Adoprazine

"目录号: HY-14789

GPCR/G Protein-

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)。

GNRH Receptor

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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

NCT01441635

AbbVie (prior sponsor, Abbott)-AbbVie

Heavy Uterine Bleeding-Uterine Fibroids

September 2011

Phase 2

NCT01620528

AbbVie (prior sponsor, Abbott)-AbbVie

Endometriosis

May 2012

Phase 3

NCT02925494

AbbVie

Uterine Fibroids-Heavy Menstrual Bleeding

September 14, 2016

Phase 3

NCT01931670

AbbVie

Endometriosis

September 2013

Phase 3

NCT02654054

AbbVie

Uterine Fibroids-Heavy Menstrual Bleeding

November 7, 2015

Phase 3

NCT03213457

AbbVie

Endometriosis

July 7, 2017

Phase 3

NCT02143713

AbbVie

Endometriosis

May 27, 2014

Phase 3

NCT02691494

AbbVie

Uterine Fibroids-Heavy Menstrual Bleeding

January 4, 2016

Phase 3

NCT01760954

AbbVie

Endometriosis

December 2012

Phase 3

NCT01403038

AbbVie (prior sponsor, Abbott)-Neurocrine Biosciences-AbbVie

Folliculogenesis

June 2011

Phase 1

NCT01817530

AbbVie

Heavy Uterine Bleeding-Uterine Fibroids

January 2013

Phase 2

NCT00973973

AbbVie (prior sponsor, Abbott)-AbbVie

Endometriosis-Pain

August 2009

Phase 2

NCT00437658

AbbVie (prior sponsor, Abbott)-AbbVie

Endometriosis

November 2006

Phase 2

NCT00619866

AbbVie (prior sponsor, Abbott)-AbbVie

Endometriosis, Pain

December 2007

Phase 2

NCT00797225

AbbVie (prior sponsor, Abbott)-AbbVie

Endometriosis

November 2008

Phase 2

NCT00109512

Abbott

Endometriosis

April 2005

Phase 2

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References

[1].Carr B, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density. Reprod Sci. 2014 Nov;21(11):1341-1351.