GnRH modulator

GnRH 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
Use Infertility; Prostate cancer; Precocious puberty; Breast cancer; Endometriosis; Uterine fibroids; Transgender people
Biological target GnRH receptor
Chemical class Peptide; Small-molecule (non-peptide)
In Wikidata

A GnRH modulator, or GnRH receptor modulator, is a type of drug which modulates the GnRH receptor, the biological target of gonadotropin-releasing hormone (GnRH).[1][2] They include GnRH agonists and GnRH antagonists. These drugs may be GnRH analogues like leuprorelin and cetrorelixpeptides that are structurally related to GnRH – or small-molecules like relugolix, which are structurally distinct. 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 progonadotropins or antigonadotropins, depending on whether they serve to increase or decrease gonadotropin levels.

References

  1. 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 Syst Pharmacol. 1: e11. PMC 3606940Freely accessible. PMID 23887363. doi:10.1038/psp.2012.10.
  2. 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.


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