| Gonadotropin-releasing hormone modulator | |
|---|---|
| Drug class | |
 Leuprorelin, a GnRH agonist and GnRH analogue and a prototypical GnRH modulator. | |
| Class identifiers | |
| Synonyms | GnRH receptor modulator; GnRH analogue; GnRH agonist; GnRH antagonist; GnRH blocker; LHRH modulator; LHRH receptor modulator; LHRH analogue; LHRH agonist; LHRH antagonist; LHRH blocker |
| Use | Infertility; prostate cancer; precocious puberty; breast cancer; endometriosis; uterine fibroids; transgender people |
| Biological target | GnRH receptor |
| Chemical class | Peptide; small-molecule (non-peptide) |
| Legal status | |
| In Wikidata | |
A GnRH modulator, or GnRH receptor modulator, also known as an LHRH modulator or LHRH receptor modulator, is a type of medication which modulates the GnRH receptor, the biological target of the hypothalamic hormone gonadotropin-releasing hormone (GnRH; also known as luteinizing-releasing hormone, or LHRH).[1][2] They include GnRH agonists and GnRH antagonists. These medications may be GnRH analogues like leuprorelin and cetrorelix – peptides that are structurally related to GnRH – or small-molecules like elagolix and relugolix, which are structurally distinct from and unrelated to GnRH analogues.
GnRH modulators affect the secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn affects the gonads, influencing their function and hence fertility as well as the production of sex steroids, including that of estradiol and progesterone in women and of testosterone in men. As such, GnRH modulators can also be described as progonadotropic or antigonadotropic, depending on whether they act to increase or decrease gonadotropins.
Shortly after the discovery of GnRH by Nobel laureates Guillemin and Schally, researchers tried to modify the GnRH decapeptide with the intent to create analogues that could activate or block the receptor. Subsequent to the development and introduction of GnRH analogues, non-peptide or small-molecule GnRH modulators were developed and introduced.
All GnRH modulators are contraindicated in pregnancy (pregnancy category X).
- ^ Riggs MM, Bennetts M, van der Graaf PH, Martin SW (2012). "Integrated pharmacometrics and systems pharmacology model-based analyses to guide GnRH receptor modulator development for management of endometriosis". CPT: Pharmacometrics & Systems Pharmacology. 1 (9): 1–9. doi:10.1038/psp.2012.10. PMC 3606940. PMID 23887363.
- ^ Catherine Racowsky, Peter N. Schlegel, Bart C.J.M. Fauser, Douglas Carrell (7 June 2011). Biennial Review of Infertility. Springer Science & Business Media. pp. 80–. ISBN 978-1-4419-8456-2.