Gonadorelin

approved

Also known as: GnRH, LHRH, Factrel

**Mechanism of Action** Gonadorelin is a synthetic decapeptide identical to endogenous gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors on anterior pituitary gonadotroph cells, stimulating the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This action is dose- and frequency-dependent: pulsatile administration mimics physiological GnRH release, promoting gonadal steroidogenesis and gametogenesis, while continuous exposure paradoxically suppresses gonadotropin secretion via receptor desensitization. **Key Research Findings** Clinical studies confirm that intravenous or subcutaneous gonadorelin reliably induces LH/FSH peaks within 30 minutes, making it a standard diagnostic tool for hypothalamic-pituitary-gonadal axis integrity (e.g., in delayed puberty or hypogonadotropic hypogonadism). Research also demonstrates its efficacy in controlled ovarian stimulation protocols for assisted reproduction, though pulsatile delivery systems are required to avoid downregulation. Long-term continuous use is not recommended due to desensitization effects. **Clinical Relevance** Gonadorelin is FDA-approved for diagnostic testing of pituitary function and for induction of ovulation in select anovulatory women with intact pituitary function. Its therapeutic use is limited by short half-life (~4 minutes) and need for precise pulsatile administration. Off-label applications include male hypogonadism and cryptorchidism, though newer GnRH analogs with longer half-lives are often preferred. For research purposes only — not medical advice.

Key data

Category
Hormonal & Endocrine
Molecular weight
1182.3 g/mol
Molecular formula
C55H75N17O13
CAS number
33515-09-2
Administration
subcutaneous, intravenous
Research status
approved
References
295
Tags
gnrh, approved, reproductive

Research & studies

Are We Considering All the Potential Drug-Drug Interactions in Women's Reproductive Health? A Predictive Model Approach
Pharmaceutics · 2025 · PubMed

The model identified 2991 new DDIs involving 192 drugs used in female reproductive conditions and other unrelated treatments.; Most new DDIs involved estradiol, acetaminophen, bupivacaine, risperidone, and follitropin, with follitropin having the highest discovery rate at 42%.; Predicted 12 DDIs between oral contraceptives and HIV drugs that could compromise efficacy.; Among new DDIs, 23 were expected to improve therapies and 11 to cause harmful effects.

Advances and perspectives in the analytical technology for small peptide hormones analysis: A glimpse to gonadorelin
Journal of pharmaceutical and biomedical analysis · 2023 · PubMed

Bioanalytical methods have evolved toward simpler, on-site techniques with reduced time and costs.; Affinity reagent production has advanced from natural receptors to biomimetic, animal-free options like aptamers and MIPs.; Peptide hormone analysis remains challenging in biomedical, pharmaceutical, and anti-doping contexts.; Gonadorelin is highlighted as a neuropeptide misused in doping, driving interest in its detection.

A biomimetic enzyme-linked immunosorbent assay (BELISA) for the analysis of gonadorelin by using molecularly imprinted polymer-coated microplates
Analytical and bioanalytical chemistry · 2022 · PubMed

A detection limit of 277 pmol L-1 for gonadorelin was achieved.; Reproducibility was good with average CV% of 4.07% in standard solutions and 5.24% in urine samples.; The assay showed adequate selectivity against non-specific control peptides.; Results were successfully validated by mass spectrometry, the reference anti-doping platform.

Effect of gonadotropin-releasing hormone administered at the time of artificial insemination for cows detected in estrus by conventional estrus detection or an automated activity-monitoring system
Journal of dairy science · 2022 · PubMed

GnRH at AI did not improve ovulation rate, plasma progesterone 7 days post-AI, or pregnancy per AI in cows detected by traditional estrus detection or AAM.; No treatment effects were observed for pregnancy at P1 (32-45 days) or P2 (60-115 days) in either experiment.; High-activity cows in the AAM system had greater pregnancy per AI and lower pregnancy loss compared to low-activity cows, with no interaction with GnRH treatment.; The study does not support routine use of GnRH at estrus detection to enhance reproductive outcomes.

Reproductive performance of goats treated with free gonadorelin or nanoconjugated gonadorelin at estrus
Domestic animal endocrinology · 2020 · PubMed

Both GnRH and NGnRH increased corpora lutea number and twinning rate compared to control.; GnRH treatment increased serum estradiol and progesterone concentrations more than NGnRH and control.; NGnRH achieved similar fertility and prolificacy to GnRH at a quarter of the dose.; Both treatments reduced estrus duration and pregnancy losses compared to control.

Endometriosis: the effects of dienogest
BMJ clinical evidence · 2015 · PubMed

Dienogest was compared to placebo, no treatment, gonadorelin analogues, combined oral contraceptives, and other progestogens.; The review included five studies and used GRADE to assess evidence quality.; Ectopic endometrial tissue occurs in 2-6% of reproductive-age women and up to 60% of those with dysmenorrhoea.; Symptoms may not correlate with laparoscopic findings.

Menorrhagia
BMJ clinical evidence · 2012 · PubMed

Menorrhagia limits normal activities and causes anaemia in two-thirds of women with objective blood loss ≥80 mL per cycle.; Prostaglandin disorders may be linked to idiopathic menorrhagia and heavy bleeding from fibroids, adenomyosis, or IUDs.; Fibroids found in 10% of women with menorrhagia overall, 40% with severe menorrhagia; half of hysterectomies for menorrhagia reveal a normal uterus.; Review included 39 systematic reviews, RCTs, or observational studies with GRADE evaluation for interventions.

Breast pain
BMJ clinical evidence · 2011 · PubMed

Cyclical breast pain resolves spontaneously in 20-30% of women but recurs in 60%.; Non-cyclical pain responds poorly to treatment but resolves spontaneously in half of women.; The review assessed 18 interventions including antibiotics, NSAIDs, and hormonal treatments.

Frequently asked questions

What is Gonadorelin?

**Mechanism of Action** Gonadorelin is a synthetic decapeptide identical to endogenous gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors on anterior pituitary gonadotroph cells, stimulating the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This actio

How does Gonadorelin work?

Synthetic GnRH decapeptide that stimulates pituitary LH and FSH release; used diagnostically and to support gonadal function.

What is the research status of Gonadorelin?

Gonadorelin is currently classified as approved, with 295 research references on record. This is for research purposes only and is not medical advice.

What is the molecular weight of Gonadorelin?

Gonadorelin has a molecular weight of approximately 1182.3 g/mol (formula C55H75N17O13).

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