Gonadotropin-releasing hormone analogue

Drug class

GnRH, the peptide hormone from which all GnRH analogues are derived.

Class identifiers
Synonyms| GnRH blockers; GnRH inhibitors; Antigonadotropins
Use| Infertility; Prostate cancer; Precocious puberty; Breast cancer; Endometriosis; Uterine fibroids; Transgender people
Biological target| GnRH receptor
Chemical class| Peptides

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 pituitary gonadotropins FSH and 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 synthesize stimulating and blocking variants. Examples include goserelin and leuprorelin.[1]

An example of a GnRH modulator that is not a GnRH analogue is elagolix, a non-peptide and small-molecule compound.

## Contents

* 1 Agonists
* 2 Antagonists
* 3 See also
* 4 References
* 5 External links

## Agonists

Main article: Chemistry:Gonadotropin-releasing hormone agonist

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.

## Antagonists

Main article: Chemistry:Gonadotropin-releasing hormone antagonist

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 also

* GnRH modulator
* Progonadotropin
* CYP17A1 inhibitor

## References

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

## External links

* History of GnRH agonist and antagonist development

* v
* t
* e

GnRH and gonadotropins

GnRH modulators
(incl. analogues)|

| Agonists|

* Peptide: Azagly-nafarelin
* Buserelin
* Deslorelin
* Fertirelin
* Gonadorelin
* Goserelin
* Histrelin
* Lecirelin
* Leuprorelin (leuprolide)
* Nafarelin
* Peforelin
* Triptorelin

|

Antagonists|

* Peptide: Abarelix
* Cetrorelix
* Degarelix
* Ganirelix

* Non-peptide: Elagolix
* Linzagolix†
* Relugolix†

Gonadotropins|

| Preparations|

* Follicle-stimulating hormone
* Human chorionic gonadotropin
* Luteinizing hormone
* Menotropin
* Urofollitropin

|

Others
(indirect)|

| Progonadotropins|

* Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide)
* Antiestrogens/SERMs (e.g., tamoxifen, Chemistry:Clomifene

|

Antigonadotropins|

* Sex steroid agonists (via negative feedback on the HPG axis): Androgens/anabolic steroids (e.g., testosterone, nandrolone esters, oxandrolone)
* D2 receptor antagonists (prolactin releasers) (incl., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
* Estrogens (incl., bifluranol, estradiol, estradiol esters, ethinylestradiol, diethylstilbestrol, paroxypropione)
* Progestogen|Progestogens (incl. progestins, e.g., Chemistry:Chlormadinone acetate

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

See also
GnRH and gonadotropin receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
Progestogens and antiprogestogens

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*[GnRH]: gonadotropin-releasing hormone
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[HPG]: hypothalamic–pituitary–gonadal
*[SERMs]: Selective estrogen receptor modulators