Synthetic gonadotropin-releasing hormone (GnRH/LHRH); decapeptide identical to endogenous GnRH; GnRH receptor agonist
Gonadorelin
Approvedaka GnRH, LHRH, Factrel, Lutrepulse
Gonadorelin is the decapeptide identical to natural GnRH. It was approved and marketed as a diagnostic agent (for example, Factrel) to assess pituitary gonadotropin reserve, and, delivered in a pulsatile fashion (for example, Lutrepulse), to induce ovulation in women with hypothalamic amenorrhea. Many branded gonadorelin products have since been discontinued in some markets, and it is now frequently supplied through pharmacy compounding; approval status differs across regions.
Mechanism
In plain terms, gonadorelin is a copy of the brain hormone that tells the pituitary to release the hormones controlling the ovaries and testes. Technically, it is a decapeptide agonist of the GnRH receptor on pituitary gonadotrophs; when delivered in physiological pulses it stimulates secretion of luteinising hormone (LH) and follicle-stimulating hormone (FSH), whereas continuous (non-pulsatile) exposure paradoxically desensitises the receptor and suppresses gonadotropins, the principle exploited by long-acting GnRH analogues.
Regulatory Status by Region
- United States (FDA)Has a history of FDA approval: gonadorelin hydrochloride (Factrel) for evaluating pituitary gonadotropic function and gonadorelin acetate (Lutrepulse) for pulsatile induction of ovulation in hypothalamic amenorrhea. Several branded products have since been discontinued in the US (not for safety reasons), and gonadorelin is now commonly supplied via pharmacy compounding.
- Australia (TGA)Gonadorelin (native GnRH) has historically been used in Australia for diagnostic and fertility indications; whether a gonadorelin-specific product is currently on the ARTG is unclear. Related GnRH analogues such as leuprorelin and goserelin are registered.
- European Union (EMA)Gonadorelin has been marketed in European countries through national approvals (as a diagnostic agent and for pulsatile fertility therapy) rather than through a single centralised EMA authorisation.
- WADAProhibited in males under Section S2: WADA lists gonadotropin-releasing hormone (GnRH) agonists among luteinising-hormone releasing factors, and gonadorelin is explicitly named; it is not prohibited in females.
Key Studies
- Structure of the porcine LH- and FSH-releasing hormone (the amino acid sequence of GnRH/LHRH) (opens in a new tab) (Matsuo H, Baba Y, Nair RM, Arimura A, Schally AV. Biochem Biophys Res Commun. 1971.)
- Pregnancies following chronic intermittent (pulsatile) administration of Gn-RH in hypothalamic amenorrhea (opens in a new tab) (Leyendecker G, Wildt L, Hansmann M. J Clin Endocrinol Metab. 1980.)
Related Clinical Trials
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- Purpose to Evaluate the Effectiveness of the Superovulation Stimulation Protocol Using Human Chorionic Gonadotropin (hCG) by Demonstrating Its Equivalence to Standard Controlled Ovarian Stimulation Protocols in Terms of Oocytes Retrieved, Blastulation While Maintaining an Economic AdvantageN/A · Enrolling By Invitation
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Common Questions
- What is Gonadorelin?
- Gonadorelin is synthetic gonadotropin-releasing hormone (GnRH/LHRH), the decapeptide that signals the pituitary to release the reproductive hormones LH and FSH. It has a history of regulatory approval as a diagnostic agent (to test pituitary function) and, given in pulses, as a therapy for certain forms of infertility; availability varies by region and several branded products have been discontinued. In sport, gonadorelin is prohibited in males by WADA.
- Is Gonadorelin approved for medical use?
- Gonadorelin is approved for one or more medical uses in at least one major jurisdiction. United States (FDA): Has a history of FDA approval: gonadorelin hydrochloride (Factrel) for evaluating pituitary gonadotropic function and gonadorelin acetate (Lutrepulse) for pulsatile induction of ovulation in hypothalamic amenorrhea. Several branded products have since been discontinued in the US (not for safety reasons), and gonadorelin is now commonly supplied via pharmacy compounding. European Union (EMA): Gonadorelin has been marketed in European countries through national approvals (as a diagnostic agent and for pulsatile fertility therapy) rather than through a single centralised EMA authorisation. Australia (TGA): Gonadorelin (native GnRH) has historically been used in Australia for diagnostic and fertility indications; whether a gonadorelin-specific product is currently on the ARTG is unclear. Related GnRH analogues such as leuprorelin and goserelin are registered.
- How does Gonadorelin work?
- In plain terms, gonadorelin is a copy of the brain hormone that tells the pituitary to release the hormones controlling the ovaries and testes. Technically, it is a decapeptide agonist of the GnRH receptor on pituitary gonadotrophs; when delivered in physiological pulses it stimulates secretion of luteinising hormone (LH) and follicle-stimulating hormone (FSH), whereas continuous (non-pulsatile) exposure paradoxically desensitises the receptor and suppresses gonadotropins, the principle exploited by long-acting GnRH analogues.
- Is Gonadorelin legal in Australia?
- Gonadorelin in Australia (TGA): Gonadorelin (native GnRH) has historically been used in Australia for diagnostic and fertility indications; whether a gonadorelin-specific product is currently on the ARTG is unclear. Related GnRH analogues such as leuprorelin and goserelin are registered.
- Is Gonadorelin banned in sport?
- Gonadorelin under the World Anti-Doping Agency (WADA) code: Prohibited in males under Section S2: WADA lists gonadotropin-releasing hormone (GnRH) agonists among luteinising-hormone releasing factors, and gonadorelin is explicitly named; it is not prohibited in females.