恶拉戈利钠的功效与作用是怎样的

Elagolix sodium can cause a dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), resulting in decreased blood concentrations of the ovarian sex hormones, estradiol, and progesterone. Elagolix, also known as Orilissa or elagolix, is an orally bioavailable, second-generation, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the treatment of moderate to severe pain associated with endometriosis.

To evaluate the efficacy and safety of the oral nonpeptide gonadotropin-releasing hormone antagonist elagolix sodium in the treatment of endometriosis-related pain over 12 months.

Methods: Elaris Endometriosis (EM) III (NCT01760954) and IV (NCT02143713) was an extension study that evaluated two doses (150 mg once daily and 200 mg twice daily) for an additional 6 months following two 6-month, double-blind, placebo-controlled Phase 3 trials (12 months of continuous treatment).

The primary efficacy endpoint was the proportion of responders (clinically meaningful pain reduction and stable or reduced rescue analgesic use) based on average monthly dysmenorrhea and non-transvaginal pelvic pain scores. Safety assessment included clinical laboratory testing, endometrial and bone density assessment. Efficacy of Elaris EM-III and -IV is based on comparison with placebo in Elaris EM-I and -II, with an estimated dropout rate of 25%.

Results: A total of 569 participants were enrolled between December 28, 2012 and October 31, 2014 (Elaris EM-III), and between May 27, 2014 and January 6, 2016 (Elaris EM-IV). After 12 months of treatment, response rates for Elaris EM-III for dysmenorrhea were 52.1% and 78.2% at 150 mg once daily (Elaris EM-IV 550.8%) and 200 mg twice daily (Elaris EMV 575.9%), respectively. Elaris EM-III had a poor response rate of 45.2% at 150 mg once daily (Elaris EM-IV=45.9%), with a response rate of 60.0% at 200 mg twice daily (Elari EM-IV=58.1%).

Flushing is the most common adverse event. After 12 months of treatment, a decrease in bone density and an increase in lipids from baseline were observed. No adverse reactions were seen in the endometrium.

Conclusion: Long-term treatment can sustainably reduce dysmenorrhea, nonmenstrual pelvic pain, and dyspareunia. This safety profile is consistent with reductions in estrogen levels, and there are no new safety concerns associated with long-term use of elagolix sodium.

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References

Surrey E, Taylor HS, Giudice L, Lessey BA, Abrao MS, Archer DF, Diamond MP, Johnson NP, Watts NB, Gallagher JC, Simon JA, Carr BR, Dmowski WP, Leyland N, Singh SS, Rechberger T, Agarwal SK, Duan WR, Schwefel B, Thomas JW, Peloso PM, Ng J, Soliman AM, Chwalisz K. Long-Term Outcomes of Elagolix in Women With Endometriosis: Results From Two Extension Studies. Obstet Gynecol. 2018 Jul;132(1):147-160. doi: 10.1097/AOG.0000000000002675. Erratum in: Obstet Gynecol. 2018 Dec;132(6):1507-1508. PMID: 29889764.