Gonadorelin
peptide · headlineFDA-approvedActs as a GnRH receptor agonist on the anterior pituitary
Overview
Gonadorelin is a synthetic gonadotropin-releasing hormone (GnRH) used for diagnostic and therapeutic purposes in reproductive and endocrine medicine. It stimulates the anterior pituitary to release LH and FSH and is used in fertility restoration, hormone replacement, and hypothalamic amenorrhea treatment.
How it works
- Acts as a GnRH receptor agonist on the anterior pituitary
- Induces secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH)
- Requires pulsatile administration to mimic physiological GnRH signaling
- Used in evaluating pituitary response and stimulating gonadal steroid production
Dosing
Standard diagnostic dose: 0.1 mg IV as a single bolus. Therapeutic pulsatile use: 5–20 mcg IV or SubQ every 90–120 minutes for HRT or fertility.
Caution: Typical clinical research doses are 50–100 μg per injection. Gonadorelin is only approved for use in select diagnostic procedures.
Cycling
- For diagnostic use: 0.1 mg IV as a single bolus. For therapeutic use: administered every 90–120 min in pulsatile infusion pumps over 7–14 days.
Side effects
- Common
- Transient headache or flushing shortly after injection
Stacking & combinations
- With
GHK-Cu
- Benefit
Used with HCG or Kisspeptin-10 in fertility and HPTA restoration protocols
Lifestyle support
- Diet
Balanced nutrition. Avoid excessive alcohol.
- Sleep
Adequate sleep (7–9 hours) supports hormonal rhythms. Stress management.
- Timing
Consistent injection schedule to support hormonal rhythms.
- Exercise
Resistance training.
Research studies
Studies summarized for educational purposes only. Inclusion does not imply human use; referenced research was conducted in vitro, in animal models, or in regulated clinical trials.
Induction of puberty in men by long-term pulsatile administration of low-dose gonadotropin-releasing hormone
Hoffman AR, Crowley WF Jr New England Journal of Medicine, 1982 View source ↗
Six men with idiopathic hypogonadotropic hypogonadism received low-dose GnRH delivered subcutaneously in episodic (pulsatile) pulses via a portable infusion pump, mimicking physiologic hypothalamic secretion. Serum gonadotropins normalized within one week and rose above normal by two weeks, and testosterone increased from a markedly suppressed baseline (77 +/- 13 ng/dL) into the adult range. Four patients showed testicular growth and three achieved spermatogenesis by 43 weeks, demonstrating that pulsatile, rather than continuous, GnRH delivery reverses the pituitary-gonadal defect.
In men whose bodies never triggered puberty because the brain fails to release the hormone that starts it, doctors used a small pump to deliver GnRH in tiny timed bursts like the body normally would. Within weeks the men's hormone levels became normal and testosterone climbed to adult levels. Several developed larger testes and began producing sperm, showing this pump approach can jump-start delayed puberty and fertility.
Induction of puberty by pulsatile gonadotropin releasing hormone
Stanhope R, Brook CG, Pringle PJ, Adams J, Jacobs HS Lancet, 1987 View source ↗
Fifteen girls and seventeen boys with delayed or arrested puberty were treated with subcutaneous pulsatile GnRH at 90-minute intervals (1-2 micrograms/pulse for girls, 2-4 micrograms/pulse for boys). Clinical features, growth acceleration, endocrine profiles, and ovarian ultrasound morphology reproduced those of normal spontaneous puberty. Measurement of spontaneous gonadotropin pulsatility after treatment withdrawal distinguished 20 patients with hypogonadotropic hypogonadism from 12 with constitutional delay of growth and puberty, confirming that normal puberty is GnRH-dependent.
Children with delayed puberty were given GnRH through a pump that released a small dose every 90 minutes, matching the body's natural rhythm. Their growth, hormone changes, and physical development matched what normally happens in puberty. Stopping the treatment and rechecking hormone patterns also helped doctors tell apart kids who were simply late bloomers from those with a permanent hormone deficiency.
Role of Gonadotropin-releasing Hormone Stimulation Test in Diagnosing Gonadotropin Deficiency in Both Males and Females with Delayed Puberty
Sun QH, Zheng Y, Zhang XL, Mu YM Chinese Medical Journal (English), 2015 View source ↗
Investigators compared GnRH (gonadorelin) stimulation test responses across 91 patients with idiopathic hypogonadotropic hypogonadism, 27 with constitutional delay of growth and puberty, 6 prepubertal children, and 20 pubertal adults to derive diagnostic cut-offs. In males, a serum basal LH <0.6 IU/L or peak LH <9.74 IU/L yielded moderate sensitivity (73.8%/80.0%) and specificity (90.9%/86.4%); in females, basal LH <0.85 IU/L or basal FSH <2.43 IU/L gave sensitivities of 80.0%/100.0% and specificities of 75.0%/50.0%. The authors concluded the test alone adequately differentiates hypogonadotropic hypogonadism from constitutional delay in males, with basal or peak LH being the most useful predictor.
Doctors gave a GnRH injection and measured how much the pituitary gland released the hormones LH and FSH, then compared results between patients with a true hormone deficiency and those who were just late to enter puberty. They identified LH threshold levels that reliably separated the two groups, especially in boys. This helps clinicians decide whether a teenager with delayed puberty needs treatment or will develop normally on their own.
Verified citations
2 · PubMed-checked- GnRH agonists: gonadorelin, leuprolide and nafarelin.reviewPMID 1835275 ↗
- Effect of gonadorelin (GnRH) products on pregnancy rates in postpartum dairy cows.clinicalPMID 25979657 ↗
Reconstitution calculator
Intravenous (IV)= 0.02 mL on a U-100 insulin syringe
Assumes a U-100 insulin syringe (100 units = 1 mL). This is a preparation aid, not a protocol — dose and route are the prescriber's decision. Refrigerate at 2–8 °C (35.6–46.4 °F); use within 4 weeks and avoid freeze–thaw
Chemistry & PK
- Sequence
- Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
- Half Life
- 2–4 minutes
- Degradation
- Rapid degradation by plasma proteases and renal clearance
- Molecular Weight
- 1182
- Molecular Formula
- C55H75N17O13
- Tissue Specificity
- Targets anterior pituitary GnRH receptors
Bioavailability
- Oral
- Very poor; not viable orally
- Subq
- Low due to enzymatic degradation; typically not used subcutaneously
Storage & handling
- Lyophilized
store at −20 °C (−4 °F); after reconstitution, refrigerate at 2–8 °C (35.6–46.4 °F); avoid freeze–thaw cycles
- Reconstituted
Refrigerate at 2–8 °C (35.6–46.4 °F); use within 4 weeks and avoid freeze–thaw
Legal / compounding
- EU
- Approved
- FDA
- Approved
- Canada
- Approved
- Australia
- Approved
Legal status is a hard gate: non-compoundable or delisted agents cannot be filled and are blocked from protocol export. Keep 503A status current.