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

Advances and perspectives in the analytical technology for small peptide hormones analysis: A glimpse to gonadorelin
Journal of pharmaceutical and biomedical analysis · 2023 · PubMed
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
Reproductive performance of goats treated with free gonadorelin or nanoconjugated gonadorelin at estrus
Domestic animal endocrinology · 2020 · PubMed
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.

Fibroids (uterine myomatosis, leiomyomas)
BMJ clinical evidence · 2011 · PubMed

Fibroids may be asymptomatic or cause menorrhagia, pain, infertility, or recurrent pregnancy loss.; Risk factors include obesity, no children, and no long-term oral contraceptive use.; Fibroids tend to shrink or fibrose after menopause.; Interventions evaluated include medical treatments, preoperative medical therapies, and surgical options such as hysterectomy, myomectomy, and uterine artery embolisation.

Breast cancer (metastatic)
BMJ clinical evidence · 2010 · PubMed

Median survival from metastatic breast cancer is 12 months without treatment, but young people can survive up to 20 years.; First-line hormonal treatments include tamoxifen, ovarian ablation, progestins, and aromatase inhibitors.; First-line chemotherapy options include taxane-based combinations and non-taxane combinations, with or without monoclonal antibodies like trastuzumab.; Treatments for bone metastases include bisphosphonates, and for spinal or cerebral metastases include radiotherapy and surgery.

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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    Gonadorelin — Mechanism, Research & Data | Peptides API