For laboratory and research use only. Not for human consumption.
Hormonal

Gonadorelin

Also known as: GnRH, LHRH, Factrel (discontinued)

Clinical Trials
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Key Facts: Gonadorelin

Category
Hormonal
FDA Status
Not FDA Approved
Clinical Status
Previously FDA approved (Factrel, diagnostic) - brand discontinued; no FDA-approved gonadorelin product currently marketed in the US. Currently sold in the US mainly through compounding pharmacies. WADA: prohibited at all times in male athletes (S2, GnRH and its analogues).
Banned in Sport (WADA)
Prohibited at all times under WADA S2 (testosterone-stimulating peptides in males: GnRH/gonadorelin is named). Males only; not prohibited for females.
Administration
IV, subcutaneous, or pulsatile pump
Typical Dose
100-500 mcg 2-3x weekly
Frequency
2-3x weekly
Duration
Single dose (diagnostic) or ongoing (therapeutic)
Also Known As
GnRH, LHRH, Factrel (discontinued)

How does Gonadorelin work?

Gonadorelin binds the GnRH receptor, a seven-transmembrane G-protein-coupled receptor on the gonadotroph cells of the anterior pituitary. Activation drives phospholipase C, which mobilizes calcium and protein kinase C, prompting the synthesis and pulsed release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Those gonadotropins then act on the testes or ovaries to drive testosterone, sperm, estrogen, and egg development. The crucial detail is the delivery pattern: the body releases GnRH in pulses roughly every 60 to 120 minutes, and gonadorelin only stimulates the gonadal axis when given in that pulsatile way. Continuous or high steady-state exposure desensitizes and downregulates the receptor, which paradoxically suppresses LH and FSH, the same trick that GnRH agonist drugs use deliberately.

What does the research show?

Gonadorelin itself is an old, well-understood molecule rather than a frontier research peptide, and its diagnostic use (the GnRH stimulation test to probe pituitary-gonadal function) is established. Pulsatile gonadorelin delivered by pump has documented use in hypogonadotropic hypogonadism, delayed puberty, and fertility induction. A 2021 meta-analysis (7 studies, 420 men with congenital hypogonadotropic hypogonadism) found pump GnRH started sperm production about 5.3 months earlier than gonadotropin injections, with no significant difference in sperm concentration or pregnancy rates. None of those men were on testosterone, so it does not test the TRT add-on use. Its very short half-life means real clinical use required pumps or frequent dosing, which is one reason longer-acting drugs largely replaced it. The popular off-label use, injecting gonadorelin a few times a week alongside testosterone to preserve testicular size and fertility, rests mostly on its known mechanism and anecdotal experience rather than randomized trials showing it matches HCG. So the underlying biology is rock solid; the specific TRT-adjunct claims are reasonable mechanistically but not trial-backed.

Trial Progress:Preclinical
Pre
I
II
III
IV
FDA

What doses have been studied?

Human Trials·Previously FDA approved (Factrel, now discontinued). Human data in hypogonadism and fertility; TRT add-on use not trial-tested.

Typical Dosingⓘ

Community experience

Common Dose

100-500 mcg 2-3x weekly

Range

50-500 mcg per dose

Frequency

2-3x weekly

Native-sequence GnRH (not a modified analog), used off-label to maintain natural testosterone and testicular function during testosterone therapy, often discussed alongside HCG protocols. Not trial-tested for this use.

Research Dosingⓘ

Scientific studies

Varies by indication

Doses from Studies

100 mcg IV/SC for diagnostic testing

FDA Approved Labeling - Prescribed dose ↗

Pulsatile: varies by protocol

FDA Approved Labeling - Prescribed dose ↗

Duration

Single dose (diagnostic) or ongoing (therapeutic)

Administration

IV, subcutaneous, or pulsatile pump

When and how is Gonadorelin taken?

Best Time to Take

Morning or as clinically directed

As prescribed, often pulsatile

Food Recommendation

With or without food

Why This Timing?

Native-sequence GnRH used for hormone stimulation. Pulsed dosing stimulates LH and FSH; continuous exposure suppresses them. Timing depends on the protocol.

What are the side effects of Gonadorelin?

Not everyone experiences these effects. Individual responses vary based on dosage, duration, and personal factors.

  • ●Injection site reactions
  • ●Headache
  • ●Flushing
  • ●Nausea
  • ●Allergic reactions (reported with pump therapy)
  • ●Risk of multiple births (fertility use)
  • ●May worsen hormone-dependent cancers

References

Research This Peptide Further

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Frequently Asked Questions

What does Gonadorelin do?

Gonadorelin is a synthetic copy of natural GnRH (gonadotropin-releasing hormone), a 10-amino-acid peptide (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) that tells the pituitary to release LH and FSH. It was once FDA-approved (Factrel) for testing pituitary function, but that brand is discontinued and no approved gonadorelin product is marketed in the US today. In the peptide world it is mostly used off-label to keep the testes working during testosterone replacement, and the catch is that timing matters enormously: pulse it and you stimulate, give it continuously and you shut the system down.

How does Gonadorelin work?

Gonadorelin binds the GnRH receptor, a seven-transmembrane G-protein-coupled receptor on the gonadotroph cells of the anterior pituitary. Activation drives phospholipase C, which mobilizes calcium and protein kinase C, prompting the synthesis and pulsed release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Those gonadotropins then act on the testes or ovaries to drive testosterone, sperm, estrogen, and egg development. The crucial detail is the delivery pattern: the body releases GnRH in pulses roughly every 60 to 120 minutes, and gonadorelin only stimulates the gonadal axis when given in that pulsatile way. Continuous or high steady-state exposure desensitizes and downregulates the receptor, which paradoxically suppresses LH and FSH, the same trick that GnRH agonist drugs use deliberately.

Is Gonadorelin FDA approved?

No, Gonadorelin is not currently FDA approved. Current status: Previously FDA approved (Factrel, diagnostic) - brand discontinued; no FDA-approved gonadorelin product currently marketed in the US. Currently sold in the US mainly through compounding pharmacies. WADA: prohibited at all times in male athletes (S2, GnRH and its analogues).

Is Gonadorelin banned in sport?

Prohibited at all times under WADA S2 (testosterone-stimulating peptides in males: GnRH/gonadorelin is named). Males only; not prohibited for females.

What are the side effects of Gonadorelin?

Reported side effects include: Injection site reactions, Headache, Flushing, Nausea, Allergic reactions (reported with pump therapy). Individual responses vary based on dosage, duration, and personal health factors.

What is the typical dose of Gonadorelin?

Community-reported common dose: 100-500 mcg 2-3x weekly (2-3x weekly). Range: 50-500 mcg per dose. Administration: IV, subcutaneous, or pulsatile pump. Community-reported doses. Not medical advice. Consult healthcare provider.

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Macimorelin (brand name Macrilen) is an orally active ghrelin receptor agonist used as a diagnostic test, not a treatment. You drink a single dose, then doctors measure how much growth hormone the pituitary releases to diagnose adult growth hormone deficiency. It was FDA approved in December 2017 as the first oral diagnostic agent for that condition.

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