恶拉戈利钠(elagolix)是什么药？

Author: Medicalhalo

Release time: 2025-10-19 11:44:20

Elagolix sodium (elagolix) was jointly developed by AbbVie and Neurocrine Biosciences. It was approved by the US FDA for marketing on July 23, 2018, and its trade name is Orilissa. This medicine is taken by mouth and is used to treat moderate to severe endometriosis pain in women.

Indications and uses

It is an active non-peptide GnRH antagonist that has been approved by the Food and Drug Administration for the treatment of moderate to severe pain associated with endometriosis.

Endometriosis often occurs in women during the childbearing period. It is a gynecological disease that relies on the regulation of estrogen and progesterone. Currently, long-term comprehensive treatment with surgery and hormonal drugs is mainly used to improve the clinical symptoms of patients and reduce the recurrence of the disease. Elagolix is the first oral, non-peptide, small molecule gonadotropin-releasing hormone receptor antagonist for the treatment of moderate to severe endometriosis.

Listing information

As of December 5, 2023, elagolix has not yet been launched in China. It is currently listed in the United States and Canada.

Drug Advantages

Compared with other GnRH antagonists, the novelty of elagolix lies in its non-peptide structure, which allows its oral administration. Several Phase I, II and III clinical trials that evaluated the safety and effectiveness of this new drug were analyzed.

Because many drugs are already on the market and gaining popularity in the treatment of endometriosis-related symptoms, equality or superiority of efficacy, tolerability, and patient compliance should be assessed when introducing new drugs. Although elagolix may have an advantage over existing GnRH agonists in that it does not cause "flare" effects, it can also have an impact on bone density. However, studies have shown that this new oral GnRH antagonist is well tolerated, with side effects described as "mild or moderate."

In addition, because the degree of ovarian suppression by elagolix is dose-dependent, it can relieve pain by regulating low estrogen levels while limiting it.

Clinical treatment effects

1. Endometriosis:

Suppressing estrogen production and reducing menstrual flow are the main methods of drug treatment for endometriosis-related pain. Traditionally, this is achieved through combined hormonal contraception, progesterone and GnRH analogues. Although the side effects are different, the efficacy is equivalent. Elagolix is a leader in an emerging class of GnRH antagonists that, unlike its peptide precursor, has a non-peptide structure, resulting in its oral bioavailability.

Phase I and II clinical trials demonstrated the safety of elagolix and its effectiveness in partial and reversible suppression of ovarian estrogen production, thereby improving endometriosis-related pain. Phase III clinical trials are currently underway, and elagolix may become an important addition to the treatment of endometriosis-related pain.

Additionally, one study showed that both high and low doses of elagolix were effective in improving dysmenorrhea and nonmenstrual pelvic pain in women with endometriosis-related pain over a 6-month period. Both doses of elagolix are associated with hypoestrogenic side effects.

2. Uterine fibroids:

Background: Uterine fibroids are hormone-responsive tumors and are related to heavy menstrual bleeding. As a new type of gonadotropin inhibitor, elagolix has a rapid and reversible effect and can effectively reduce the occurrence of uterine smooth muscle bleeding.

Methods: Two identical, randomized, placebo-controlled, 6-month phase 3 trials (Elaris Uterine Fibroids No. 1 and 2 [UF-1 and UF-2]) were conducted to evaluate the efficacy and safety of elagolix at a dose of 300 mg twice daily in women with fibroid-related bleeding using hormonal "add-back" therapy.

Treatment with elagolix alone was performed to evaluate its hypoestrogenic effects compared with elagolix. The initial goal of the study was that the menstrual volume should be less than 80 ml in the first month of treatment, and the menstrual volume should decrease by no less than 50% from baseline to the most recent month. Various interpolation methods were used to interpolate missing data.

Results: A total of 412 women in the UF-1 group and 378 women in the UF-2 group were randomized to receive elagolix or placebo and were included in the analysis. Sixty-eight percent of 206 women in the UF-1 group who received elagolix plus add-back therapy and 76.5% of 189 women in the UF-2 group met criteria for the primary endpoint, compared with 8.7% of 102 women and 10% of 94 women who received placebo (P<0.001 in both trials).

Among women who received elagolix alone, 84.1% of 104 women in the UF-1 group and 77% of 95 women in the UF-2 group met the primary endpoint. The incidence of hot flashes (in both trials) and uterine bleeding (in UF-1) was significantly higher in the elagolix plus add-back group than in the placebo group. The hypoestrogenic effects of elagolix, especially the reduction in bone density, are attenuated during add-back therapy.

Conclusion: Elagolix sodium (elagolix) plus reinfusion therapy can effectively reduce heavy menstrual bleeding in patients with uterine fibroids.

Summary

Elagolix is a prescription drug used to treat moderate to severe pain associated with endometriosis. It is not known whether elagolix is safe and effective in children.