Gonadorelin
Also known as: GnRH, LHRH, Factrel (discontinued)
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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)
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.
What doses have been studied?
Typical Dosingⓘ
Community experience
100-500 mcg 2-3x weekly
50-500 mcg per dose
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
Pulsatile: varies by protocol
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
- https://pubchem.ncbi.nlm.nih.gov/compound/Gonadorelin
- https://en.wikipedia.org/wiki/Gonadotropin-releasing_hormone
- https://www.bachem.com/peptide-api-drug-substance-manufacturer/gonadorelin/
- https://pubmed.ncbi.nlm.nih.gov/32777865/
- https://www.drugs.com/mtm/gonadorelin.html
- https://www.wada-ama.org/en/prohibited-list
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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.
Related Peptides
Peptides commonly compared with Gonadorelin or used in similar applications.
Kisspeptin
Clinical TrialsKisspeptin is the master switch that tells your brain to start reproduction. It is a family of peptides (the full length is kisspeptin-54, with shorter active fragments KP-14, KP-13, and KP-10) made from the KISS1 gene, and it acts as the upstream trigger for the entire reproductive hormone cascade. It is not an approved drug, but it has been tested in real human trials for fertility, hypothalamic amenorrhea, and male hypogonadism, with promising early results.
HormonalLeuprolide
FDALeuprolide (brand name Lupron) is a synthetic GnRH agonist, a modified peptide far more potent than natural GnRH, and it is FDA-approved for advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. The clever part is counterintuitive: it works by overstimulating the GnRH system so hard that the pituitary shuts down sex hormone production. It is a real, long-established prescription drug (first US approval 1985), not a research peptide, and it carries meaningful side effects from the low-hormone state it creates.
HormonalOctreotide
FDAOctreotide is a synthetic eight-amino-acid mimic of the natural hormone somatostatin, the body's main 'off switch' for hormone secretion. It shuts down excess growth hormone, so it is a frontline FDA-approved drug for acromegaly, and it also tames the flushing and diarrhea of hormone-secreting carcinoid and other neuroendocrine tumors. This is real, approved medicine with decades of clinical data behind it, sold as Sandostatin (injectable, since 1988), Sandostatin LAR (monthly depot), and Mycapssa (oral capsule, approved 2020).
HormonalLanreotide
FDALanreotide (development code BIM-23014) is an eight-amino-acid somatostatin analog, a close cousin of octreotide, given as a long-acting deep-injection gel (Somatuline Depot/Autogel) usually once a month. The FDA approved it for acromegaly in 2007, for gastroenteropancreatic neuroendocrine tumors in 2014, and for carcinoid syndrome in 2017. Generic versions now exist alongside Ipsen's Somatuline Depot. It is established prescription medicine, not an experimental compound.
HormonalPegvisomant
FDAPegvisomant (brand name Somavert) flips the usual acromegaly strategy on its head: instead of telling the tumor to make less growth hormone, it blocks growth hormone's receptor on target tissues directly. It is a PEGylated, genetically modified version of human growth hormone that acts as a receptor antagonist, FDA-approved in 2003 for acromegaly patients who do not respond well to surgery or other drugs. It is the single most effective option for normalizing IGF-1, which is why it is a key second-line therapy.
HormonalMacimorelin
FDAMacimorelin (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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