To verify the non-inferiority of KLH-2109 to leuprorelin acetate in a double-blind manner in terms of efficacy in endometriosis patients with pelvic pain.

开始日期2025-06-09

申办/合作机构

Kissei Pharmaceutical Co., Ltd.

NCT05738382

/ Unknown status临床2期

A Randomized, Double-blind, Open for Active Comparator, Parallel, Multi-center Phase II Study to Explore the Efficacy, Safety and Tolerability of BG2109 Compared With Cetrorelix During COH in Female Subjects Undergoing ART Procedures

To explore the optimal effective daily dose of BG2109 to suppress premature luteinizing hormone (LH) surge during COH in female subjects undergoing ART procedures.

开始日期2023-08-01

申办/合作机构

上海葆正医药科技有限公司

NCT05894135

/ Recruiting临床3期

A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Phase III Study to Evaluate the Efficacy and Safety of BG2109 in Chinese Subjects With Endometriosis

The objective of this study is to demonstrate the efficacy and safety of BG2109 administered orally once daily at a dose of 100 mg alone or of 200 mg in combination with add-back hormone replacement therapy (ABT: estradiol (E2) 1 mg / norethisterone acetate (NETA) 0.5 mg) versus placebo, while under randomized treatment, in the management of moderate to severe endometriosis-associated pain (EAP) in chinese women with surgically confirmed endometriosis

开始日期2023-07-14

申办/合作机构

上海葆正医药科技有限公司

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100 项与林扎戈利相关的专利（医药）

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项与林扎戈利相关的文献（医药）

2025-10-01·FERTILITY AND STERILITY

Linzagolix with and without hormonal add-back therapy for symptomatic uterine fibroids: PRIMROSE 1 & 2 long-term extension and withdrawal study

Article

作者: Satoshi Hori ; Hugh Taylor ; Francisco Carmona Herrera ; Elke Bestel ; Sven Becker ; Marie-Madeleine Dolmans ; Christian M Becker ; Felice Petraglia ; Jacques Donnez

OBJECTIVE:

To evaluate whether oral linzagolix administered once daily for up to 52 weeks (extension study) at a dose of 100 mg or 200 mg with or without hormonal add-back therapy (ABT) (1.0 mg estradiol; 0.5 mg norethisterone acetate) can maintain the efficacy and tolerability seen at 6 months of therapy and whether there is any recurrence of symptoms (bleeding and pain) after cessation of therapy (withdrawal study).

DESIGN:

PRIMROSE 1 and PRIMROSE 2 were essentially identical, randomized, parallel, double-blind, and placebo-controlled phase 3 trials conducted in women with uterine fibroid-associated heavy menstrual bleeding (HMB) (menstrual blood loss [MBL] of more than 80 mL per cycle over 2 menstrual cycles).

SUBJECTS:

In PRIMROSE 1 and 2, 1,012 women were included in the full analysis set. Eligible subjects were women aged 18 years or older with ultrasound-confirmed fibroids and HMB of at least 80 mL blood loss per cycle for a minimum of two cycles, as determined by the alkaline hematin method. Eligible participants had to have at least one fibroid measuring 2 cm in diameter or more (or multiple small fibroids with overall uterine volume exceeding 200 cm³), but no fibroids greater than 12 cm in diameter.

INTERVENTION:

Eligible women with uterine fibroid-associated HMB were randomly assigned at a 1:1:1:1:1 ratio to one of five masked daily treatment: placebo, 100 mg linzagolix alone, 100 mg linzagolix with hormonal ABT (1 mg estradiol and 0.5 mg norethisterone acetate), 200 mg linzagolix alone , or 200 mg linzagolix with hormonal ABT (1 mg estradiol and 0.5 mg norethisterone acetate). After 24 weeks, patients assigned to the placebo or 200 mg linzagolix alone groups were switched to 200 mg linzagolix with ABT, except in PRIMROSE 1, in which 50% of subjects on a placebo continued with the placebo (random selection) until week 52. All other women continued on the original study medication. Efficacy and safety were evaluated at week 52 (extension study) as well as week 64 (withdrawal study). Bone mineral density was also assessed at week 76 (6 months after cessation of therapy).

MAIN OUTCOME MEASURES:

The primary endpoint was decreased MBL to less than 80 mL and a reduction of more than 50% from baseline. Specifically, this study sought to determine whether the reduction in MBL and other secondary outcomes, such as uterine volume and pain, observed at 24 weeks could be maintained over an extended (52 weeks) treatment period and further withdrawal period.

RESULTS:

In the pooled data from PRIMROSE 1 and PRIMROSE 2 extension studies, the significantly higher proportion of women showing a reduction in HMB in all linzagolix (with or without ABT) treatment groups observed at week 24, was maintained until week 52. Percentages of women with reduced MBL at week 52 (based on the pooled week 52 full analysis set) were 55.0% in the 100 mg group, 86.1% in the 100 mg with ABT group, 76.7% in the 200 mg group/200 mg with ABT, and 89.9% in the 200 mg with ABT group. Of subjects previously treated with linzagolix and in amenorrhea by week 52, 88.8% reported their first bleed or heavy bleeding between weeks 52 and 64. In both PRIMROSE studies, the most common adverse events up to week 52 were hot flushes. Their incidence had returned to baseline values by week 64. Bone mineral density was well preserved in all groups at week 52. In women treated with 200 mg linzagolix alone up to week 24, initial bone mineral density loss (lumbar spine) recovered by week 52 after adding ABT from week 24 onwards.

CONCLUSION:

Findings at 52 weeks confirmed the benefits of treatment observed at 24 weeks. At 52 weeks, linzagolix 100 mg or 200 mg with or without ABT was found to reduce HMB, which is a burden for women with uterine fibroids. Their quality of life was improved. Risks of bone loss and vasomotor symptoms were minimized as a result of ABT administration. Partial suppression with once-daily linzagolix 100 mg without ABT potentially provides a unique option for chronic treatment of symptomatic uterine fibroids in women who do not wish to have ABT or in whom it is contraindicated. The relatively fast recurrence of uterine fibroid-associated symptoms after cessation of therapy is an argument in favor of long-term continuation of treatment.

TRIAL REGISTRATION:

PRIMROSE1 (NCT03070899) PRIMROSE 2 (NCT03070951).

2025-08-01·BJOG-AN INTERNATIONAL JOURNAL OF OBSTETRICS AND GYNAECOLOGY

Pain Reduction in Linzagolix‐Treated Patients With Uterine Fibroids: A Secondary Mediation Analysis of the PRIMROSE 1 and 2 Phase 3 Trials

Article

作者: Boolell, Mitra ; Petraglia, Felice ; Dolmans, Marie‐Madeleine ; Becker, Sven ; Bestel, Elke ; Herrera, Francisco Carmona ; Ionescu‐Ittu, Raluca ; Donnez, Jacques ; Renner, Stefan P. ; Hori, Satoshi ; St‐Pierre, Julien

ABSTRACT:

Objective:

Among women with uterine fibroids (UFs), we assess the extent to which the linzagolix effect on pain alleviation is explained by its effect on reducing heavy menstrual bleeding (HMB) and fibroid volume (FV).

Design:

Post hoc analysis on the pooled data from two randomised double‐blind placebo‐controlled phase 3 trials.

Setting:

94 sites in the US (PRIMROSE 1 trial) and 95 sites in Europe/US (PRIMROSE 2 trial).

Population:

Women aged ≥ 18 years with ultrasound‐confirmed UFs and HMB (n = 1012).

Methods:

Participants were randomised to linzagolix (100 mg and 200 mg, with and without hormonal add‐back therapy) versus placebo. A post hoc mediation analysis was conducted on the pooled PRIMROSE 1 and PRIMROSE 2 data. The effect of linzagolix versus placebo on pain reduction was divided into three components (effect explained by HMB reduction associated with linzagolix, FV reduction associated with linzagolix, and remaining [not yet explained] treatment effect), with proportions of each component reported.

Main Outcome Measures:

The mediation analysis outcome was clinically significant pain reduction, defined as a change of ≥ 2 pain categories from baseline to Week 24 using the Numeric Rating Scale (pain categories: no pain (0), and mild (1–3), moderate (4–6), severe pain (7–10)).

Results:

In the mediation analysis, 28%–51% (depending on treatment arm) of linzagolix effect on pain reduction was explained by its effect on HMB reduction, while 2%–8% was explained by its effect on FV reduction. The residual proportion ranged between 44% and 67%, depending on treatment arm, and was statistically significant only in the linzagolix 200 mg without add‐back therapy arm (p = 0.002).

Conclusions:

This analysis showed that reductions in pain were significantly mediated by reductions in HMB (all doses) and FV (200 mg alone) in linzagolix‐treated women with UFs. Further research is needed to identify additional mediating factors.

Trial Registration:

ClinicalTrials.gov: NCT03070899 and NCT03070951

2025-06-07·Human Reproduction Open

Two-year follow-up study (PRIMROSE 3) to assess bone mineral density in subjects with uterine fibroids completing the PRIMROSE 1 and PRIMROSE 2 linzagolix trials

Article

作者: Taylor, Hugh ; Becker, Sven ; Carmona Herrera, Francisco ; Petraglia, Felice ; Bestel, Elke ; Becker, Christian ; Donnez, Jacques ; Hori, Satoshi ; Dolmans, Marie-Madeleine ; Paszkowski, Maciej

Abstract:

STUDY QUESTION:

How important was the change in lumbar spine (L1–L4), femoral neck, and total hip bone mineral density (BMD) from post-treatment baseline values to 24 months after the end of treatment in PRIMROSE 1 and PRIMROSE 2 study participants?

SUMMARY ANSWER:

In the present study (PRIMROSE 3), mean percentage changes in lumbar spine BMD from the post-treatment baseline to month 24 (primary endpoint) were small in most treatment groups and similar to variations in the placebo group.

WHAT IS KNOWN ALREADY:

Due to its mechanism of action, some BMD decreases are observed with oral GnRH antagonist treatment, depending on the dose administered and addition or not of add-back therapy (ABT) (1 mg oestradiol and 0.5 mg norethisterone acetate). In PRIMROSE 1 and PRIMROSE 2, no significant changes in BMD were observed in any of the three anatomic sites investigated (lumbar spine, femoral neck, and total hip) in any of the treated groups but one. Indeed, at 24 weeks, mean differences were most pronounced in the lumbar spine in participants given 200 mg linzagolix alone.

STUDY DESIGN, SIZE, DURATION:

PRIMROSE 3 is a long-term follow-up study on BMD in subjects who completed at least 20 weeks of treatment in the main linzagolix trials (PRIMROSE 1 or PRIMROSE 2) and underwent dual-energy X-ray absorptiometry (DEXA) within 35 days of their last treatment (week 24 or week 52 [extension study]). The primary endpoint was the change in lumbar spine (L1–L4), femoral neck, and total hip BMD from post-treatment baseline values to 24 months after the end of treatment in PRIMROSE 1 and PRIMROSE 2 study participants. The secondary endpoint was the change in lumbar spine (L1–L4), femoral neck, and total hip BMD from pre-treatment baseline values to 24 months after the end of treatment. The study involved an eligibility visit and up to three follow-up consultations at 12, 18 and/or 24 months after the end of treatment in either PRIMROSE 1 or PRIMROSE 2.

PARTICIPANTS/MATERIALS, SETTING, METHODS:

Patients given an end-of-treatment DEXA scan within 35 days of their last treatment were invited to participate in the PRIMROSE 3 study. Those who were pregnant or unable to undergo a DEXA scan on the same type of equipment as used for the end-of-treatment DEXA scan in PRIMROSE 1 or PRIMROSE 2 were not eligible for this trial. A total of 137 subjects were screened, 134 (97.8%) of whom were enrolled and 130 (94.9%) included in the safety analysis set. Subject groups were small and ranged from 7 subjects (placebo group) to 30 subjects (200 mg/200 mg+ABT group). Most subjects (n = 110, 80.3%) completed the study by evaluation of their BMD by DEXA at 2 years post-treatment.This study (EudraCT number: 2021-000452-19) was conducted at 3 sites in Bulgaria, 4 sites in the Czech Republic, 4 sites in Hungary, 1 site in Latvia, 6 sites in Poland, 1 site in Romania, 5 sites in Ukraine, and 32 sites in the USA.

MAIN RESULTS AND THE ROLE OF CHANCE:

The most notable percentage increase from the end of treatment to month 24 was in the 200 mg/200 mg+ABT treatment group, which was also the group showing the greatest mean percentage BMD loss during linzagolix treatment. This marked upturn in BMD after cessation of treatment demonstrated the crucial role of ABT.Percentage changes in lumbar spine BMD from the pre-treatment baseline to month 24 (secondary endpoint) remained above −2% in all linzagolix treatment groups. Small BMD modifications observed from both the post-treatment and pre-treatment baseline to month 24 after the end of therapy may not have any clinically relevant impact on overall bone health of linzagolix-treated individuals, since the Z-score of most subjects was within the expected range for age. In addition, changes in BMD values and Z-scores in the linzagolix treatment groups were mostly within the same range as in the placebo group.

LIMITATIONS, REASONS FOR CAUTION:

The number of patients is relatively small. Since interpretation of results from the month-12 and month-18 visits is limited due to the small number of subjects in each treatment arm at corresponding time points, giving rise to high data variability, this manuscript focuses on the month-24 visit only.

WIDER IMPLICATIONS OF THE FINDINGS:

It can be assumed that the small BMD changes observed from both the post-treatment and pre-treatment baseline to month 24 after cessation of therapy may not have any clinically relevant impact on overall bone health of linzagolix-treated individuals.Changes in BMD values and Z-scores in the linzagolix treatment groups were mostly within the same range as in the placebo group, indicating that there are no long-term consequences on BMD after the end of linzagolix treatment.

STUDY FUNDING/COMPETING INTEREST(S):

Funding for the PRIMROSE studies was provided by ObsEva (Geneva, Switzerland). Analysis of data was partially supported by ObsEva (Geneva, Switzerland), Theramex (London, UK), and Kissei (Japan). Grant 5/4/150/5 was awarded to M.-M.D. by the FNRS.J.D. was a member of the scientific advisory board of ObsEva and Preglem until 2023 and reports consulting fees from ObsEva, Gedeon Richter, and Theramex. F.P. has received consulting fees and honoraria for lectures from Theramex. H.T. has received grants from Abbvie, reports consulting fees from ObsEva and Gedeon Richter, has a patent on endometriosis biomarkers owned by Yale University, and was a past president of American Society of Reproductive Medicine (ASRM). C.B. was a member of the independent data monitoring board for the PRIMROSE trials and member of the advisory board for Spirit 1 and 2 trials. He was also the Chair for the ESHRE endometriosis guideline committee. Consulting fees from Myovant and Theramex went to the University of Oxford. S.B. has received consulting fees and honoraria for lectures from Theramex. F.C.H. reports consulting fees and honoraria for lectures, presentations, or educational events from Theramex and Gedeon Richter and receiving honoraria for participation in a data safety monitoring board for Organon. M.P. was a principal investigator in the ObsEva-sponsored PRIMROSE 2 and 3 trials. E.B. and S.H. are employees of Theramex. M.-M.D. has received fees for lectures from Gedeon Richter and Theramex.

TRIAL REGISTRATION NUMBER:

EudraCT number: 2021-000452-19.

项与林扎戈利相关的新闻（医药）

2026-03-24

·allsci.com

Insilico partners with ASKA Pharma on AI-driven target discovery for gynecological diseases

Insilico Medicine and ASKA Pharmaceutical have entered a research collaboration to identify novel therapeutic targets for gynecological conditions including endometriosis, uterine fibroids, and adenomyosis. Cambridge, Massachusetts-based Insilico Medicine (HKEX: 3696), a clinical-stage company using generative AI for drug discovery, will deploy its PandaOmics target identification engine to generate and prioritize candidate targets. Tokyo-based ASKA Pharmaceutical, which focuses on internal medicine, obstetrics, and gynecology, will validate the AI-predicted targets for translational potential. The deal expands an existing relationship in which ASKA has been a user of Insilico’s AI software. Financial terms of the collaboration were not disclosed. The press release does not specify upfront payments, milestone structures, royalties, or equity components. The absence of disclosed economics is consistent with early-stage research collaborations where the primary deliverable is target nomination rather than compound development or clinical advancement. The collaboration operates at the earliest stage of drug discovery: target identification and validation. No specific drug candidate has been named. Insilico will use PandaOmics, its AI-driven biological data analysis platform, which integrates multi-modal omics data and biomedical text mining to generate disease hypotheses and rank candidate targets. The company recently introduced TargetPro, a framework within PandaOmics that builds disease-specific models to predict which targets are most likely to advance into clinical development. ASKA will then apply its gynecological disease expertise to experimentally validate the computationally nominated targets. The three indications covered by the deal represent areas with limited mechanistic diversity in approved therapies. Endometriosis affects approximately 190 million women globally according to World Health Organization estimates. Uterine fibroids and adenomyosis affect larger populations and frequently co-occur. Current pharmacological options include GnRH-based therapies, particularly in endometriosis and uterine fibroids, including AbbVie’s elagolix (Orilissa) and the Myovant Sciences/Pfizer relugolix combination (Myfembree). There is no US FDA-approved drug specifically indicated for adenomyosis; management typically relies on off-label hormonal therapy, symptom control, procedures, or surgery depending on severity and fertility goals. • Elagolix (Orilissa) — AbbVie — marketed for endometriosis pain; AbbVie’s elagolix-containing combination product Oriahnn is marketed for heavy menstrual bleeding associated with uterine fibroids. • Relugolix combination (Myfembree) — Myovant/Pfizer — marketed for endometriosis and uterine fibroids • Linzagolix (Yselty) — Gedeon Richter — marketed in the EU for uterine fibroids and symptomatic endometriosis Your email address will not be published. Required fields are marked * Comment * Name * Email * Website

上市批准

2026-03-08

·和其瑞 Hope Medicine

献给每一位她：关于内异症，你需要知道的6件事

3月8日，是属于每一位女性的节日，在今天，女性谈独立、谈成长、谈爱自己，但有一种痛，却常常被忽视，被一句“痛经嘛，忍忍就过去了”轻描淡写地带过。这种常常被忽视的痛，可能来自一个叫子宫内膜异位症的“隐形敌人”。它常被称为 “不死的癌症”。它不致命，却足以让很多患病女性每个月的那几天变成噩梦；它不罕见，每10位育龄期女性中就有1位患有子宫内膜异位症，却平均要花上4-12年才能被确诊；它不显眼，却可能悄悄偷走你的生育力与生活质量。今天，让我们一起撕掉"忍痛"的标签，认真地认识这位"不死的癌症"。 Q 子宫内膜异位症，到底是一种什么病？ A 简单来说，子宫内膜异位症（简称"内异症"）就是子宫内膜"长错了地方"。正常情况下，子宫内膜长在子宫腔内，随着月经周期脱落出血形成月经。但在内异症患者体内，这些内膜组织"叛逆"地跑到了子宫以外的地方——可能是卵巢、输卵管、盆腔腹膜，甚至是肠道、膀胱或肺部。这些异位的内膜组织依然受激素影响，每个月都会增生、出血，但血液无法排出体外，只能在局部淤积，形成炎症、粘连和囊肿（也就是常说的"巧克力囊肿"）。这个过程就像身体在内部不停地"淤青"和"结疤"，久而久之引发慢性疼痛和各种并发症。 Q 为什么会得这个病？哪些人更容易得？ A 目前医学界的共识是：病因尚未完全明确，很可能是多种因素共同作用的结果。最经典的发病学说是"经血逆流种植"——月经期间，部分经血通过输卵管逆流到盆腔，其中的子宫内膜细胞"安家落户"，在盆腔内生长繁殖。但这只是前提，并非所有经血逆流的女性都会患病，关键还在于免疫系统的"失职"未能及时清除这些异位细胞，以及局部炎症微环境的"纵容"。患病的高危人群特征包括：有家族遗传史（母亲或姐妹患病，风险增加7-10倍）、月经周期短（<27天）或经期长（>7天）、初潮年龄早（<11岁）、从未生育或生育年龄较晚、生殖系统解剖异常导致经血流出不畅等。值得注意的是，该病主要影响育龄期女性，但青春期少女和绝经后女性也可能患病。 Q 这个病严重吗？它会带来哪些困扰？ A 内异症的危害远不止"痛经"这么简单，它可能从生理到心理全方位影响生活质量，主要包括：（1）疼痛"三重奏"，表现为进行性加重的痛经，从月经前1-2天开始，持续整个经期，止痛药效果越来越差；慢性盆腔痛，非经期也存在的隐痛、坠痛，长期折磨；性交痛和排便痛，深部浸润型内异症患者在性生活或排便时疼痛明显。（2）生育路上的"拦路虎"。约30%-50%的内异症患者合并不孕。异位病灶会导致盆腔粘连、输卵管堵塞、卵巢储备功能下降，同时，炎症环境也会影响卵子和胚胎质量。（3）全身性影响。长期慢性疼痛可导致焦虑、抑郁、睡眠障碍、性功能障碍，甚至影响工作效率和社交生活。有研究显示，内异症患者的生产力损失相当于每月损失1-2个工作日。（4）恶变风险。虽然概率较低（约1%），但长期存在的内异症病灶（特别是卵巢巧克力囊肿）有恶变为子宫内膜样癌或透明细胞癌的风险。 Q 怎样才能知道自己是不是得了这个病？做什么检查能确诊？ A 内异症的诊断是一场"医学侦探工作"，需要结合症状、体征和辅助检查。首先，自我觉察症状和及时就医非常重要。如果出现痛经逐渐加重，需要卧床休息或影响工作学习、非经期盆腔疼痛或性交疼痛，需寻求医生帮助。在就诊时，医生通过妇科检查可触及盆腔内的触痛结节、子宫活动度受限或附件区包块。同时，医生会结合超声检查（可发现卵巢巧克力囊肿、盆腔粘连等）或磁共振检查评估盆腔深部的内异症（如肠道、输尿管受累）。目前，唯一能够100%确诊的方法是腹腔镜手术+病理活检。医生通过微创手术直接观察盆腔内病灶，取组织送病理检查，看到内膜腺体和间质即可确诊。值得提醒的是，不要因为"怕手术"而拖延就诊，早期诊断有助于早期干预和改善预后。 Q 这个病能治好吗？有哪些传统治疗方法？ A 内异症目前无法治愈。目前，内异症治疗的目的包括：减灭和消除病灶、减轻和消除疼痛、改善和促进生育、减少和避免复发。传统治疗方式包括药物治疗和手术治疗。药物治疗包括非甾体类抗炎药和激素类药物。非甾体类抗炎药对轻中度疼痛效果较好，但长期应用易导致胃溃疡及增加心血管事件风险。激素类药物包括口服避孕药、高效孕激素、雄激素衍生物以及促性腺激素释放激素激动剂（GnRH-a，即"假绝经疗法"），此类药物通过抑制卵巢功能，降低体内雌激素水平，导致子宫内膜萎缩，改善内异症的症状。激素类药物的副作用包括抑郁、骨质丢失、潮热出汗、突破性出血、乳房胀痛、体重增加和血栓风险增加等。停药后5年复发率可达50%。手术治疗主要是腹腔镜下病灶切除、囊肿剥除、粘连松解等，严重者可能需要子宫切除。内异症很难通过手术清除全部病灶，术后复发十分普遍。 Q 除了传统的治疗方法，目前有什么新药或研发新进展吗？ A 近年来，GnRH拮抗剂类药物在国外逐步被批准用于治疗中重度内异症疼痛，包括elagolix、relugolix和linzagolix。这类药物通过阻断GnRH受体，降低雌激素水平发挥疗效。在国内，目前已有GnRH拮抗剂的3期临床研究在开展中。由于GnRH拮抗剂通过抑制雌激素而发挥疗效，会导致围绝经期症状、骨质丢失等副作用，用药时长不能超过两年。目前，非激素类靶向药物也在加速研发中，包括和其瑞的主要管线产品HMI-115，一种靶向泌乳素受体的单克隆抗体。HMI-115不抑制雌激素，而是通过抗炎、抗细胞增殖和抑制痛觉敏化等机制发挥疗效。HMI-115已被中国国家药品监督管理局（NMPA）药品评审中心（CDE）纳入突破性治疗药物品种名单（BTD），以及获得美国食品药品监督管理局（FDA）授予快速通道资格认定（Fast Track Designation, FTD）。 HMI-115已完成一项治疗子宫内膜异位症相关的中重度疼痛的全球2期临床试验。在这项国际多中心、随机、双盲、安慰剂对照研究中，评估了108例经手术确诊的子宫内膜异位症患者接受12周的HMI-115治疗的安全性与疗效，患者来自美国、波兰和中国。结果显示，HMI-115显著改善子宫内膜异位症相关的痛经、非月经期盆腔疼痛评分，较安慰剂组的差异具有统计学显著性。HMI-115的整体耐受性和安全性良好，未发生与HMI-115治疗相关的严重不良事件，在治疗期间，患者维持正常性激素水平、月经模式和骨密度。试验结果于2025年11月发表于《柳叶刀-妇产科学与女性健康》（The Lancet Obstetrics, Gynaecology & Women’s Health）。在国内，HMI-115治疗子宫内膜异位症相关的中重度疼痛的3期临床试验正在启动。远离病痛，拥抱美好人生在这个属于女性的节日里，我们想说：你的痛，不需要忍。如果你或身边的亲友姐妹正被内异症困扰，请记住——它不是"娇气"，不是"矫情"，而是一种真实存在的疾病。医学在进步，新的治疗选择正在不断涌现。关注身体发出的信号，及时就医，是对自己最好的关爱。愿每一个她都不再独自忍耐病痛，我们呼吁更多的妇科疾病被看见、被关注，让女性更好地认识自己的身体，远离疾病困扰，拥抱未来与希望。关于和其瑞医药和其瑞医药是一家科学驱动的临床阶段创新生物制药公司，在中国北京、上海和南京设有研发基地及办公室。公司的创立是基于北京大学未来技术学院院长肖瑞平教授及其团队在转化医学研究领域的深入理解及数十年的研究成果。和其瑞以卓越科学研究为基础，以改善生命质量为目标，针对威胁人类健康的常见病和重大疾病，致力于研究、开发和商业化首创新药。参考文献： 1.子宫内膜异位症诊治指南（第三版）. 中华妇产科杂志, 2021, 56 (12):812-824. 2.子宫内膜异位症长期管理中国专家共识. 中华妇产科杂志, 2018, 53 (12):836-841. 3.促性腺激素释放激素拮抗剂在子宫内膜异位症治疗中的应用. 中华妇产科杂志, 2023, 58 (1)70-73. 4.Endometriosis: A Review. JAMA. 2025 Jul 1;334(1):64-78. 5.Global and regional trends in the burden of surgically confirmed endometriosis from 1990 to 2021. Reprod Biol Endocrinol. 2025 Jun 7;23(1):88. 6.ESHRE guideline: endometriosis. Human Reproduction Open, pp. 1–26, 2022. 7.Prolactin and pain of endometriosis. Pharmacol Ther. 2023 Jul;247:108435. 联系我们运营团队办公室上海市浦东新区亮秀路112号Y1座项目及媒体联系pr@hopemedinc.com 人才招聘hopemed.hr@hopemedinc.com 年轻的和其瑞期待您的加入！共同成就源头创新，走向全球！有志者，请与我们联系！

疫苗

2025-12-04

·孕育前线

子宫内膜异位症的治愈之路何在？

子宫内膜异位症，这一影响全球约1.9亿女性与女孩的疾病，始终面临着“研究不足、无药可愈”的困境。其核心病理是子宫内膜样组织在子宫外异常增殖，引发剧烈盆腔疼痛、月经过多，更有50%的患者会遭遇生育难题。尽管它困扰着十分之一的育龄人群，但其研究关注度与资金支持却长期处于“被忽视”状态——美国国立卫生研究院对糖尿病、乳腺癌的 funding 分别是它的15倍和30倍，即便是罕见病克罗恩病，每位患者获得的研究资金也高达其65倍。这种资源失衡导致患者平均需等待8年才能确诊，而现有激素疗法无法解决不孕，手术切除病灶的复发率更是高达50%，每年仅美国就因此产生780亿至1200亿美元的经济损失。值得欣慰的是，近年来该领域的研究终于迎来转机，不仅多款创新药物进入临床阶段，Dim（二吲哚甲烷）与生育酶等新兴方向也逐渐进入科研视野，为患者带来新的希望。研究困局：资金匮乏下的临床挑战 Hera Biotech联合创始人Bruce Nicholson直言，研究资金的长期短缺是子宫内膜异位症治疗进展缓慢的关键。2025年Organon公司的OG-6219二期试验失败，更是给患者群体带来沉重打击——这款靶向HSD17B1酶的小分子药物，本希望通过抑制子宫壁组织异常生长缓解疼痛，却因未达主要终点被迫终止开发。但困境之下，行业对女性健康的关注度正在觉醒。Gesynta Pharma完成2700万美元B轮融资、Cyclana Bio筹集500万英镑用于药物研发，这些投资信号预示着女性医疗保健领域的变革。正如Innovestor合伙人Pekka Simula所言：“大型制药公司终于意识到，世界一半人口是女性。” 药物突破：口服制剂与靶向疗法的崛起 Linzagolix：口服给药革新治疗体验 2025年，日本Kissei公司研发的linzagolix成为焦点——继英国NHS批准后，该药又在中国台湾获批，不仅适用于子宫肌瘤，更为子宫内膜异位症患者提供了便捷的治疗选择。作为促性腺激素释放激素受体拮抗剂，它能阻断与病灶生长相关的激素过量分泌，搭配低剂量激素替代疗法，可在显著缓解痛经与盆腔疼痛的同时，避免更年期症状和骨质流失。与传统注射类药物不同，这款每日一次的口服药片让患者无需频繁往返诊所，真正实现了“居家掌控健康”。此前，英国与欧盟批准的口服药物relugolix（商品名Ryeqo）已开创先河，其将GnRH受体拮抗剂与附加疗法合二为一的设计，同样为患者带来了便利。两款口服制剂的接连获批，标志着子宫内膜异位症治疗正在告别“注射依赖”。 HMI-115：非激素靶点的疼痛克星上海和其瑞医药的HMI-115在二期试验中取得重大突破，这款单克隆抗体以催乳素受体为靶点，实现了“不干扰性激素却能缓解疼痛”的突破。试验数据显示，它能使痛经疼痛减轻42%，非经期盆腔疼痛下降52%。北京协和医院妇科主任朱兰指出，催乳素受体过度表达与子宫内膜异位症密切相关，且高催乳素水平会降低女性疼痛阈值，而HMI-115通过阻断该受体，既避免了更年期副作用，又不会影响生育功能，有望彻底改变治疗模式。目前，该药已计划启动全球三期试验。 Vipoglanstat：抑制炎症的小分子新贵瑞典Gesynta Pharma的vipoglanstat获英国药监局批准进入二期临床试验。这款小分子药物通过抑制特定酶的活性，减少促炎分子前列腺素E2的生成，从而阻断病灶进展与疼痛传导。临床前研究已证实其能有效下调子宫内膜异位病灶，而2700万美元的融资则为其临床推进提供了有力支撑。跨界探索：老药新用与天然疗法的潜力二氯乙酸：癌症药物的“跨界尝试”子宫内膜异位症患者体内会过量产生乳酸，这种代谢副产品会加速异常细胞增殖。研究发现，常用于治疗癌症的二氯乙酸能有效降低乳酸水平，抑制病灶扩散。爱丁堡大学的动物实验显示，该药可使病灶在七天内缩小，目前已进入人体临床试验阶段，为“老药新用”提供了典型范例。大麻：疼痛管理的新可能澳大利亚西悉尼大学正在开展双盲随机对照试验，探索药用大麻对子宫内膜异位症疼痛的缓解作用。早期研究显示，59%的患者使用大麻后可摆脱止痛药依赖，其机制可能与调节内源性大麻素系统、抑制炎症相关。Ananda Pharma的MRX1 CBD候选药物也已启动临床试验，计划在100名患者中验证其镇痛效果。新兴方向：Dim与生育酶的研究新视角在创新药物不断涌现的同时，Dim（二吲哚甲烷）与生育酶的相关研究为子宫内膜异位症治疗开辟了新路径。Dim是十字花科蔬菜中的天然活性成分，研究发现其具有调节雌激素代谢、抑制异常细胞增殖的作用——子宫内膜异位症的发生与雌激素失衡密切相关，Dim可通过调节芳香化酶活性，减少雌激素对异位病灶的刺激，同时增强机体抗氧化能力，减轻盆腔炎症反应，为缓解疼痛和延缓病灶进展提供辅助支持。而生育酶的作用则聚焦于患者的生育难题。子宫内膜异位症患者常存在输卵管纤毛运动异常、盆腔微环境紊乱等问题，导致受精与着床困难。相关研究表明，补充特定生育酶（如透明质酸酶、菠萝蛋白酶等）可改善盆腔局部血液循环，降解粘连组织与炎性渗出物，优化生殖系统微环境；同时，这些酶类还能调节子宫内膜容受性，增强卵子与精子的结合能力，为有生育需求的患者提供新的辅助治疗思路。目前，关于Dim与生育酶联合应用于子宫内膜异位症的临床研究正在推进，有望为患者提供“控痛+助孕”的双重解决方案。诊断革新：早发现才能早干预治疗的突破离不开诊断技术的支撑。子宫内膜异位症拖延诊断时间越长，病灶侵袭越严重，可能引发瘢痕组织、粘连、囊肿等并发症，增加治疗难度。法国Ziwig公司的Endotest诊断器械，通过检测唾液中的microRNA（子宫内膜异位症中会出现失调），实现了便捷无创的筛查；巴黎Endogene Bio推出的经血检测方法，可在数周内完成诊断，为早期干预提供了可能。这些创新工具的出现，有望缩短诊断周期，让患者在病情初期就能获得有效治疗。总结：困境中突围，希望在前方尽管OG-6219的失败仍让人惋惜，但linzagolix、HMI-115等药物的获批与推进，Dim、生育酶等新兴方向的探索，以及诊断技术的革新，都预示着子宫内膜异位症的治疗格局正在改变。随着女性健康关注度的提升、研究资金的增加，曾经“被忽视”的领域正迎来前所未有的发展机遇。未来，随着多靶点药物、跨界疗法与辅助干预手段的深度融合，有望为患者提供兼具“控痛、抑灶、保生育”的综合解决方案，让这一致衰性疾病不再成为女性健康的“绊脚石”。相关阅读腺肌、内异症整体自然疗法，一条自救之路逆转子宫内膜异位症不孕的5个步骤子宫腺肌症、内膜异位症、肌瘤不想开刀，这招全身酶疗法送给有缘人解锁8大秘密武器：自然舒缓子宫内膜异位症&腺肌症疼痛 Endok™宫巢净化三剑客+草本茶：生殖系统深度净化调养

100 项与林扎戈利相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11609	-	-	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
子宫肌瘤	日本	Kissei Pharmaceutical Co., Ltd.	2025-12-22
子宫内膜异位症	欧盟	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	冰岛	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	列支敦士登	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	挪威	Theramex Ireland Ltd.	2024-12-20
平滑肌瘤	欧盟	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	冰岛	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	列支敦士登	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	挪威	Theramex Ireland Ltd.	2022-06-14

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
疼痛	临床3期	日本	Kissei Pharmaceutical Co., Ltd.	2022-10-11
Primrose 综合征	临床3期	-	-	2021-08-30
月经过多	临床3期	美国	ObsEva SA	2017-04-20
卵巢过度刺激综合征	临床2期	中国	上海葆正医药科技有限公司	2023-08-01
Cohen综合征	临床2期	中国	上海葆正医药科技有限公司	2022-09-27
Cohen综合征	临床2期	中国	Kissei Pharmaceutical Co., Ltd.	2022-09-27
女性不孕症	临床2期	中国	Kissei Pharmaceutical Co., Ltd.	2022-09-27
女性不孕症	临床2期	中国	上海葆正医药科技有限公司	2022-09-27
肝损伤	临床1期	美国	ObsEva SA	2019-05-15

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03070951 \| NCT03070899 (PRIMROSE 2, Pubmed \| Fertil Steril)	临床3期	子宫肌瘤	1,012	Linzagolix 100 mg	鏇廠艱鑰積繭鹹淵範觸(製鹹構構廠廠遞簾餘鹽) = hot flushes 膚衊選夢糧淵網艱艱積 (齋憲糧齋網衊淵範獵衊 ) 更多	积极	2025-10-01
				Linzagolix 100 mg with ABT
NCT04372121 (EDELWEISS 5, CTgov)	临床3期	子宫内膜异位症	30	LGX (LGX 75 mg)	觸窪築窪願簾範顧繭簾(夢鑰遞壓築餘積築築繭) = 繭餘顧積蓋獵窪襯積齋鑰獵鏇蓋積壓艱繭憲製 (壓膚壓夢壓餘壓積繭艱, 0.0) 更多	-	2025-03-19
				LGX (LGX 200 mg+ABT)	觸窪築窪願簾範顧繭簾(夢鑰遞壓築餘積築築繭) = 齋鏇鹽膚憲遞淵糧襯襯鑰獵鏇蓋積壓艱繭憲製 (壓膚壓夢壓餘壓積繭艱, 0.0) 更多
NCT03986944 (CTgov)	临床3期	子宫内膜异位症	85	Placebo capsule to match Add-back capsule	繭鏇鏇鑰鬱構獵膚衊餘(淵廠鬱積壓簾構製憲選) = 膚蓋選鏇積糧簾餘顧糧構獵簾遞鹹構網糧襯鹹 (窪淵艱鬱窪選製築鹽襯, 0.5) 更多	-	2024-10-29
NCT05445167 (KLH2302, NEWS)	-	子宫肌瘤	89	Linzagolix	膚網窪簾齋衊憲壓齋醖(襯壓構蓋鏇鏇鏇憲觸鹹) = Clinical results have reached the endpoint 糧蓋蓋顧製鏇築衊選壓 (繭餘簾鹽襯選醖齋鬱廠 )	积极	2024-07-16
				安慰剂
NCT03992846 (EDELWEISS 3, CTgov)	临床3期	子宫内膜异位症	486	Placebo capsule to match Add-back capsule	選糧艱網願製廠網顧製 = 膚窪廠鏇廠壓餘衊艱製鹽壓繭夢鏇壓網鑰憲鏇 (醖廠鹹鬱醖範繭糧獵構, 餘淵範製襯壓構夢夢構 ~ 艱製膚遞願壓鬱選願糧) 更多	-	2024-05-29
NCT04335591 (CTgov)	临床3期	子宫内膜异位症	356	LGX (LGX 75 mg)	鑰衊蓋憲製觸壓廠壓壓 = 觸網醖繭構夢觸餘蓋醖壓鏇鏇遞網鑰憲獵鑰獵 (鑰鬱襯鑰餘膚餘廠積廠, 願簾願壓積遞顧鹹淵膚 ~ 襯網構鹽簾夢獵鑰築獵) 更多	-	2024-04-30
				LGX (LGX 200 mg+ABT)	鑰衊蓋憲製觸壓廠壓壓 = 築鹹構艱鏇獵夢觸繭壓壓鏇鏇遞網鑰憲獵鑰獵 (鑰鬱襯鑰餘膚餘廠積廠, 願積觸衊衊夢簾鹹衊鏇 ~ 範鹽選廠壓蓋獵願願願) 更多
NCT03992846 (EDELWEISS 3, Pubmed)	临床3期	子宫内膜异位症 \| 疼痛一线	486	Placebo	齋鑰夢鹽鬱淵窪憲觸簾(構壓簾齋齋鏇網顧壓遞) = 窪選構築鏇齋齋鏇鬱範憲蓋蓋觸蓋構鹽顧齋鏇 (簾艱獵繭網顧鏇簾願選 )	积极	2024-04-22
				Linzagolix 75 mg	齋鑰夢鹽鬱淵窪憲觸簾(構壓簾齋齋鏇網顧壓遞) = 網鏇糧構鑰網壓廠網夢憲蓋蓋觸蓋構鹽顧齋鏇 (簾艱獵繭網顧鏇簾願選 )
NCT03070951 (PRIMROSE 2, GlobeNewswire) 人工标引	临床3期	子宫肌瘤	535	add-back therapy+linzagolix	蓋鬱艱獵夢憲醖衊糧淵(鹽繭獵選鏇範簾窪蓋選) = 憲壓餘壓範積範願夢製鹽築獵襯簾鏇鹹構廠獵 (積夢選壓獵鹽構鬱構壓 )	积极	2020-07-06
				linzagolix	蓋鬱艱獵夢憲醖衊糧淵(鹽繭獵選鏇範簾窪蓋選) = 蓋遞築選構襯製網衊遞鹽築獵襯簾鏇鹹構廠獵 (積夢選壓獵鹽構鬱構壓 )