Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain

  title={Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain},
  author={Mohammad Ezzati and Bruce Richard Carr},
  journal={Women's Health},
  pages={19 - 28}
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… 

Elagolix in endometriosis-related pain: a profile of its use as approved in the USA

In phase 3 trials in women with moderate to severe endometriosis-related pain, elagolix improved clinical response rates for dysmenorrhea and non-menstrual pelvic pain to a significantly greater extent than placebo at 3 and 6 months of treatment.

Research development of a new GnRH antagonist (Elagolix) for the treatment of endometriosis: a review of the literature

From the results of the phase III studies, elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.

Overview of elagolix for the treatment of endometriosis

Elagolix demonstrated efficacy in the management of endometriosis-associated pain and had an acceptable safety and tolerability profile, however, further studies are necessary to evaluate its non-inferiority in comparison with other endometRIosis’s treatments.

Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas

Linzagolix showed a dose-dependent and rapidly reversible action on the pituitary-gonadal axis and the preliminary results of international, double-blind phase III trials reported its efficacy in treating heavy menstrual bleeding related to uterine myomas with a good safety profile.


All trials examining the utility of VPR for the treatment of UF are halted due to the recent reported cases of hepato-toxicity with UPA, in addition to non reassuring toxicology results from pre-clinical long-term testing on rodents, carried out in parallel with late stage testing on humans.

New insights on the pathogenesis of endometriosis and novel non-surgical therapies

Dienogest, AI, and GnRH antagonists are effective novel treatments with good tolerance and safety, while anti-TNF-α is still in the animal experimental stage and HIFU is a potential futuristic treatment.

Comparing the pharmacokinetic and pharmacodynamic qualities of current and future therapies for uterine fibroids

This manuscript aims to give an updated overview of the pharmacodynamic and pharmacokinetic properties of current and new investigational medical drugs for the treatment of symptomatic uterine fibroids.

The potential role of elagolix for treating uterine bleeding associated to uterine myomas

The aim of this drug evaluation is to give a complete overview of pharmacokinetic and pharmacodynamic data on elagolix for treating HMB related to uterine myomas and to report the results of the current clinical trials in this setting.

New Therapeutics in Endometriosis: A Review of Hormonal, Non-Hormonal, and Non-Coding RNA Treatments

The most recent medications under investigation in endometriosis treatment are summarized with an emphasis on non-coding RNAs that are emerging as key players in several human diseases, including cancer and endometRIosis.



Elagolix, an Oral GnRH Antagonist for Endometriosis-Associated Pain: A Randomized Controlled Study

Elagolix effectively reduced endometriosis-associated pelvic pain over a 24-week period and was well-tolerated.

Dienogest: A New Therapeutic Agent for the Treatment of Endometriosis

Dienogest (DNG), a progestin of 19-nortestosterone derivative, has good oral bioavailability and is highly selective for progesterone receptors, and is expected to be an effective treatment for endometriosis.

The Hormonal Profile of Norethindrone Acetate: Rationale for Add-Back Therapy With Gonadotropin-Releasing Hormone Agonists in Women With Endometriosis

Norethindrone acetate (NETA) is a unique progestin that has both estrogenic and androgenic properties and is effective as an add-back regimen without estrogen supplementation, which exerts beneficial effects on bone mineral density and vasomotor symptoms in women treated with GnRHa.

Gonadotrophin-releasing hormone analogues for pain associated with endometriosis.

GnRHas appear to be more effective at relieving pain associated with endometriosis than no treatment/placebo and limited on optimal dosage or duration of treatment for GnRHas.

Dienogest is as effective as leuprolide acetate in treating the painful symptoms of endometriosis: a 24-week, randomized, multicentre, open-label trial.

Dienogest 2 mg/day orally demonstrated equivalent efficacy to depot LA at standard dose in relieving the pain associated with endometriosis, although offering advantages in safety and tolerability.

Gonadotrophin receptor hormone analogues in combination with add-back therapy: an update

This review article is an update on the evidence supporting gonadotrophin receptor hormone analogues in combination with add-back therapy.

Add-back therapy in the treatment of endometriosis: the European experience.

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  • Medicine, Biology
    British journal of obstetrics and gynaecology
  • 1996
In a small open study the gonadomimetic tibolone totally prevented the loss of bone structure during GnRH agonist therapy, suggesting that if a Gn RH agonist is considered the treatment of choice, then HRT should be used in combination.

Hormone treatment of endometriosis: the estrogen threshold hypothesis.

  • R. Barbieri
  • Medicine, Biology
    American journal of obstetrics and gynecology
  • 1992
Differences in organ response to estradiol may allow the design of regimens with a gonadotropin-releasing hormone agonist that maintain a therapeutic response and ameliorate potential adverse effects.