Therapeutic uses of gonadotropin-releasing hormone analogs

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GnRH analogs, developed since 1971, desensitize pituitary receptors with chronic use, decreasing gonadotropin secretion and potentially serving as contraceptives or treatments for conditions requiring reduced gonadal steroid production.

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This review examines the clinical utility of long-acting agonistic and antagonistic gonadotropin-releasing hormone (GnRH) analogs developed since their synthesis in 1971. Agonistic analogs function by desensitizing pituitary GnRH receptors through chronic use, which leads to decreased gonadotropin secretion and a resulting hypogonadal state. The authors highlight substantial progress in utilizing these agents as potential contraceptives and for treating various conditions where reduced gonadal steroid production is therapeutically beneficial. Relevance to endometriosis: listed as one indication for GnRH antagonists, though the paper's main focus is uterine fibroids.

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Abstract

Since the discovery and synthesis of gonadotropin-releasing hormone (GnRH) in 1971, numerous long-acting agonistic and antagonistic analogs have been synthesized. Agonistic analogs were found to desensitize pituitary GnRH receptors with chronic use, resulting in decreased gonadotropin secretion and a hypogonadal state. These analogs are being investigated as potential contraceptives and in the treatment of several conditions in which decreased gonadal steroid production is desired. Substantial progress has been made in these areas. The purpose of this review is to provide the clinician with data regarding the potential clinical utility of this class of peptides.
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Review: PDF Only Therapeutic Uses of Gonadotropin-Releasing Hormone Analogs - JANICE L. ANDREYKO - LORNA A. MARSHALL - DANIEL A. DUMESIC - ROBERT B. JAFFE Obstetrical & Gynecological Survey 42(1):p 1-21, January 1987. Since the discovery and synthesis of gonadotropin-releasing hormone (GnRH) in 1971, numerous long-acting agonistic and antagonistic analogs have been synthesized. Agonistic analogs were found to desensitize pituitary GnRH receptors with chronic use, resulting in decreased gonadotropin secretion and a hypogonadal state. These analogs are being investigated as potential contraceptives and in the treatment of several conditions in which decreased gonadal steroid production is desired. Substantial progress has been made in these areas. The purpose of this review is to provide the clinician with data regarding the potential clinical utility of this class of peptides. Copyright © Williams & Wilkins 1987. All Rights Reserved.

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Condition tags

endometriosis

MeSH descriptors

Pituitary Hormone-Releasing Hormones Contraceptive Agents, Female Contraceptive Agents, Female Contraceptive Agents, Male Contraceptive Agents, Male Endometriosis Endometriosis Endometriosis Female Female Hirsutism Hirsutism Hirsutism Humans Humans Leiomyoma Leiomyoma Leiomyoma Male Male

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europepmc
last seen: 2026-10-04T09:26:46.659050+00:00
pubmed
last seen: 2026-10-08T21:34:55.717994+00:00
unpaywall
last seen: 2026-10-09T06:36:44.367587+00:00
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