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Gonadotropin-releasing hormone analogue

  (Redirected from GnRH analogue)

A gonadotropin-releasing hormone analogue (GnRH analogue or analog), also known as a luteinizing hormone releasing hormone agonist (LHRH agonist) or LHRH analogue is a synthetic peptide drug modeled after the human hypothalamic gonadotropin-releasing hormone (GnRH). A GnRH analogue is designed to interact with the GnRH receptor and modify the release of the pituitary gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH) for therapeutic purposes. 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. Examples include goserelin and leuprorelin.[1]

Gonadotropin-releasing hormone analogue
Drug class
GNRH1 structure.png
GnRH, the peptide hormone from which all GnRH analogues are derived.
Class identifiers
SynonymsGnRH blockers; GnRH inhibitors; Antigonadotropins
UseInfertility; Prostate cancer; Precocious puberty; Breast cancer; Endometriosis; Uterine fibroids; Transgender people
Biological targetGnRH receptor
Chemical classPeptides
In Wikidata

Examples of GnRH modulators that are not GnRH analogues include elagolix and relugolix, which are non-peptide, small-molecule, and orally active compounds.

Contents

AgonistsEdit

A gonadotropin-releasing hormone agonist (GnRH agonist) is an analogue that activates the GnRH receptor resulting in increased secretion of FSH and LH. Initially it was thought that agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release, but it was soon recognized that agonists, after their initial stimulating action – termed a “flare” effect - eventually caused a paradoxical and sustained drop in gonadotropin secretion. This second effect was termed “downregulation” and can be observed after about 10 days. While this phase is reversible upon stopping the medication, it can be maintained when GnRH agonists use is continued for a long time.

AntagonistsEdit

A gonadotropin-releasing hormone antagonist (GnRH antagonist) is an analogue that blocks the GnRH receptor resulting in an immediate drop in gonadotropin (FSH, LH) secretion. The GnRH antagonist is primarily used in IVF treatments to block natural ovulation.

All GnRH analogues are contraindicated in pregnancy (pregnancy category X).

See alsoEdit

ReferencesEdit

  1. ^ Speroff L, Glass RH, Kase NG. Clinical Gynecologic Endocrinology and Infertility. Fifth Edition. Willimas 7 Wilkins, Baltimore. 1994. Pages 160-161.

External linksEdit