主要研究目的：研究空腹状态下单次口服受试制剂艾拉戈克钠片（规格：200 mg，常州制药厂有限公司生产）与参比制剂艾拉戈克钠片（ORILISSA®，规格：200 mg，AbbVie Inc.生产）在健康参与者体内的药代动力学特征，评价空腹状态口服两种制剂的生物等效性。次要研究目的：研究受试制剂艾拉戈克钠片（规格：200 mg）和参比制剂艾拉戈克钠片（ORILISSA®，规格：200 mg）在健康参与者中的安全性。

开始日期2026-03-01

申办/合作机构

常州制药厂有限公司

CTRI/2025/11/096880

/ Not yet recruitingN/A

Reducing endometriosis-related pain with ELagolix (T. Evagolix): Investigation of EFficacy and saFety - RELIEF STUDY

开始日期2025-11-21

申办/合作机构

CORONA Remedies Ltd.

CTRI/2025/05/087630

/ Not yet recruitingN/AIIT

An observational study evaluating the efficacy of elagolix versus multi-drug regimen for the prevention of ovarian hyperstimulation syndrome (OHSS) - OHSS trial

开始日期2025-06-06

申办/合作机构-

100 项与噁拉戈利钠相关的临床结果

登录后查看更多信息

100 项与噁拉戈利钠相关的转化医学

登录后查看更多信息

100 项与噁拉戈利钠相关的专利（医药）

登录后查看更多信息

184

项与噁拉戈利钠相关的文献（医药）

2026-05-01·EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS

Atypical gelation of Elagolix sodium in aqueous media: Mechanistic insights and Inhibition via coamorphization

Article

作者: Qian, Shuai ; Zhang, Jianjun ; Wei, Yuanfeng ; Su, Meiling ; Shen, Peiya ; Gao, Yuan ; Shi, Jitong ; Zhang, Xiaohua ; Tang, Mi

Elagolix sodium (ELS), a non-peptide oral gonadotropin-releasing hormone receptor (GnRH) antagonist approved for the treatment of endometriosis-associated pain, displays atypical gelation in aqueous environments along with challenging physical properties such as high hygroscopicity. To address the formulation challenges posed by ELS gelation and high hygroscopicity, this study not only investigates the molecular mechanisms governing ELS gel formation but also evaluates co-amorphization with quercetin as a practical strategy to suppress gelation and enhance stability. Unlike conventional gelation mechanisms of small molecules, ELS was found to self-assemble into a metastable spherulitic gel network in aqueous media, where water molecules acted as critical "binders" for both initiation and stabilization. Comprehensive morphological, thermal, spectroscopic, and rheological analyses were employed to elucidate ELS gelation process. Polarized light microscopy (PLM) revealed that the hydrogel consists of transient spherulite domains, while Fourier Transform Infrared Spectroscopy (FTIR), Raman spectroscopy and Liquid-state ¹H nuclear magnetic resonance spectroscopy (¹H NMR) demonstrated that gel formation is driven by a combination of dipole-dipole electrostatic interactions and π-π stacking between ELS molecules, along with intermolecular hydrogen bonding between ELS and water. Rheological studies further confirmed a temperature-dependent transition from fibrous structure to a densely cross-linked spherulitic network, indicating enhanced gel strength at lower gelation temperatures. Coamorphization of ELS with quercetin (QUE) not only completely inhibits gelation but also significantly reduces the hygroscopicity of ELS. Overall, this study provides fundamental insights into the mechanism of atypical small-molecule gelation while offering a practical strategy to overcome gelation challenges in the formulation and processing of ELS-based pharmaceuticals.

2026-03-01·JCPSP-Journal of the College of Physicians and Surgeons Pakistan

Comparison of Letrozole with Elagolix for the Management of Endometriosis-Associated Pain: A Quasi-Experimental Study

Article

作者: Hussain, Ujala ; Iqbal, Sofia ; Irshad, Hina ; Nasir-Ud-Din, Alia ; Munir, Shamila Ijaz

OBJECTIVE:

To compare the efficacy of Letrozole and Elagolix in the medical management of endometriosis-associated pain Study Design: A quasi-experimental study. Place and Duration of the Study: Department of Obstetrics and Gynaecology, Fatima Jinnah Medical University/Sir Ganga Ram Hospital, Lahore, Pakistan, from March to August 2025.

METHODOLOGY:

Women presenting with endometriosis-related pain were allocated to treatment groups. Patients in Group A (n = 29) received oral Letrozole 2.5 mg, while patients in Group B (n = 30) received oral Elagolix 150 mg once daily for three months. VAS pain scores were recorded before and 3 months post-intervention, and compared between the Letrozole and Elagolix groups using an independent samples t-test and chi-square test.

RESULTS:

Baseline data were comparable between the study groups (all p > 0.05). At 3 months post-intervention, the Elagolix group showed a significantly lower VAS score for dyspareunia (3.6 ± 2.2 vs. 4.7 ± 0.9; p = 0.016) and a greater reduction in dysmenorrhoea scores (2.2 ± 0.9 vs. 1.4 ± 1.8; p = 0.048). A shift from severe to mild was evident with significant improvements in pelvic pain (p = 0.043) and dysmenorrhoea (p = 0.036). Stratified analysis revealed significantly greater reductions in dysmenorrhea scores among Elagolix users aged ≤29 years (p = 0.025), with BMI <25 kg/m2 (p = 0.013) and regular menstrual cycles (p = 0.027). Pelvic pain scores also improved significantly in participants with a monthly household income of ≥ 50,000 PKR (p = 0.037).

CONCLUSION:

Elagolix demonstrated greater efficacy than Letrozole in reducing endometriosis-related pain after three months of treatment. This efficacy was more evident for dysmenorrhoea among specific patient subgroups, including those with younger age, lower BMI, or regular menstrual periods.

KEY WORDS:

Elagolix, Endometriosis, Letrozole, VAS pain.

2026-02-01·AJOG global reports

Safety of 48 months of elagolix with add-back therapy for endometriosis-associated pain

Article

作者: Kim, Jin Hee ; Thomas, James W ; Chan, Anna ; Miller, Charles E ; Simon, James A ; Snabes, Michael C

Background:

Elagolix (ELA) 200 mg twice daily is an oral treatment approved for moderate-to-severe endometriosis-associated pain. However, the clinical use of ELA is limited by potential hypoestrogenic effects, including the loss of bone mineral density (BMD). The addition of hormonal add-back (AB) therapy (1-mg estradiol/0.5-mg norethindrone acetate once daily) may attenuate BMD loss.

Objectives:

To provide long-term safety results from a 48-month phase 3 trial assessing ELA+AB therapy in premenopausal women with moderate-to-severe endometriosis-associated pain.

Study Design:

This multicenter, phase 3 trial was conducted between July 7, 2017, and December 6, 2023, and included a 12-month double-blind treatment period, a 36-month open-label extension period, and a 12-month post-treatment follow-up (PTFU) period. At the beginning of the double-blind period, premenopausal women (aged 18-49 years) with moderate-to-severe endometriosis-associated pain were randomized 4:1:2 to ELA+AB therapy, ELA monotherapy for 6 months followed by ELA+AB therapy for the remaining 6 months, or placebo. After the double-blind treatment period, all patients were treated with open-label ELA+AB therapy (referred to as the ELA+AB/ELA+AB, ELA/ELA+AB, and placebo/ELA+AB groups) for the remainder of the 36-month open-label treatment period. Safety was assessed throughout the open-label treatment period. BMD was measured by dual-energy X-ray absorptiometry in the lumbar spine, total hip, and femoral neck during the screening period and every 6 months throughout the study. BMD was analyzed using an analysis of covariance model with treatment as the main effect and baseline values as covariates.

Results:

Among 380 patients who entered the open-label period, 140 (36.8%) completed the treatment period, and 240 (63.2%) discontinued, primarily due to withdrawn consent and adverse events (AEs). In total, 159 (74.0%) patients in the ELA+AB/ELA+AB group, 41 (69.5%) patients in the ELA/ELA+AB group, and 80 (75.5%) patients in the placebo/ELA+AB group reported at least 1 treatment-emergent adverse event (TEAE) during the open-label period. TEAEs were generally mild or moderate and nonserious. The most commonly reported TEAEs were COVID-19, bone density decreases, and sinusitis. No serious AEs were reported in >1 patient in any study group. BMD remained generally stable, with a least squares mean percent decrease from baseline to week 48 <2% in all groups and at all anatomical sites. Similarly, the least squares mean decrease from baseline in BMD was <2% in the ELA+AB/ELA+AB group at all anatomical sites and all time points throughout the study period. For patients in the ELA+AB/ELA+AB group with ≥48 months of treatment and reduced BMD at the final on-treatment visit, the majority (lumbar spine, 13 [59.1%]; total hip, 8 [53.3%]; femoral neck, 12 [57.1%]) partially or fully recovered at month 12 of the PTFU period.

Conclusions:

This study extends findings from a previously reported 12-month analysis of the efficacy and safety of ELA+AB therapy in premenopausal women with moderate-to-severe endometriosis-associated pain. The safety profile of ELA+AB therapy was generally consistent with that observed in prior studies. BMD remained mostly stable through 48 months of continuous treatment. This analysis represents the longest safety study of ELA+AB therapy to date and supports long-term treatment with ELA+AB therapy.

项与噁拉戈利钠相关的新闻（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

2026-03-02

·东方科软

【Discovery Studio文献解读】GnRH1R与小分子拮抗剂elagolix结合模式分析

努力做到技术一流坚持做好服务一流 400-886-8338 01 文献解读 GnRH1R 是视紫红质类 G 蛋白偶联受体（GPCR），调控下丘脑 - 垂体 - 性腺（HPG）轴，是不孕、子宫内膜异位症、前列腺癌等疾病的重要药物靶点。已有 elagolix、relugolix 等小分子拮抗剂获批或进入临床试验，但GnRH1R 与配体相互作用的分子机制缺乏结构学证据，限制了药物优化。GnRH1R晶体结构包含7个跨膜螺旋（TM），但缺失胞质 C 端螺旋（ helix 8），与其他 A 类 GPCR 存在差异。晶体结构为非活性构象，TM5 和 TM6 向内移动，缩小了G蛋白结合腔。口袋由 N 端、TM2、TM3、TM5-TM7 构成，呈扩大状态，允许 elagolix 与受体 N 端（18-33 位氨基酸）共占据，N 端在晶体和分子动力学模拟中稳定性高，仅参与小分子拮抗剂结合，不影响激动剂（GnRH）的信号传导。 Discovery Studio在本文中的应用：由于研究已解析了 GnRH1R 与 elagolix 的晶体结构，但需进一步明确同类小分子拮抗剂（如已获批的 relugolix、在研的 sufugolix）与 GnRH1R 的结合差异，尤其是这些拮抗剂因 “臂 2” 结构延长（如 relugolix/sufugolix 的甲氧基苯基脲基团）可能产生的结合适应性，因此通过分子对接模拟补充结构学证据，解释不同化学型拮抗剂的结合机制一致性与差异性。Discovery Studio 软件通过其内置的CDOCKER程序应用于分子对接实验，核心目的是解析除 elagolix 外的其他临床相关 GnRH1R 拮抗剂（如 relugolix、sufugolix）的结合模式，验证 GnRH1R 正构结合口袋的可塑性，为药物设计提供结构依据。其具体应用过程及细节如下：为确保对接模型接近野生型 GnRH1R 的生理状态，需先对晶体结构进行优化，步骤包括：移除晶体结构中的PGS 融合蛋白（用于结晶的热稳定结构域），并将之前为提高稳定性引入的P128³.³⁹K 突变恢复为野生型（避免突变影响配体结合位点）；对受体中缺失的胞外环 2（ECL2）和胞内环（ICLs）区域，使用 MODELLER 模块进行从头建模（ab initio modeling），补全受体结构；按标准流程对受体进行预处理（如加氢、优化电荷分布），确保结合口袋区域的结构完整性，为对接提供准确的受体模型。针对 relugolix 和 sufugolix 两种拮抗剂，配体通过优化其原子坐标后，确保配体构象能量最低，接近生理状态下的结合构象，再将优化后的配体结构导入 Discovery Studio，用于后续对接。本文中的Discovery Studio的CDOCKER程序（基于 CHARMM 力场的分子动力学对接算法）核心参数与逻辑包括：以 GnRH1R 与 elagolix 结合的正构口袋为对接区域（明确配体结合的空间范围，确保对接结果针对性）；通过分子动力学模拟生成配体的多种可能构象，并基于结合能评分（如 CDOCKER Energy）筛选出与受体结合亲和力最高的构象（即 “top-ranked pose”）；对接过程中考虑受体与配体间的疏水作用、氢键、范德华力等非共价相互作用。 CDOCKER分子对接结果分析，构象一致性验证：对接结果显示，relugolix 和 sufugolix 的噻吩并嘧啶核心与 elagolix 的尿嘧啶核心重叠，且 “臂 1”“臂 3” 的结合位置与 elagolix 高度一致，证实了同类拮抗剂结合模式的保守性；结构差异性分析：发现两种拮抗剂的 “臂 2”（含更长的甲氧基苯基脲基团）可占据比 elagolix 更大的口袋空间，受体的 N 端和 ECL1 区域会发生构象摆动，TM7 胞外区向外移动，形成适配 “臂 2” 的扩展 cavity；同时，受体残基 R38和 H306与 “臂 2” 形成强氢键，解释了其高亲和力的结构基础。后续验证：将对接得到的最优构象进一步通过 200 ns 分子动力学（MD）模拟验证稳定性，确认受体- 配体复合物在动态过程中仍能维持关键相互作用，增强对接结果的可信度。通过分子模拟与实验结合，明确了GnRH1R “N 端 - 小分子共占据” 的独特结合模式，解释了不同化学型拮抗剂（elagolix、relugolix、sufugolix）的结合共性与差异，为药物优化提供了原子级靶点，如针对臂 2 的扩展口袋设计更长侧链配体，利用受体构象可塑性提升亲和力。同时揭示了 GnRH1R 在微开关元件、极性网络等方面与其他 A 类 GPCR 的差异，丰富了 GPCR 结构生物学理论体系，为同类无 C 端螺旋 GPCR 的研究提供参考范式。为性激素依赖性疾病（如子宫内膜异位症、前列腺癌、子宫肌瘤）的药物研发提供了精准方向，可基于明确的关键结合残基设计高选择性、口服有效的新型 GnRH1R 拮抗剂。参考文献： Yan, W., Cheng, L., Wang, W. et al. Structure of the human gonadotropin-releasing hormone receptor GnRH1R reveals an unusual ligand binding mode. Nat Commun 11, 5287 (2020). https://doi.org/10.1038/s41467-020-19109-w 02 往期阅读【Discovery Studio文献解读】新型分枝杆菌 F-ATP 合酶抑制剂的发现及其与二芳基喹啉联合使用的效力【Discovery Studio文献解读】双抗聚集体无影踪，药明生物现神功【Discovery Studio文献解读】结核杆菌FtsZ抑制剂计算药理学研究【Discovery Studio文献解读】抗体可开发性预测-基于Discovery Studio计算描述符的机器学习【Discovery Studio文献解读】抗体工程Discovery Studio 如何助力平衡 “电荷-亲和力” 【Discovery Studio文献解读】抗体工程片段降低预存ADA的理性设计【Discovery Studio文献解读】Discovery Studio抗原表位鉴定中的应用【Discovery Studio文献解读】抗体成药性表征中的电荷变体分析分子模拟方法【Discovery Studio文献解读】Fab影响ADCC效应的结构分析【Discovery Studio文献解读】非催化抗体转化催化抗体的作用机制研究【Discovery Studio文献解读】NadDsg酶底物选择性的理性设计 03 购买软件杨经理 18911931394 相关软件问题可咨询杨经理

100 项与噁拉戈利钠相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D09336	噁拉戈利钠	H01CC03	DBSALT002117

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
疼痛	加拿大	AbbVie, Inc.	2018-10-05
子宫内膜异位症	美国	AbbVie, Inc.	2018-07-23

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
中度疼痛	临床3期	中国	齐鲁制药（海南）有限公司	2022-09-04
重度疼痛	临床3期	中国	齐鲁制药（海南）有限公司	2022-09-04
痛经	临床3期	美国	AbbVie, Inc.	2020-08-10
月经过多	临床3期	美国	AbbVie, Inc.	2015-12-22
月经过多	临床3期	加拿大	AbbVie, Inc.	2015-12-22
子宫肌瘤	临床3期	美国	AbbVie, Inc.	2015-12-22
子宫肌瘤	临床3期	加拿大	AbbVie, Inc.	2015-12-22
多囊卵巢综合征	临床2期	美国	AbbVie, Inc.	2019-08-12
不孕	临床1期	美国	AbbVie, Inc.	2020-09-01
绝经期综合征	临床1期	美国	AbbVie, Inc.	2011-06-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03271489 (CTgov)	临床3期	月经过多 \| 子宫肌瘤	478	Elagolix+Estradiol /norethindrone acetate (E2/NETA) (Elagolix Plus Estradiol (E2)/Norethindrone Acetate (NETA))	範鬱繭夢積淵淵願積簾 = 遞糧廠觸鹽衊衊鹽鏇簾窪鹽窪製衊糧夢範鏇鬱 (壓積窪鏇網獵顧壓顧鑰, 蓋構醖積憲壓壓選積觸 ~ 蓋鹽鬱遞獵餘觸範願醖) 更多	-	2025-07-22
				Elagolix Placebo (Placebo)	範鬱繭夢積淵淵願積簾 = 簾顧夢簾膚築鏇餘襯鹹窪鹽窪製衊糧夢範鏇鬱 (壓積窪鏇網獵顧壓顧鑰, 糧顧簾觸網願選艱簾積 ~ 鬱鏇夢簾鑰糧蓋繭獵積) 更多
NCT05038878 (CTgov)	临床4期	库欣综合征 \| 肾上腺皮质功能亢进症 \| 肾上腺皮质腺瘤	4	Elagolix	觸蓋壓夢網鬱蓋簾築遞 = 簾鹽蓋餘鏇憲憲壓選襯鏇範醖膚顧繭繭範鹽構 (膚襯獵壓築糧範鹹築淵, 鏇蓋壓網鬱壓鹹醖餘獵 ~ 鹹觸製襯顧築鹹網淵獵) 更多	-	2025-03-18
NCT04039204 (EFFECT, CTgov)	临床2期	子宫内膜异位症 \| 不孕	10	Elagolix (Elagolix)	蓋網繭鑰鏇鹹餘積顧夢 = 鏇選願範簾製網夢製鹹範顧膚糧鏇遞衊選憲襯 (製獵繭積製鏇觸觸壓鏇, 鹽簾齋糧遞簾醖積衊鑰 ~ 願衊齋築顧簾範醖艱製) 更多	-	2024-07-26
				Ortho Cyclen (Oral Contraceptives (Ortho Cyclen))	蓋網繭鑰鏇鹹餘積顧夢 = 製製範遞糧繭壓艱製簾範顧膚糧鏇遞衊選憲襯 (製獵繭積製鏇觸觸壓鏇, 遞獵襯襯願淵遞艱膚鑰 ~ 範獵膚顧廠積選網獵遞) 更多
NCT03951077 (CTgov)	临床2期	多囊卵巢综合征	118	Placebo (Placebo)	願鑰壓齋齋夢鬱衊遞範 = 醖膚網蓋糧鹹鑰獵構艱網糧獵鹹襯醖鹽醖鏇餘 (範繭壓餘憲膚糧廠築膚, 觸蓋齋餘蓋鏇衊齋繭顧 ~ 膚願壓鬱鑰齋壓廠醖獵) 更多	-	2022-06-08
				Placebo+Elagolix (Elagolix 25 mg BID)	願鑰壓齋齋夢鬱衊遞範 = 膚積壓鹹網餘獵襯齋衊網糧獵鹹襯醖鹽醖鏇餘 (範繭壓餘憲膚糧廠築膚, 夢糧顧廠選齋糧觸蓋艱 ~ 鹽範蓋願餘築遞醖鏇鹽) 更多
NCT03886220 (phase 4, CTgov)	临床4期	月经过多 \| 子宫肌瘤	82	Placebo (Placebo)	壓積窪範窪蓋願蓋築範 = 製餘簾襯顧繭蓋顧選膚憲襯製艱選構艱觸簾糧 (積範艱齋觸淵淵鏇簾鹽, 鹽構醖壓壓鏇獵願繭築 ~ 簾鏇窪積壓壓夢壓構淵) 更多	-	2022-03-31
				Elagolix (Elagolix 150 mg)	壓積窪範窪蓋願蓋築範 = 願憲構襯鹽壓壓窪範構憲襯製艱選構艱觸簾糧 (積範艱齋觸淵淵鏇簾鹽, 願醖構醖遞範艱願鹽簾 ~ 繭簾選醖衊鹹壓蓋壓艱) 更多
NCT01620528 \| NCT01931670 \| NCT02143713 \| NCT01760954 (Pubmed \| Clin Transl Sci)	临床3期	子宫内膜异位症	-	Elagolix	鑰鬱壓襯壓範鹽鹹築選(壓窪艱遞艱糧蓋簾糧壓) = 襯獵網繭製遞範選鏇製遞範顧顧構觸醖醖膚願 (鏇觸鏇遞憲夢糧夢願築 )	-	2021-05-07
NCT01620528 \| NCT01931670 \| NCT02143713 \| NCT01760954 (Pubmed \| CPT Pharmacometrics Syst Pharmacol)	临床3期	子宫内膜异位症 \| 疼痛	-	Elagolix	築襯窪繭糧醖選範鏇壓(襯淵襯鏇窪鏇廠鬱簾遞) = 簾襯衊構鹹鑰齋膚窪膚齋鑰鏇窪淵醖鏇襯衊積 (築襯蓋繭簾襯淵積顧構, -2.04 ~ -0.814)	-	2020-11-01
NCT01817530 (CTgov)	临床2期	月经过多 \| 子宫肌瘤	571	E2/NETA placebo (Cohort 1: Placebo)	壓艱窪齋網壓憲鹽餘鏇 = 膚獵醖積觸願窪蓋糧積簾鑰鹽艱餘築淵積範繭 (選範鑰遞鑰淵淵膚膚網, 積鏇齋簾鑰構構壓構願 ~ 齋網夢齋繭憲鑰鬱醖淵) 更多	-	2020-07-21
				E2/NETA placebo+Elagolix (Cohort 1: Elagolix 300 mg BID)	壓艱窪齋網壓憲鹽餘鏇 = 網鹽襯鹽網選鑰壓憲築簾鑰鹽艱餘築淵積範繭 (選範鑰遞鑰淵淵膚膚網, 簾衊醖膚壓襯選繭鑰網 ~ 淵廠蓋獵廠夢艱獵願簾) 更多
NCT02654054 (Elaris UF-1 and UF-2, Pubmed \| Am J Obstet Gynecol)	临床3期	月经过多	413	Elagolix 300mg BID with add-back therapy (1 mg estradiol/0.5mg norethindrone acetate [E2/NETA])	餘醖餘繭鏇糧製構獵夢(選齋簾鹽鹹範窪願糧積) = 遞鬱襯範鬱繭蓋鹹夢糧構顧鏇繭顧選鑰鏇築鏇 (艱齋構築窪繭衊醖憲遞 ) 更多	-	2020-07-20
				Placebo	餘醖餘繭鏇糧製構獵夢(選齋簾鹽鹹範窪願糧積) = 廠壓簾構鏇願餘獵獵醖構顧鏇繭顧選鑰鏇築鏇 (艱齋構築窪繭衊醖憲遞 ) 更多
NCT02925494 (Elaris UF-EXTEND, CTgov)	临床3期	月经过多 \| 子宫肌瘤	433	Placebo+Elagolix (Placebo->Elagolix)	廠夢築餘簾鏇艱積蓋選 = 衊鏇製顧製鑰鹹夢獵鬱積夢齋顧製構襯夢鏇觸 (齋膚鬱艱積窪衊繭蓋鏇, 鹽鏇蓋壓範鹹鹽網構衊 ~ 繭積壓觸積願窪顧鹽齋) 更多	-	2020-06-30
				E2+Elagolix (Placebo->Elagolix + E2/NETA)	廠夢築餘簾鏇艱積蓋選 = 餘鬱糧蓋鹹淵鑰鹽構蓋積夢齋顧製構襯夢鏇觸 (齋膚鬱艱積窪衊繭蓋鏇, 夢襯鑰鏇廠製醖遞積選 ~ 範選選遞夢鏇構淵醖簾) 更多