Gonadotropin-releasing hormone modulator

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Gonadotropin-releasing hormone modulator
Drug class
Leuprorelin ball-and-stick.png
Leuprorelin, a GnRH agonist and GnRH analogue and a prototypical GnRH modulator.
Class identifiers
SynonymsGnRH receptor modulator; GnRH analogue; GnRH agonist; GnRH antagonist
UseInfertility; Prostate cancer; Precocious puberty; Breast cancer; Endometriosis; Uterine fibroids; Transgender people
Biological targetGnRH receptor
Chemical classPeptide; Small-molecule (non-peptide)
In Wikidata

A GnRH modulator, or GnRH receptor modulator, is a type of medication which modulates the GnRH receptor, the biological target of the hypothalamic hormone gonadotropin-releasing hormone (GnRH).[1][2] They include GnRH agonists and GnRH antagonists. These medications may be GnRH analogues like leuprorelin and cetrorelixpeptides that are structurally related to GnRH – or small-molecules like elagolix, which are structurally distinct from 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.

GnRH agonists[edit]

Peptides[edit]

GnRH antagonists[edit]

Peptides[edit]

Non-peptides[edit]

a = Under development; not yet marketed.

See also[edit]

References[edit]

  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. doi:10.1038/psp.2012.10. PMC 3606940. PMID 23887363.
  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.