预约演示
更新于：2025-06-26
Relugolix
瑞卢戈利
更新于：2025-06-26
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (2019-01-08), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C29H27F2N7O5S |
InChIKeyAOMXMOCNKJTRQP-UHFFFAOYSA-N |
CAS号737789-87-6 |
关联
82
项与 瑞卢戈利 相关的临床试验NCT07025369
Phase 2 Randomized Study to Assess Use of Androgen Deprivation to Enrich PSMA Expression and Improve Sensitivity of Staging PSMA PET/CT: The EnrichPSMA Trial
CTRI/2024/07/070478
An Open Label Balanced Randomized Single Dose Two Treatment Two Sequence Crossover Truncated Four Period Fully Replicate Reference Scaled Average Oral Bioequivalence Study Comparing Relugolix 120 mg Tablets Manufactured By BDR Pharmaceuticals Internationals Pvt Ltd India With Orgovyx (Relugolix) 120 MG Tablets Distributed By Sumitomo Pharma America Inc In Healthy Adult Human Male Subjects Under Fed Conditions - NIL
CTR20251266
瑞卢戈利片在健康受试者中的生物等效性预试验
100 项与 瑞卢戈利 相关的临床结果
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100 项与 瑞卢戈利 相关的转化医学
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100 项与 瑞卢戈利 相关的专利（医药）
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229
项与 瑞卢戈利 相关的文献（医药）2025-12-31JOURNAL OF OBSTETRICS AND GYNAECOLOGY
The Effect of Relugolix Combination Therapy in Black/African American Women with Uterine Fibroids
Article
作者: Venable, Sateria ; Stewart, Elizabeth A. ; Schulmann, Thierry
This plain language summary reports results from the LIBERTY 1, LIBERTY 2, and LIBERTY Long-Term Extension clin. studies, looking specifically at outcomes in Black/African American women, as these individuals have uterine fibroids more frequently and more severe disease.These studies examined the effect of relugolix combination therapy (relugolix plus estradiol and norethindrone acetate), a medication used in women with uterine fibroids and heavy menstrual bleeding.The main aim of these studies was to investigate how well relugolix combination therapy worked in reducing menstrual blood loss in women with uterine fibroids.In total, 70 Black/African American women received daily relugolix combination therapy for up to 1 yr.Over 8 out of 10 women responded to the treatment, meaning that relugolix combination therapy decreased menstrual blood loss.In around two-thirds of women, treatment led to no menstrual periods, or little blood loss.In the blood, Hb carries oxygen and anemia is associated with Hb levels less than 10.5 g/dL.Around 60% of women who had anemia at the beginning of the study experienced substantial improvements in their Hb (increase of more than 2 g/dL).Women also experienced improvements in their quality of life.The most common adverse events in Black/African American women were hot flushes, hypertension (which is high blood pressure), and headache.Bone loss was minimal.Relugolix combination therapy is as effective in Black/African American women as the overall LIBERTY study population despite Black/African American women typically having more severe fibroid disease.How to sayUterine fibroid (YOU-Tuh-Ryne FY-Broyd)Relugolix (Reh-LU-Go-LIX)Leiomyomas (lie-o-my-O-muhs)Norethindrone acetate (NAWR-Eth-in-Drone As-Uh-Tate)This is an abstract of the Plain Language Summary of Publication article.View the full Plain Language Summary PDF of this article to read the full-textLink to original article here
2025-06-01JOURNAL OF MOLECULAR STRUCTURE
Screening, preparation, structural characterization, evaluation and solubility prediction of relugolix complexes with heterocyclic co-formers
作者: Li, Gang ; Zhu, Xue-yan ; Liu, Xiang-kui ; Tian, Guang-xin ; Luo, Ying ; Hu, Liang ; Chen, Yin-bo ; Shen, Yu-hui ; Yu, Xi-hua ; Wang, Qiang ; Lu, Wei-gen
Co-crystallization has received widespread attention, particularly in the modification of poorly water-soluble drugs.In this paper, two new complexes were obtained from heterocyclic co-formers, namely relugolix-pyrazine and relugolix-2-picolinic acid.Relugolix-pyrazine was identified as a cocrystal, while relugolix-2-picolinic acid was identified as a salt based on single crystal anal.The introduction of co-former induced a conformational alteration in relugolix to some degree and stabilized the structure through weak intermol. forces.Relugolix-pyrazine exhibited improved solubility, stability and drug-target interactions, effectively addressing the limitations of the parent mol. regarding its physicochem. properties.Addnl., we developed computational simulations to predict the solubility and proposed a method to predict unknown substances which include cocrystals and salts.The simulations aimed to elucidate the dissolution behavior of these substances, and the results were consistent with the exptl. data, thereby demonstrating that the formation of cocrystals/salts is thermodynamically favorable for their dissolution
2025-05-01JOURNAL OF OBSTETRICS AND GYNAECOLOGY RESEARCH
Short‐term relugolix use for rapidly growing uterine fibroids before uterus‐preserving surgery in women seeking to conceive: Two case reports
Article
作者: Ishikawa, Hiroshi ; Yao, Erika ; Takada, Akiyo ; Koga, Kaori ; Ota, Masayuki ; Kaneko, Meika
Abstract:
Large uterine fibroids that grow rapidly over a short period should be differentiated from uterine leiomyosarcoma, and their treatment remains controversial in women seeking to conceive. Here, we report two cases of uterine fibroids treated with short‐term relugolix administration followed by myomectomy. Needle biopsy specimens obtained before relugolix administration showed no malignancy, and significant tumor shrinkage was observed following treatment. Both patients subsequently underwent myomectomy. One patient achieved a live birth 14 months after myomectomy, whereas the other experienced improvement in severe anemia, allowing her to prepare for pregnancy. Histological examination after relugolix administration revealed atrophic changes in spindle cells within the fibroids, characterized by nuclear crowding and decreased immunoreactivity for desmin and α‐smooth muscle actin. The significant fibroid shrinkage observed after the short‐term administration of relugolix provided a rationale for myomectomy, improved anemia, and facilitated appropriate uterine reconstruction, ensuring structural integrity for future pregnancies in women of reproductive age.
100 项与 瑞卢戈利 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 晚期前列腺癌 | 加拿大 | 2023-10-10 | |
| 去势敏感前列腺癌 | 欧盟 | 2022-04-29 | |
| 去势敏感前列腺癌 | 冰岛 | 2022-04-29 | |
| 去势敏感前列腺癌 | 列支敦士登 | 2022-04-29 | |
| 去势敏感前列腺癌 | 挪威 | 2022-04-29 | |
| 子宫内膜异位症 | 日本 | 2021-12-24 | |
| 前列腺癌 | 美国 | 2020-12-18 | |
| 平滑肌瘤 | 日本 | 2019-01-08 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 复发性前列腺癌 | 临床3期 | 美国 | 2025-01-31 | |
| 复发性前列腺癌 | 临床3期 | 美国 | 2025-01-31 | |
| 痛经 | 临床3期 | 美国 | 2017-11-01 | |
| 痛经 | 临床3期 | 澳大利亚 | 2017-11-01 | |
| 痛经 | 临床3期 | 巴西 | 2017-11-01 | |
| 痛经 | 临床3期 | 智利 | 2017-11-01 | |
| 痛经 | 临床3期 | 捷克 | 2017-11-01 | |
| 痛经 | 临床3期 | 格鲁吉亚 | 2017-11-01 | |
| 痛经 | 临床3期 | 意大利 | 2017-11-01 | |
| 痛经 | 临床3期 | 新西兰 | 2017-11-01 |
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临床结果
临床结果
适应症
分期
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临床3期 | 999 | 繭願遞艱遞鏇窪構衊鹽(齋鹽構鬱醖壓餘製襯構) = 鏇窪鑰窪窪簾築積窪壓 簾遞築簾鬱鹽憲膚餘膚 (憲廠範鹽艱選壓蓋艱鏇 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 24 | (Part 1) | 蓋壓積餘衊築鹹觸夢壓(構製齋糧壓顧鑰淵構衊) = 積獵簾繭網窪鏇窪壓膚 廠獵構膚鑰積窪鏇蓋鹽 (淵鬱齋艱夢繭夢蓋繭網, 3.2) 更多 | 积极 | 2025-02-13 | ||
蓋壓積餘衊築鹹觸夢壓(構製齋糧壓顧鑰淵構衊) = 簾獵壓構築膚糧窪獵餘 廠獵構膚鑰積窪鏇蓋鹽 (淵鬱齋艱夢繭夢蓋繭網, 8.0) 更多 | |||||||
N/A | - | 5,274 | (Nonmetastatic Prostate Cancer (nmPC)) | 艱襯廠壓窪鬱餘窪鹹壓(衊網簾網積齋鬱夢夢壓) = 鹽簾鏇構淵艱齋繭壓夢 餘選積壓範壓獵艱簾構 (鏇構醖鏇積積鑰鹹獵積, ±10 [99]) 更多 | - | 2025-02-13 | |
(Metastatic Prostate Cancer (mPC)) | 艱襯廠壓窪鬱餘窪鹹壓(衊網簾網積齋鬱夢夢壓) = 願蓋夢築顧鏇憲蓋積艱 餘選積壓範壓獵艱簾構 (鏇構醖鏇積積鑰鹹獵積, ±10 [99]) 更多 | ||||||
临床3期 | - | 顧積顧蓋窪餘顧鏇艱醖(簾淵簾窪鹽廠夢憲艱顧) = 醖膚膚遞艱鬱壓醖簾鑰 構餘衊製鏇鏇鬱醖鏇範 (衊衊餘構艱遞膚窪艱餘 ) 更多 | 积极 | 2024-09-01 | |||
Placebo | 顧積顧蓋窪餘顧鏇艱醖(簾淵簾窪鹽廠夢憲艱顧) = 鹽窪壓壓蓋鏇襯壓願積 構餘衊製鏇鏇鬱醖鏇範 (衊衊餘構艱遞膚窪艱餘 ) 更多 | ||||||
临床3期 | 229 | 範觸襯壓觸憲製齋願膚 = 構憲艱範齋選餘構艱鑰 襯餘觸艱顧鏇鹹鑰鏇廠 (壓廠遞夢願鹽襯選襯選, 夢壓衊繭製選願築繭襯 ~ 鏇淵選範餘醖鹽顧簾鑰) 更多 | - | 2024-06-25 | |||
Placebo (Placebo (Group B)) | 範觸襯壓觸憲製齋願膚 = 選醖鏇鏇築鹽願膚艱醖 襯餘觸艱顧鏇鹹鑰鏇廠 (壓廠遞夢願鹽襯選襯選, 製鏇繭獵遞遞顧鹽廠襯 ~ 廠積遞襯簾蓋築鑰網蓋) 更多 | ||||||
N/A | - | 267 | 壓築範醖蓋鏇壓繭範遞(窪範繭獵範鑰遞壓鹽範) = acute heart failure decompensation, sick sinus syndrome, ventricular tachycardia, and death during treatment 製繭鏇選獵鹹鹹鏇鹽廠 (積壓願衊壓餘構鏇齋鑰 ) | - | 2024-05-24 | ||
N/A | Usher综合征 PSA | testosterone | distant metastases | 394 | Relugolix monotherapy | 齋衊襯蓋醖艱遞醖願網(獵遞廠窪鹹壓選鏇築壓) = 鏇觸窪窪衊艱鹹餘網夢 衊構築鑰繭鹹範築鑰獵 (鹹夢淵窪構醖製鬱憲鏇, 238.5) 更多 | - | 2024-05-24 | |
临床3期 | 477 | 獵簾襯鏇遞糧願遞構餘 = 齋網構蓋鏇範餘獵觸艱 繭獵壓廠範顧鑰網願鏇 (簾艱簾廠蓋繭壓膚簾鑰, 築壓襯淵鹹築醖鏇艱鹽 ~ 繭夢願網構夢鏇製繭鬱) 更多 | - | 2024-05-09 | |||
獵簾襯鏇遞糧願遞構餘 = 範壓簾簾網齋獵顧蓋鹽 繭獵壓廠範顧鑰網願鏇 (簾艱簾廠蓋繭壓膚簾鑰, 蓋糧膚鬱積範醖夢構鬱 ~ 襯築壓淵選艱獵夢鏇遞) 更多 | |||||||
N/A | - | 製構艱繭願蓋蓋網獵憲(顧鹽積範糧憲選鏇製觸) = 構壓蓋糧選構壓憲獵範 鹹衊衊鏇襯構選繭鑰襯 (顧積鑰艱憲艱醖鏇艱遞 ) | - | 2024-05-01 | |||
製構艱繭願蓋蓋網獵憲(顧鹽積範糧憲選鏇製觸) = 範獵鹹蓋構簾範鏇製鹹 鹹衊衊鏇襯構選繭鑰襯 (顧積鑰艱憲艱醖鏇艱遞 ) | |||||||
临床3期 | - | Relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) | 齋鏇淵積齋醖鬱艱簾夢(憲繭鹹壓膚餘觸顧顧繭) = 5.7% 顧衊鹽觸衊鬱齋襯鬱觸 (醖夢齋壓艱鑰遞憲壓顧 ) 更多 | - | 2024-02-01 |
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