1982) and Lutrepulse (gonadorelin acetate, approved October 1989) are both listed as discontinued in FDA’s database, and the Factrel, Cystorelin, Fertagyl, OvaCyst and GonaBreed labels on DailyMed now are animal drugs, not human medicines. In Europe it is still authorized: Lutrelef for pump therapy (France, Austria, Netherlands), the nasal spray Kryptocur (Germany, Austria, Italy) and a 100 mcg diagnostic injection in the UK.
US compounding
Gonadorelin acetate sits in Category 1 on FDA’s 503B list for outsourcing facilities (updated March 21, 2025), marked as a component of an approved drug. It is in no category on the 503A list; pharmacies compound it under 503A because gonadorelin acetate has a USP monograph, not through the bulks list. Compounded gonadorelin is not an FDA-approved product.
Sport (WADA 2026)
Restricted in sportS2.2.1 testosterone-stimulating peptides: gonadotropin-releasing hormone (GnRH, gonadorelin) and its agonist analogues are named, and the whole subsection applies to males only. Banned at all times in males, not prohibited for female athletes.

Category 2 is FDA’s list of bulk substances that may present significant safety risks in compounding. The 503A bulks list adds substances that pharmacies may compound with. Advisory committee votes are advice; FDA makes the final decision. Sport status follows the WADA Prohibited List in force since January 1, 2026; athletes should confirm with their anti-doping organization. Checked October 5, 2026. Status of every compound.

How it works

Gonadorelin is identical to GnRH, the brain hormone that controls reproduction. It binds GnRH receptors on the pituitary gland at the base of the brain, which then makes and releases LH and FSH, the hormones that drive the testes and ovaries. Half of a dose is broken down in the blood within about 4 minutes, so each injection acts as a short pulse. In monkeys unable to make GnRH, hourly pulses restored LH and FSH release, but a steady infusion did not.

LabelBased on the product label.

Not known

Outside pump therapy, no trial has tested whether a few injections a week, each acting for minutes, keep the testes working during testosterone therapy.

Protocol

Label

UK gonadorelin SmPC

Diagnostic test: a single 100 mcg dose under the skin or into a vein, with LH measured before the dose and at 15, 30, 45, 60 and 120 minutes.

Trial

Mao 2016

Pulsatile pump: 10 mcg under the skin every 90 minutes, adjusted to keep LH and FSH in range; ovulation-induction practice uses about 5–20 mcg per pulse every 60–120 minutes.

Community

100–200 mcg under the skin, 2–3× weekly alongside testosterone therapy; some guides argue the short half-life makes daily dosing the minimum.

Frequency
2–3× per week (community); every 60–120 minutes by pump in approved use
Route
Subcutaneous injection (community); single injection under the skin or into a vein, pump infusion, or nasal spray in approved use
Timing
No set time of day. Guides keep the same days each week.
Cycle
Community use runs continuously for as long as testosterone therapy does. Pump therapy runs for months, until puberty, sperm or pregnancy targets are met.

Continuous, shown over 26 weeks

Common protocols

The ways Gonadorelin is most often run, each tagged with where it comes from.

Diagnostic test

Label
Dose
100 mcg
How often
Single dose
How long
One test, about 2 hours of blood draws

The approved use: it shows whether the pituitary can still respond. It says nothing about whether repeated dosing helps anything.

Draw 10 units2 mg + 2 mL

Pump, men

Trial
Dose
10 mcg per pulse
How often
Under the skin every 90 minutes, around the clock
How long
12–27 months in the published cohorts

For men whose own GnRH is missing. First sperm appeared at a median of 6 months, against 18 months on hCG plus hMG (Mao 2016).

Pump, ovulation

Trial
Dose
About 5–20 mcg per pulse
How often
Under the skin every 60–120 minutes
How long
One cycle at a time, repeated

Ovulation in 96% of cycles and one follicle only in 75%, with twins in 1.6% — fewer multiples than injected gonadotropins (Quaas 2022).

Alongside testosterone

Community
Dose
100–200 mcg
How often
2–3× weekly, sometimes daily
How long
Ongoing with testosterone therapy

Took the place of hCG for many users after hCG became a biologic in 2020 and could no longer be compounded. Never tested in a trial for this use.

Draw 10–20 units2 mg + 2 mL

Taking it

Where it goes

Under the skin of the belly or thigh, rotating sites (community). Approved use is one injection under the skin or into a vein, a pump that delivers small pulses, or a nasal spray sold in parts of Europe.

If you miss a dose

The approved label covers a single diagnostic dose, so it gives no missed-dose rule. Skip it and resume the usual schedule; don’t double up, since bunched doses push toward suppression rather than stimulation.

What to expect

  1. 15–45 minutes after a dose

    LH rises and peaks. This is the whole basis of the diagnostic test.

    Label
  2. Months 6–18 on a pump

    In men with no GnRH of their own, first sperm at a median of 6 months versus 18 months on hCG plus hMG; testicles grew faster too, though testosterone ran lower (8.3 vs 16.2 nmol/L).

    Trial
  3. Per cycle on a pump

    Ovulation in 96% of cycles, live birth in 65.9% of treatment courses in a 25-year single-center series of 66 women.

    Trial
  4. Weeks 2–3, community use

    Users describe testicular fullness returning. Whether LH, FSH and intratesticular testosterone actually hold up on a twice-weekly schedule has not been measured.

    Community

Side effects and what to do

Injection-site hardening, pain or swelling (label: rare for the single dose; common with pumps)

Rotate sites. In the pump studies, allergic redness at the site was the main complaint.

Headache, dizziness (label: rare)

Usually mild and brief. Tell the prescriber if it persists.

Nausea or belly discomfort (label: rare)

Reported more at higher amounts; splitting the dose is the usual community answer.

Hypersensitivity reactions, including bronchospasm (label: rare)

The label says to watch anyone who gets a repeat dose, especially into a vein.

Antibodies against the peptide (label: rare)

Reported with longer use. It can blunt the response over time.

Stop and get medical help

Get medical help for hives, swelling of the face or throat or trouble breathing, wheezing, or a hot, spreading red injection site with fever. A sudden severe headache with vomiting or a change in vision needs emergency care.

Who should avoid it

What its label rules out or warns about, most important first.

Pregnancy or breastfeeding
LabelRuled out in known or suspected pregnancy, and the UK label says not to give it to nursing mothers.
Allergy to gonadorelin
LabelRuled out. Rare allergic reactions, including bronchospasm (sudden narrowing of the airways), are listed; the label says to watch closely anyone given it again, especially into a vein.
A pituitary tumor (adenoma)
LabelNot recommended: the label warns that bleeding and tissue death in the gland (pituitary apoplexy) can occur with gonadorelin and similar drugs.
Women who could become pregnant
LabelA dose in the first half of the menstrual cycle can trigger early ovulation; the label advises steps to prevent an unwanted pregnancy.

Interactions

Only interactions stated on a product label or measured in a human study are listed.

Sex hormones and steroids (testosterone and other androgens, estrogens, progestogens, and glucocorticoids such as prednisolone)
LabelThe label says to run the gonadorelin test without drugs that directly affect the pituitary’s release of LH and FSH, which include these.
Drugs that raise prolactin, a pituitary hormone (phenothiazine antipsychotics such as chlorpromazine, and other dopamine blockers such as metoclopramide)
LabelThey can blunt the response to gonadorelin, the label says.
Spironolactone and methyldopa
LabelSpironolactone can briefly raise LH and FSH, and methyldopa can raise them slightly, the label says.
Birth control pills and digoxin
LabelBoth can lower LH and FSH, the label says.

Label: a product label rules it out, warns about it or lists the interaction. This isn’t a complete list: a pharmacist or doctor can check a specific medicine or condition.

Tracking and pairing

Worth tracking

  • LH and FSH
  • Total testosterone (men)
  • Estradiol
  • Semen analysis if fertility matters

Often paired with

  • hCG

    The drug it is used in place of. hCG acts directly on the testes, gonadorelin one step earlier at the pituitary. Some guides run both; the combination has not been tested.

  • Kisspeptin-10

    Acts one step earlier still, on the neurons that release GnRH. Sold as a fertility pairing, with no trial behind the combination.

Human studies

4 key published human studies, with how many people took part. Animal studies aren’t listed here.

  1. 2017202 people

    First sperm at a median of 6 months on the pump versus 18 months on hCG/hMG (p<0.001); testicles reached each size target sooner, while testosterone ran lower (8.3 vs 16.2 nmol/L).

    Design
    Retrospective cohort in men with congenital hypogonadotropic hypogonadism, randomization not described
    Dose
    Pulsatile GnRH 10 mcg under the skin every 90 minutes by pump (20 men) versus hCG plus hMG (182 men)
    Length
    At least 12 months; mean follow-up 15.6 months on the pump

    Mao et al., Asian J Androl 2017, PMID 28051040

  2. 202266 people

    Ovulation in 96% of cycles, a single follicle in 75%, clinical pregnancy in 74.4% and live birth in 65.9% per course, with one twin pregnancy (1.6%).

    Design
    Single-center retrospective cohort of women with functional hypothalamic amenorrhea, 1996 to 2020 (82 treatment courses, 212 cycles)
    Dose
    Pulsatile GnRH pump under the skin, pulses about every 90 minutes
    Length
    25 years of practice; one or more treatment courses per patient

    Quaas et al., J Assist Reprod Genet 2022, PMID 36378460

  3. 2020420 people

    GnRH gave earlier sperm appearance (5.3 months sooner, p=0.004) and larger testicles, with no significant difference in sperm detection, sperm count or pregnancy rate; allergic reactions were commoner on GnRH, gynecomastia and acne on gonadotropins.

    Design
    Systematic review and meta-analysis of eight articles from seven comparative studies
    Dose
    Pulsatile GnRH by pump versus hCG plus hMG
    Length
    Varies by study

    Wei et al., World J Mens Health 2020, PMID 32777865

  4. 201828 people

    Sperm appeared at a median of 6 months on the pump versus 14 months on hCG/hMG (p=0.01); 90% versus 83.3% produced sperm. Allergic redness at the infusion site was the pump’s common side effect.

    Design
    Prospective comparison in azoospermic men with congenital hypogonadotropic hypogonadism, not randomized (patients chose their treatment)
    Dose
    Pulsatile gonadorelin pump, 10 mcg every 90 minutes under the skin (10 men) versus cyclical hCG/hMG (18 men)
    Length
    Up to 24 months

    Zhang et al., Am J Mens Health 2018, PMID 30569789

All human studies on Vial Guide

Limits of the evidence

The UK label covers only a single diagnostic dose. Treatment evidence comes from pump studies in people whose brains make too little GnRH, mostly non-randomized, plus a pooled analysis of 7 comparative studies in 420 men. No controlled trial has tested a few injections a week, use alongside testosterone therapy, or the long-term safety of repeated injections.

Mixing your vial

VialWaterCommon doseDrawStrengthAction
2 mg2 mL100 mcg10 units (0.10 mL)1 mg/mL
5 mg2.5 mL100 mcg5 units (0.05 mL)2 mg/mL

Bacteriostatic water. A 2 mg vial in 2 mL gives 1 mg/mL, so 100 mcg is 10 units on a U-100 syringe. The approved 100 mcg diagnostic vial is different: it is mixed with 1 mL of sterile water, used at once, and any remainder discarded.

Dose chart

Syringe units for common doses at different water volumes. Select a cell to open it in the calculator.

DoseWater added
1 mL2 mL3 mL
50 mcg
60 mcg
75 mcg
100 mcg
150 mcg
200 mcg

U-100 insulin syringe: 100 units is 1 mL. Draws over 100 units show in mL. Faded values are under 2 units, which is hard to measure. Check that your vial holds the larger volumes.

Datasheet

Half-life
about 4 minutes LabelBroken down in plasma and cleared in the urine after injection.
Type
Peptide, 10 amino acids
Molecular weight
1,182.3 g/mol
Formula
C55H75N17O13
Sequence
(pGlu)-HWSYGLRPG-NH2
Storage before use
Approved vial: store below 25 °C. Research powder: freezer for long storage, fridge for short periods (community practice).
After mixing or opening
Approved vial: mix immediately before use, refrigerate and use within 1 day; discard the rest. Mixed research vials: 2–8 °C, about 4 weeks (community practice).
  • Half-life: UK gonadorelin 100 micrograms summary of product characteristics, section 5.2 (revised 30 August 2022)
  • Molecule: PubChem CID 638793 (gonadorelin free base, UNII 9O7312W37G, CAS 33515-09-2). The acetate salt is 1,242.3 and the hydrochloride 1,218.7.
  • Storage: Label UK gonadorelin 100 micrograms summary of product characteristics, sections 6.3, 6.4 and 6.6 (revised 30 August 2022)

Every compound side by side: the half-life chart and the storage chart.

Cautions

  • Pulses stimulate; steady exposure suppresses. Continuous or too-frequent dosing desensitizes the pituitary and lowers LH and FSH instead of raising them.
  • The half-life is about 4 minutes, so a once-weekly injection is a single pulse in a week and does close to nothing.
  • Using it to protect testicular function during testosterone therapy is an extrapolation from pump studies in men who make no GnRH at all. No controlled trial has tested it.
  • The label warns against use with a pituitary adenoma, because bleeding into the gland (pituitary apoplexy) has been reported with GnRH and its analogues.
  • Not for use in pregnancy; a dose in the first half of a cycle can trigger early ovulation.

Questions

What is gonadorelin?

The ten-amino-acid hormone the hypothalamus releases in pulses to tell the pituitary to make LH and FSH, which in turn drive the testes or ovaries. Given in pulses it stimulates; given continuously it does the opposite and shuts the pituitary down.

How does gonadorelin work?

Gonadorelin is identical to GnRH, the brain hormone that controls reproduction. It binds GnRH receptors on the pituitary gland at the base of the brain, which then makes and releases LH and FSH, the hormones that drive the testes and ovaries. Half of a dose is broken down in the blood within about 4 minutes, so each injection acts as a short pulse. In monkeys unable to make GnRH, hourly pulses restored LH and FSH release, but a steady infusion did not. Outside pump therapy, no trial has tested whether a few injections a week, each acting for minutes, keep the testes working during testosterone therapy.

Is gonadorelin FDA-approved?

No gonadorelin medicine is approved and marketed in the US today. Factrel (gonadorelin hydrochloride, approved September 1982) and Lutrepulse (gonadorelin acetate, approved October 1989) are both listed as discontinued in FDA’s database, and the Factrel, Cystorelin, Fertagyl, OvaCyst and GonaBreed labels on DailyMed now are animal drugs, not human medicines. In Europe it is still authorized: Lutrelef for pump therapy (France, Austria, Netherlands), the nasal spray Kryptocur (Germany, Austria, Italy) and a 100 mcg diagnostic injection in the UK. Gonadorelin acetate sits in Category 1 on FDA’s 503B list for outsourcing facilities (updated March 21, 2025), marked as a component of an approved drug. It is in no category on the 503A list; pharmacies compound it under 503A because gonadorelin acetate has a USP monograph, not through the bulks list. Compounded gonadorelin is not an FDA-approved product.

What is the usual gonadorelin dose?

From the label (UK gonadorelin SmPC): Diagnostic test: a single 100 mcg dose under the skin or into a vein, with LH measured before the dose and at 15, 30, 45, 60 and 120 minutes. From human studies (Mao 2016): Pulsatile pump: 10 mcg under the skin every 90 minutes, adjusted to keep LH and FSH in range; ovulation-induction practice uses about 5–20 mcg per pulse every 60–120 minutes. These are the amounts sources reference, not recommendations.

How much water do I mix gonadorelin with?

There’s no single right amount, because the water only sets the strength. With 2 mL of bacteriostatic water in a 2 mg vial, the strength is 1 mg/mL, so 100 mcg is 10 units on a U-100 insulin syringe. More water makes small doses easier to measure. The dose chart above shows other volumes.

Who should avoid gonadorelin?

Pregnancy or breastfeeding: Ruled out in known or suspected pregnancy, and the UK label says not to give it to nursing mothers. Allergy to gonadorelin: Ruled out. Rare allergic reactions, including bronchospasm (sudden narrowing of the airways), are listed; the label says to watch closely anyone given it again, especially into a vein. A pituitary tumor (adenoma): Not recommended: the label warns that bleeding and tissue death in the gland (pituitary apoplexy) can occur with gonadorelin and similar drugs. The “Who should avoid it” section lists 1 more group and 4 interactions.

What is the half-life of gonadorelin?

About 4 minutes, according to the prescribing information. Broken down in plasma and cleared in the urine after injection.

How should gonadorelin be stored?

Approved vial: store below 25 °C. Research powder: freezer for long storage, fridge for short periods (community practice). Approved vial: mix immediately before use, refrigerate and use within 1 day; discard the rest. Mixed research vials: 2–8 °C, about 4 weeks (community practice).

Is gonadorelin banned in sport?

In some cases. S2.2.1 testosterone-stimulating peptides: gonadotropin-releasing hormone (GnRH, gonadorelin) and its agonist analogues are named, and the whole subsection applies to males only. Banned at all times in males, not prohibited for female athletes.

Has gonadorelin been studied in people?

Yes. The human studies section lists 4 published studies. The largest, from 2020, included 420 people. GnRH gave earlier sperm appearance (5.3 months sooner, p=0.004) and larger testicles, with no significant difference in sperm detection, sperm count or pregnancy rate; allergic reactions were commoner on GnRH, gynecomastia and acne on gonadotropins.

Sources

  • Gonadorelin 100 micrograms powder for solution for injection (HRF), UK summary of product characteristics, revised 30 August 2022
  • FDA Drugs@FDA records for Factrel (NDA 018123, approved 1982) and Lutrepulse (NDA 019687, approved 1989), both discontinued
  • Mao et al., pulsatile GnRH versus combined gonadotropin therapy in congenital hypogonadotropic hypogonadism (Asian J Androl 2017) PMID 28051040
  • Quaas et al., pulsatile GnRH in functional hypothalamic amenorrhea, 25-year cohort (J Assist Reprod Genet 2022) PMID 36378460
  • FDA, bulk drug substances nominated for use in compounding under section 503B, categories 1 to 3 (updated March 21, 2025)

For the protocol details

  • Wei et al., pulsatile GnRH versus gonadotropin therapy, systematic review and meta-analysis (World J Mens Health 2020) PMID 32777865

For how it works, who should avoid it and the limits of the evidence

  • Gonadorelin 100 micrograms powder for solution for injection (HRF), UK summary of product characteristics, sections 4.3–4.6, 5.1 and 5.2 (rev. August 30, 2022)
  • Belchetz et al., pulsed versus continuous GnRH in monkeys (Science 1978) PMID 100883

Doses tagged Community come from public dosing guides and user reports, checked against at least two of them. Those sites aren’t named here because many of them sell peptides or earn commissions on them.