Objective

To evaluate the efficacy and safety of 40-mg relugolix (REL) compared with those of leuprorelin (LEU) in women with endometriosis-associated pain.

Design

Phase 3, multicenter, randomized, double-blind, double-dummy, active-controlled study in Japanese patients.

Setting

Hospitals and clinics.

Patient(s)

Women aged ≥20 years with regular menstrual cycles (25–38 days) experiencing endometriosis or ovarian endometrioma and reporting pelvic pain.

Intervention(s)

In the REL group, 40 mg of REL was orally administered once a day for 24 weeks. In the LEU group, 3.75 or 1.88 mg of LEU was subcutaneously injected every 4 weeks for 24 weeks.

Main Outcome Measure(s)

The primary endpoint was the change in the maximum visual analog scale score for pelvic pain from baseline until 28 days before the end of treatment.

Result(s)

Changes in the maximum visual analog scale score were −52.6 ± 1.3 for REL and −57.5 ± 1.4 for LEU. Ovarian endometrioma decreased by 12.26 ± 17.52 cm³ for REL and 14.10 ± 18.81 cm³ for LEU. Drug-related treatment emergent adverse events with an incidence of >10% for both groups were hot flush, metrorrhagia, headache, and genital hemorrhage. Discontinuations from treatment emergent adverse events were 2.9% for REL and 4.3% for LEU.

Conclusion(s)

Relugolix was noninferior to LEU for treating endometriosis-associated pelvic pain. Safety profiles of both medications were comparable, although menses returned earlier in patients taking REL, a huge benefit for women who plan to conceive after treatment.

Clinical Trial Registration Number

ClinicalTrials.gov: NCT03931915.

中文翻译：

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Relugolix 是一种口服促性腺激素释放激素受体拮抗剂，与亮丙瑞林相比，可减轻日本女性子宫内膜异位症相关的疼痛：一项 3 期、随机、双盲、非劣效性研究

客观的

评估 40 毫克 relugolix (REL) 与亮丙瑞林 (LEU) 治疗子宫内膜异位症相关疼痛的疗效和安全性。

设计

在日本患者中进行的多中心、随机、双盲、双模拟、主动对照研究的 3 期。

环境

医院和诊所。

耐心）

年龄≥20 岁且月经周期规律（25-38 天）的女性患有子宫内膜异位症或卵巢子宫内膜异位症并报告盆腔疼痛。

干预措施

在 REL 组中，每天一次口服 40 mg REL，持续 24 周。在 LEU 组中，每 4 周皮下注射 3.75 或 1.88 mg LEU，持续 24 周。

主要观察指标）

主要终点是从基线到治疗结束前 28 天的盆腔疼痛最大视觉模拟量表评分的变化。

结果）

REL 的最大视觉模拟量表评分变化为 -52.6 ± 1.3，LEU 为 -57.5 ± 1.4。卵巢子宫内膜异位症的 REL 减少了 12.26 ± 17.52 cm ³ ，LEU 减少了14.10 ± 18.81 cm ³。两组发生率均>10%的药物相关治疗突发不良事件为潮热、子宫出血、头痛和生殖器出血。REL 和 LEU 的治疗紧急不良事件中止率为 2.9% 和 4.3%。

结论

Relugolix 在治疗子宫内膜异位症相关的盆腔疼痛方面不劣于 LEU。两种药物的安全性相当，尽管服用 REL 的患者月经恢复得更早，这对计划在治疗后怀孕的女性来说是一个巨大的好处。

临床试验注册号

ClinicalTrials.gov：NCT03931915。