Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain

Mohammad Ezzati, Bruce R. Carr

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

Suppression of estrogen production and reduction of menstrual blood flow are the mainstays of medical treatment of endometriosis-related pain and have been traditionally achieved by methods such as combined hormonal contraception, progestins and GnRH analogs, all with comparable efficacies, though different side-effect profiles. Elagolix is the frontrunner among an emerging class of GnRH antagonists, which unlike their peptide predecessors has a nonpeptide structure resulting in its oral bioavailability. Phase I and II clinical trials have demonstrated safety of elagolix and its efficacy in partial and reversible suppression of ovarian estrogen production resulting in improvements in endometriosis-related pain. Phase III clinical trials are currently underway and elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.

Original languageEnglish (US)
Pages (from-to)19-28
Number of pages10
JournalWomen's Health
Volume11
Issue number1
DOIs
StatePublished - Jan 1 2015

Fingerprint

Endometriosis
Gonadotropin-Releasing Hormone
Pain
Estrogens
Progesterone Congeners
Phase III Clinical Trials
Phase II Clinical Trials
Clinical Trials, Phase I
Contraception
Biological Availability
Therapeutics
Pharmacology
Safety
Peptides
elagolix

Keywords

  • Bone mineral density
  • elagolix
  • endometriosis
  • GnRH antagonists
  • medical treatment

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. / Ezzati, Mohammad; Carr, Bruce R.

In: Women's Health, Vol. 11, No. 1, 01.01.2015, p. 19-28.

Research output: Contribution to journalArticle

@article{4b203f3ecc4f4248993c9cbf43f95a52,
title = "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain",
abstract = "Suppression of estrogen production and reduction of menstrual blood flow are the mainstays of medical treatment of endometriosis-related pain and have been traditionally achieved by methods such as combined hormonal contraception, progestins and GnRH analogs, all with comparable efficacies, though different side-effect profiles. Elagolix is the frontrunner among an emerging class of GnRH antagonists, which unlike their peptide predecessors has a nonpeptide structure resulting in its oral bioavailability. Phase I and II clinical trials have demonstrated safety of elagolix and its efficacy in partial and reversible suppression of ovarian estrogen production resulting in improvements in endometriosis-related pain. Phase III clinical trials are currently underway and elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.",
keywords = "Bone mineral density, elagolix, endometriosis, GnRH antagonists, medical treatment",
author = "Mohammad Ezzati and Carr, {Bruce R.}",
year = "2015",
month = "1",
day = "1",
doi = "10.2217/whe.14.68",
language = "English (US)",
volume = "11",
pages = "19--28",
journal = "Women's health (London, England)",
issn = "1745-5065",
publisher = "Future Medicine Ltd.",
number = "1",

}

TY - JOUR

T1 - Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain

AU - Ezzati, Mohammad

AU - Carr, Bruce R.

PY - 2015/1/1

Y1 - 2015/1/1

N2 - Suppression of estrogen production and reduction of menstrual blood flow are the mainstays of medical treatment of endometriosis-related pain and have been traditionally achieved by methods such as combined hormonal contraception, progestins and GnRH analogs, all with comparable efficacies, though different side-effect profiles. Elagolix is the frontrunner among an emerging class of GnRH antagonists, which unlike their peptide predecessors has a nonpeptide structure resulting in its oral bioavailability. Phase I and II clinical trials have demonstrated safety of elagolix and its efficacy in partial and reversible suppression of ovarian estrogen production resulting in improvements in endometriosis-related pain. Phase III clinical trials are currently underway and elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.

AB - Suppression of estrogen production and reduction of menstrual blood flow are the mainstays of medical treatment of endometriosis-related pain and have been traditionally achieved by methods such as combined hormonal contraception, progestins and GnRH analogs, all with comparable efficacies, though different side-effect profiles. Elagolix is the frontrunner among an emerging class of GnRH antagonists, which unlike their peptide predecessors has a nonpeptide structure resulting in its oral bioavailability. Phase I and II clinical trials have demonstrated safety of elagolix and its efficacy in partial and reversible suppression of ovarian estrogen production resulting in improvements in endometriosis-related pain. Phase III clinical trials are currently underway and elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.

KW - Bone mineral density

KW - elagolix

KW - endometriosis

KW - GnRH antagonists

KW - medical treatment

UR - http://www.scopus.com/inward/record.url?scp=84920982682&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84920982682&partnerID=8YFLogxK

U2 - 10.2217/whe.14.68

DO - 10.2217/whe.14.68

M3 - Article

C2 - 25581052

AN - SCOPUS:84920982682

VL - 11

SP - 19

EP - 28

JO - Women's health (London, England)

JF - Women's health (London, England)

SN - 1745-5065

IS - 1

ER -