"目录号: HY-14789
Elagolix是一种高度有效的, 选择性, 口服活性的, 短期的, 非肽类促性腺激素释放激素受体 (GnRH受体) 拮抗剂 (KD = 54 pM)。
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生物活性
Description
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).Target: GnRHin vitro: Elagolix is a short-acting, nonpeptide, GnRH antagonist, administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
Clinical Trial
AbbVie (prior sponsor, Abbott)-AbbVie
Heavy Uterine Bleeding-Uterine Fibroids
September 2011
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Endometriosis
May 2012
Phase 3
AbbVie
Uterine Fibroids-Heavy Menstrual Bleeding
September 14, 2016
Phase 3
AbbVie
Endometriosis
September 2013
Phase 3
AbbVie
Uterine Fibroids-Heavy Menstrual Bleeding
November 7, 2015
Phase 3
AbbVie
Endometriosis
July 7, 2017
Phase 3
AbbVie
Endometriosis
May 27, 2014
Phase 3
AbbVie
Uterine Fibroids-Heavy Menstrual Bleeding
January 4, 2016
Phase 3
AbbVie
Endometriosis
December 2012
Phase 3
AbbVie (prior sponsor, Abbott)-Neurocrine Biosciences-AbbVie
Folliculogenesis
June 2011
Phase 1
AbbVie
Heavy Uterine Bleeding-Uterine Fibroids
January 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Endometriosis-Pain
August 2009
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Endometriosis
November 2006
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Endometriosis, Pain
December 2007
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Endometriosis
November 2008
Phase 2
Abbott
Endometriosis
April 2005
Phase 2
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References
